recent publications
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academic article
- Guerrero, M., Urbano, M., Kim, E. K., Gamo, A. M., Riley, S., Abgaryan, L., Leaf, N., Van Orden, L. J., Brown, S. J., Xie, J. Y., Porreca, F., Cameron, M. D., et al. Design and synthesis of a novel and selective kappa opioid receptor (KOR) antagonist (BTRX-335140) Journal of Medicinal Chemistry 2019 62:1761-1780 DOI:10.1021/acs.jmedchem.8b01679 PMID:30707578 PMCID:PMC6395531
- Morgan, G. J., Yan, N. L., Mortenson, D. E., Rennella, E., Blundon, J. M., Gwin, R. M., Lin, C. Y., Stanfield, R. L., Brown, S. J., Rosen, H., Spicer, T. P., Fernandez-Vega, V., et al. Stabilization of amyloidogenic immunoglobulin light chains by small molecules Proceedings of the National Academy of Sciences of the United States of America 2019 116:8360-8369 DOI:10.1073/pnas.1817567116 PMID:30971495 PMCID:PMC6486714
- Baillargeon, P., Fernandez-Vega, V., Sridharan, B. P., Brown, S., Griffin, P. R., Rosen, H., Cravatt, B., Scampavia, L., Spicer, T. P. The Scripps Molecular Screening Center and Translational Research Institute SLAS Discovery 2019 24:386-397 DOI:10.1177/2472555218820809 PMID:30682260
- Huppe, C. A., Lecours, P. B., Lechasseur, A., Gendron, D. R., Lemay, A. M., Bissonnette, E. Y., Blanchet, M. R., Duchaine, C., Morissette, M. C., Rosen, H., Marsolais, D. A sphingosine-1-phosphate receptor 1 agonist inhibits tertiary lymphoid tissue reactivation and hypersensitivity in the lung Mucosal Immunology 2018 11:112-119 DOI:10.1038/mi.2017.37 PMID:28422187
- Ogasawara, D., Ichu, T. A., Vartabedian, V. F., Benthuysen, J., Jing, H., Reed, A., Ulanovskaya, O. A., Hulce, J. J., Roberts, A., Brown, S., Rosen, H., Teijaro, J. R., et al. Selective blockade of the lyso-PS lipase ABHD12 stimulates immune responses in vivo Nature Chemical Biology 2018 14:1099-1108 DOI:10.1038/s41589-018-0155-8 PMID:30420694 PMCID:PMC6263940
- Hur, W., Rosen, H., Gray, N. S. A benzo[b]thiophene-based selective type 4 S1P receptor agonist Bioorganic & Medicinal Chemistry Letters 2017 27:1-5 DOI:10.1016/j.bmcl.2016.11.050 PMID:27894870
- Xie, J. Y., De Felice, M., Kopruszinski, C. M., Eyde, N., LaVigne, J., Remeniuk, B., Hernandez, P., Yue, X., Goshima, N., Ossipov, M., King, T., Streicher, J. M., et al. Kappa opioid receptor antagonists: A possible new class of therapeutics for migraine prevention Cephalalgia 2017 37:780-794 DOI:10.1177/0333102417702120 PMID:28376659
- Marro, B. S., Ware, B. C., Zak, J., de la Torre, J. C., Rosen, H., Oldstone, M. B. A. Progression of type 1 diabetes from the prediabetic stage is controlled by interferon-α signaling Proceedings of the National Academy of Sciences of the United States of America 2017 114:3708-3713 DOI:10.1073/pnas.1700878114 PMID:28325871 PMCID:PMC5389329
- Skerry, C., Scanlon, K., Ardanuy, J., Roberts, D., Zhang, L., Rosen, H., Carbonetti, N. H. Reduction of pertussis inflammatory pathology by therapeutic treatment with sphingosine-1-phosphate receptor ligands by a pertussis toxin-insensitive mechanism Journal of Infectious Diseases 2017 215:278-286 DOI:10.1093/infdis/jiw536 PMID:27815382
- Tran, J. Q., Hartung, J. P., Peach, R. J., Boehm, M. F., Rosen, H., Smith, H., Brooks, J. L., Timony, G. A., Olson, A. D., Gujrathi, S., Frohna, P. A. Results from the first-in-human study with ozanimod, a novel, selective sphingosine-1-phosphate receptor modulator Journal of Clinical Pharmacology 2017 57:988-996 DOI:10.1002/jcph.887 PMID:28398597 PMCID:PMC5516232
- Yung, B. S., Brand, C. S., Xiang, S. Y., Gray, C. B. B., Means, C. K., Rosen, H., Chun, J., Purcell, N. H., Brown, J. H., Miyamoto, S. Selective coupling of the S1P3 receptor subtype to S1P-mediated RhoA activation and cardioprotection Journal of Molecular and Cellular Cardiology 2017 103:1-10 DOI:10.1016/j.yjmcc.2016.12.008 PMID:28017639
- Dusaban, S. S., Chun, J., Rosen, H., Purcell, N. H., Brown, J. H. Sphingosine 1-phosphate receptor 3 and RhoA signaling mediate inflammatory gene expression in astrocytes Journal of Neuroinflammation 2017 14 DOI:10.1186/s12974-017-0882-x PMID:28577576 PMCID:PMC5455202
- Karuppuchamy, T., Behrens, E. H., Gonzalez-Cabrera, P., Sarkisyan, G., Gima, L., Boyer, J. D., Bamias, G., Jedlicka, P., Veny, M., Clark, D., Peach, R., Scott, F., et al. Sphingosine-1-phosphate receptor-1 (S1P1) is expressed by lymphocytes, dendritic cells, and endothelium and modulated during inflammatory bowel disease Mucosal Immunology 2017 10:162-171 DOI:10.1038/mi.2016.35 PMID:27049060 PMCID:PMC5053832
- Song, J., Dagan, A., Yakhtin, Z., Gatt, S., Riley, S., Rosen, H., Or, R., Almogi-Hazan, O. The novel sphingosine-1-phosphate receptors antagonist AD2900 affects lymphocyte activation and inhibits T-cell entry into the lymph nodes Oncotarget 2017 8:53563-53580 DOI:10.18632/oncotarget.18626
- Horning, B. D., Suciu, R. M., Ghadiri, D. A., Ulanovskaya, O. A., Matthews, M. L., Lum, K. M., Backus, K. M., Brown, S. J., Rosen, H., Cravatt, B. F. Chemical proteomic profiling of human methyltransferases Journal of the American Chemical Society 2016 138:13335-13343 DOI:10.1021/jacs.6b07830 PMID:27689866 PMCID:PMC5072128
- Ewing, H., Fernandez-Vega, V., Spicer, T. P., Chase, P., Brown, S., Scampavia, L., Roush, W. R., Riley, S., Rosen, H., Hodder, P., Lambeau, G., Gelb, M. H. Fluorometric high-throughput screening assay for secreted phospholipases A(2) using phospholipid vesicles Journal of Biomolecular Screening 2016 21:713-721 DOI:10.1177/1087057116646742 PMID:27146384
- Johnson, J. L., Ramadass, M., He, J., Brown, S. J., Zhang, J., Abgaryan, L., Biris, N., Gavathiotis, E., Rosen, H., Catz, S. D. Identification of neutrophil exocytosis inhibitors (Nexinhibs), small molecule inhibitors of neutrophil exocytosis and inflammation: druggability of the small GTPase Rab27a Journal of Biological Chemistry 2016 291:25965-25982 DOI:10.1074/jbc.M116.741884 PMID:27702998 PMCID:PMC5207069
- Scott, F. L., Clemons, B., Brooks, J., Brahmachary, E., Powell, R., Dedman, H., Desale, H. G., Timony, G. A., Martinborough, E., Rosen, H., Roberts, E., Boehm, M. F., et al. Ozanimod (RPC1063) is a potent sphingosine-1-phosphate receptor-1 (S1P(1)) and receptor-5 (S1P(5)) agonist with autoimmune disease-modifying activity British Journal of Pharmacology 2016 173:1778-1792 DOI:10.1111/bph.13476 PMID:26990079 PMCID:PMC4867749
- Teijaro, J. R., Studer, S., Leaf, N., Kiosses, W. B., Nguyen, N., Matsuki, K., Negishi, H., Taniguchi, T., Oldstone, M. B. A., Rosen, H. S1PR1-mediated IFNAR1 degradation modulates plasmacytoid dendritic cell interferon-alpha autoamplification Proceedings of the National Academy of Sciences of the United States of America 2016 113:1351-1356 DOI:10.1073/pnas.1525356113 PMID:26787880 PMCID:PMC4747766
- Plate, L., Cooley, C. B., Chen, J. J., Paxman, R. J., Gallagher, C. M., Madoux, F., Genereux, J. C., Dobbs, W., Garza, D., Spicer, T. P., Scampavia, L., Brown, S. J., et al. Small molecule proteostasis regulators that reprogram the ER to reduce extracellular protein aggregation ELife 2016 5 DOI:10.7554/eLife.15550 PMID:27435961 PMCID:PMC4954754
- Sanna, M. G., Vincent, K. P., Repetto, E., Nguyen, N., Brown, S. J., Abgaryan, L., Riley, S. W., Leaf, N. B., Cahalan, S. M., Kiosses, W. B., Kohno, Y., Brown, J. H., et al. Bitopic sphingosine 1-phosphate receptor 3 (S1P3) antagonist rescue from complete heart block: pharmacological and genetic evidence for direct S1P3 regulation of mouse cardiac conduction Molecular Pharmacology 2016 89:176-186 DOI:10.1124/mol.115.100222 PMID:26494861 PMCID:PMC4702096
- Niphakis, M. J., Lum, K. M., Cognetta III, A. B., Correia, B. E., Ichu, T. A., Olucha, J., Brown, S. J., Kundu, S., Piscitelli, F., Rosen, H., Cravatt, B. F. A global map of lipid-binding proteins and their ligandability in cells Cell 2015 161:1668-1680 DOI:10.1016/j.cell.2015.05.045 PMID:26091042 PMCID:PMC4615699
- Schreiber, S. L., Kotz, J. D., Li, M., Aube, J., Austin, C. P., Reed, J. C., Rosen, H., White, E. L., Sklar, L. A., Lindsley, C. W., Alexander, B. R., Bittker, J. A., et al. Advancing biological understanding and therapeutics discovery with small-molecule probes Cell 2015 161:1252-1265 DOI:10.1016/j.cell.2015.05.023 PMID:26046436 PMCID:PMC4564295
- Chang, J. W., Zuhl, A. M., Speers, A. E., Niessen, S., Brown, S. J., Mulvihill, M. M., Fan, Y. C., Spicer, T. P., Southern, M., Scampavia, L., Fernandez-Vega, V., Dix, M. M., et al. Selective inhibitor of platelet-activating factor acetylhydrolases 1b2 and 1b3 that impairs cancer cell survival ACS Chemical Biology 2015 10:925-932 DOI:10.1021/cb500893q PMID:25602368 PMCID:PMC4402257
- Skerry, C., Scanlon, K., Rosen, H., Carbonetti, N. H. Sphingosine-1-phosphate receptor agonism reduces Bordetella pertussis-mediated lung pathology Journal of Infectious Diseases 2015 211:1883-1886 DOI:10.1093/infdis/jiu823 PMID:25538274 PMCID:PMC4836722
- Blanc, C. A., Grist, J. J., Rosen, H., Sears-Kraxberger, I., Steward, O., Lane, T. E. Sphingosine-1-phosphate receptor antagonism enhances proliferation and migration of engrafted neural progenitor cells in a model of viral-induced demyelination American Journal of Pathology 2015 185:2819-2832 DOI:10.1016/j.ajpath.2015.06.009 PMID:26435414 PMCID:PMC4607760
- Zhao, N., Darby, C. M., Small, J., Bachovchin, D. A., Jiang, X., Burns-Huang, K. E., Botella, H., Ehrt, S., Boger, D. L., Anderson, E. D., Cravatt, B. F., Speers, A. E., et al. Target-based screen against a periplasmic serine protease that regulates intrabacterial pH homeostasis in Mycobacterium tuberculosis ACS Chemical Biology 2015 10:364-371 DOI:10.1021/cb500746z PMID:25457457 PMCID:PMC4340348
- Walsh, K. B., Teijaro, J. R., Brock, L. G., Fremgen, D. M., Collins, P. L., Rosen, H., Oldstone, M. B. A. Animal model of respiratory syncytial virus: CD8(+) T cells cause a cytokine storm that is chemically tractable by sphingosine-1-phosphate 1 receptor agonist therapy Journal of Virology 2014 88:6281-6293 DOI:10.1128/jvi.00464-14 PMID:24672024
- Urbano, M., Guerrero, M., Rosen, H., Roberts, E. Antagonists of the kappa opioid receptor Bioorganic & Medicinal Chemistry Letters 2014 24:2021-2032 DOI:10.1016/j.bmcl.2014.03.040 PMID:24690494
- Oldstone, M. B. A., Rosen, H. Cytokine storm plays a direct role in the morbidity and mortality from influenza virus infection and is chemically treatable with a single sphingosine-1-phosphate agonist molecule Current Topics in Microbiology and Immunology 2014 378:129-147 DOI:10.1007/978-3-319-05879-5_6 PMID:24728596
- Blanc, C. A., Rosen, H., Lane, T. E. FTY720 (fingolimod) modulates the severity of viral-induced encephalomyelitis and demyelination Journal of Neuroinflammation 2014 11:138 DOI:10.1186/s12974-014-0138-y PMID:25138356 PMCID:PMC4148542
- Sarkisyan, G., Gay, L. J., Nguyen, N., Felding, B. H., Rosen, H. Host endothelial S1PR(1) regulation of vascular permeability modulates tumor growth American Journal of Physiology-Cell Physiology 2014 307:C14-C24 DOI:10.1152/ajpcell.00043.2014 PMID:24740542 PMCID:PMC4080184
- Teijaro, J. R., Walsh, K. B., Rice, S., Rosen, H., Oldstone, M. B. A. Mapping the innate signaling cascade essential for cytokine storm during influenza virus infection Proceedings of the National Academy of Sciences of the United States of America 2014 111:3799-3804 DOI:10.1073/pnas.1400593111 PMID:24572573 PMCID:PMC3956176
- Teijaro, J. R., Walsh, K. B., Long, J. P., Tordoff, K. P., Stark, G. V., Eisfeld, A. J., Kawaoka, Y., Rosen, H., Oldstone, M. B. A. Protection of ferrets from pulmonary injury due to H1N1 2009 influenza virus infection: immunopathology tractable by sphingosine-1-phosphate 1 receptor agonist therapy Virology 2014 452:152-157 DOI:10.1016/j.virol.2014.01.003 PMID:24606692 PMCID:PMC3954990
- Chang, M. R., Rosen, H., Griffin, P. R. RORs in autoimmune disease Current Topics in Microbiology and Immunology 2014 378:171-182 DOI:10.1007/978-3-319-05879-5_8 PMID:24728598
- Ohotski, J., Rosen, H., Bittman, R., Pyne, S., Pyne, N. J. Sphingosine kinase 2 prevents the nuclear translocation of sphingosine 1-phosphate receptor-2 and tyrosine 416 phosphorylated c-Src and increases estrogen receptor negative MDA-MB-231 breast cancer cell growth: the role of sphingosine 1-phosphate receptor-4 Cellular Signalling 2014 26:1040-1047 DOI:10.1016/j.cellsig.2014.01.023 PMID:24486401
- Rosen, H., Sanna, M. G., Gonzalez-Cabrera, P. J., Roberts, E. The organization of the sphingosine 1-phosphate signaling system Current Topics in Microbiology and Immunology 2014 378:1-21 DOI:10.1007/978-3-319-05879-5_1 PMID:24728591
- Cisar, E. A. G., Nguyen, N., Rosen, H. A GTP affinity probe for proteomics highlights flexibility in purine nucleotide selectivity Journal of the American Chemical Society 2013 135:4676-4679 DOI:10.1021/ja400839e PMID:23473570
- Hulleman, J. D., Brown, S. J., Rosen, H., Kelly, J. W. A high-throughput cell-based Gaussia luciferase reporter assay for identifying modulators of fibulin-3 secretion Journal of Biomolecular Screening 2013 18:647-658 DOI:10.1177/1087057112469405 PMID:23230284 PMCID:PMC4435789
- Satsu, H., Schaeffer, M. T., Guerrero, M., Saldana, A., Eberhart, C., Hodder, P., Cayanan, C., Schurer, S., Bhhatarai, B., Roberts, E., Rosen, H., Brown, S. J. A sphingosine 1-phosphate receptor 2 selective allosteric agonist Bioorganic & Medicinal Chemistry 2013 21:5373-5382 DOI:10.1016/j.bmc.2013.06.012 PMID:23849205 PMCID:PMC3786410
- Guerrero, M., Poddutoori, R., Urbano, M., Peng, X., Spicer, T. P., Chase, P. S., Hodder, P. S., Schaeffer, M. T., Brown, S., Rosen, H., Roberts, E. Discovery, design and synthesis of a selective S1P(3) receptor allosteric agonist Bioorganic & Medicinal Chemistry Letters 2013 23:6346-6349 DOI:10.1016/j.bmcl.2013.09.075 PMID:24135724 PMCID:PMC3963471
- Oldstone, M. B. A., Teijaro, J. R., Walsh, K. B., Rosen, H. Dissecting influenza virus pathogenesis uncovers a novel chemical approach to combat the infection Virology 2013 435:92-101 DOI:10.1016/j.virol.2012.09.039 PMID:23217619 PMCID:PMC3523270
- Urbano, M., Guerrero, M., Rosen, H., Roberts, E. Modulators of the Sphingosine 1-phosphate receptor 1 Bioorganic & Medicinal Chemistry Letters 2013 23:6377-6389 DOI:10.1016/j.bmcl.2013.09.058 PMID:24125884 PMCID:PMC3926431
- Guerrero, M., Urbano, M., Schaeffer, M. T., Brown, S., Rosen, H., Roberts, E. SAR analysis of novel non-peptidic NPBWR1 (GPR7) antagonists Bioorganic & Medicinal Chemistry Letters 2013 23:614-619 DOI:10.1016/j.bmcl.2012.12.030 PMID:23287738 PMCID:PMC3621982
- Nagano, J. M. G., Hsu, K. L., Whitby, L. R., Niphakis, M. J., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Hodder, P., Srinivasan, P., Gonzalez, T. D., et al. Selective inhibitors and tailored activity probes for lipoprotein-associated phospholipase A(2) Bioorganic & Medicinal Chemistry Letters 2013 23:839-843 DOI:10.1016/j.bmcl.2012.11.061 PMID:23260346 PMCID:PMC3549684
- Cahalan, S. M., Gonzalez-Cabrera, P. J., Nguyen, N., Guerrero, M., Cisar, E. A. G., Leaf, N. B., Brown, S. J., Roberts, E., Rosen, H. Sphingosine 1-phosphate receptor 1 (S1P(1)) upregulation and amelioration of experimental autoimmune encephalomyelitis by an S1P(1) antagonist Molecular Pharmacology 2013 83:316-321 DOI:10.1124/mol.112.082958 PMID:23204443 PMCID:PMC3558813
- Roberts, E., Guerrero, M., Urbano, M., Rosen, H. Sphingosine 1-phosphate receptor agonists: A patent review (2010 - 2012) Expert Opinion on Therapeutic Patents 2013 23:817-841 DOI:10.1517/13543776.2013.783022 PMID:23541049
- Rosen, H., Stevens, R. C., Hanson, M., Roberts, E., Oldstone, M. B. A. Sphingosine-1-phosphate and its receptors: Structure, signaling, and influence Annual Review of Biochemistry 2013 82:637-662 DOI:10.1146/annurev-biochem-062411-130916 PMID:23527695
- Stevens, R. C., Cherezov, V., Katritch, V., Abagyan, R., Kuhn, P., Rosen, H., Wuthrich, K. The GPCR Network: a large-scale collaboration to determine human GPCR structure and function Nature Reviews Drug Discovery 2013 12:25-34 DOI:10.1038/nrd3859 PMID:23237917 PMCID:PMC3723354
- Matheu, M. P., Teijaro, J. R., Walsh, K. B., Greenberg, M. L., Marsolais, D., Parker, I., Rosen, H., Oldstone, M. B. A., Cahalan, M. D. Three phases of CD8 T cell response in the lung following H1N1 influenza infection and sphingosine 1 phosphate agonist therapy PLoS One 2013 8:e58033 DOI:10.1371/journal.pone.0058033 PMID:23533579 PMCID:PMC3606384
- Adibekian, A., Martin, B. R., Chang, J. W., Hsu, K. L., Tsuboi, K., Bachovchin, D. A., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Hodder, P. S., et al. Confirming target engagement for reversible inhibitors in vivo by kinetically tuned activity-based probes Journal of the American Chemical Society 2012 134:10345-10348 DOI:10.1021/ja303400u PMID:22690931 PMCID:PMC3392194
- Hanson, M. A., Roth, C. B., Jo, E. J., Griffith, M. T., Scott, F. L., Reinhart, G., Desale, H., Clemons, B., Cahalan, S. M., Schuerer, S. C., Sanna, M. G., Han, G. W., et al. Crystal structure of a lipid G protein-coupled receptor Science 2012 335:851-855 DOI:10.1126/science.1215904 PMID:22344443 PMCID:PMC3338336
- Urbano, M., Guerrero, M., Zhao, J., Velaparthi, S., Saldanha, S. A., Chase, P., Wang, Z. W., Civelli, O., Hodder, P., Schaeffer, M. T., Brown, S., Rosen, H., et al. Design, synthesis and SAR analysis of novel potent and selective small molecule antagonists of NPBWR1 (GPR7) Bioorganic & Medicinal Chemistry Letters 2012 22:7135-7141 DOI:10.1016/j.bmcl.2012.09.074 PMID:23079522 PMCID:PMC3601546
- Guerrero, M., Urbano, M., Zhao, J., Crisp, M., Chase, P., Hodder, P., Schaeffer, M. T., Brown, S., Rosen, H., Roberts, E. Discovery, design and synthesis of novel potent and selective sphingosine-1-phosphate 4 receptor (s1p(4)-r) agonists Bioorganic & Medicinal Chemistry Letters 2012 22:537-542 DOI:10.1016/j.bmcl.2011.10.096 PMID:22119461 PMCID:PMC3248976
- Dillon, M. B. C., Bachovchin, D. A., Brown, S. J., Finn, M. G., Rosen, H., Cravatt, B. F., Mowen, K. A. Novel inhibitors for PRMT1 discovered by high-throughput screening using activity-based fluorescence polarization ACS Chemical Biology 2012 7:1198-1204 DOI:10.1021/cb300024c PMID:22506763 PMCID:PMC3401332
- Jo, E. J., Bhhatarai, B., Repetto, E., Guerrero, M., Riley, S., Brown, S. J., Kohno, Y., Roberts, E., Schurer, S. C., Rosen, H. Novel selective allosteric and bitopic ligands for the S1P(3) receptor ACS Chemical Biology 2012 7:1975-1983 DOI:10.1021/cb300392z PMID:22971058 PMCID:PMC3528827
- Sarkisyan, G., Cahalan, S. M., Gonzalez-Cabrera, P. J., Leaf, N. B., Rosen, H. Real-time differential labeling of blood, interstitium, and lymphatic and single-field analysis of vasculature dynamics in vivo American Journal of Physiology-Cell Physiology 2012 302:C1460-C1468 DOI:10.1152/ajpcell.00382.2011 PMID:22357735
- Gonzalez-Cabrera, P. J., Cahalan, S. M., Nguyen, N., Sarkisyan, G., Leaf, N. B., Cameron, M. D., Kago, T., Rosen, H. S1P(1) receptor modulation with cyclical recovery from lymphopenia ameliorates mouse model of multiple sclerosis Molecular Pharmacology 2012 81:166-174 DOI:10.1124/mol.111.076109 PMID:22031473 PMCID:PMC3263953
- Lone, A. M., Bachovchin, D. A., Westwood, D. B., Speers, A. E., Spicer, T. P., Fernandez-Vega, V., Chase, P., Hodder, P. S., Rosen, H., Cravatt, B. F., Saghatelian, A. A substrate-free activity-based protein profiling screen for the discovery of selective PREPL inhibitors Journal of the American Chemical Society 2011 133:11665-11674 DOI:10.1021/ja2036095 PMID:21692504 PMCID:PMC3145007
- Bachovchin, D. A., Mohr, J. T., Speers, A. E., Wang, C., Berlin, J. M., Spicer, T. P., Fernandez-Vega, V., Chase, P., Hodder, P. S., Schurer, S. C., Nomura, D. K., Rosen, H., et al. Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors Proceedings of the National Academy of Sciences of the United States of America 2011 108:6811-6816 DOI:10.1073/pnas.1015248108 PMID:21398589 PMCID:PMC3084096
- Cahalan, S. M., Gonzalez-Cabrera, P. J., Sarkisyan, G., Nguyen, N., Schaeffer, M. T., Huang, L. M., Yeager, A., Clemons, B., Scott, F., Rosen, H. Actions of a picomolar short-acting S1P(1) agonist in S1P(1)-eGFP knock-in mice Nature Chemical Biology 2011 7:254-256 DOI:10.1038/nchembio.547 PMID:21445057 PMCID:PMC3430385
- Bachovchin, D. A., Zuhl, A. M., Speers, A. E., Wolfe, M. R., Weerapana, E., Brown, S. J., Rosen, H., Cravatt, B. F. Discovery and optimization of sulfonyl acrylonitriles as selective, covalent inhibitors of protein phosphatase methylesterase-1 Journal of Medicinal Chemistry 2011 54:5229-5236 DOI:10.1021/jm200502u PMID:21639134 PMCID:PMC3144155
- Guerrero, M., Urbano, M., Velaparthi, S., Zhao, J., Schaeffer, M. T., Brown, S., Rosen, H., Roberts, E. Discovery, design and synthesis of the first reported potent and selective sphingosine-1-phosphate 4 (s1p(4)) receptor antagonists Bioorganic & Medicinal Chemistry Letters 2011 21:3632-3636 DOI:10.1016/j.bmcl.2011.04.097 PMID:21570287 PMCID:PMC3107912
- Urbano, M., Guerrero, M., Velaparthi, S., Crisp, M., Chase, P., Hodder, P., Schaeffer, M. T., Brown, S., Rosen, H., Roberts, E. Discovery, synthesis and sar analysis of novel selective small molecule s1p(4)-r agonists based on a (2z,5z)-5-((pyrrol-3-yl)methylene)-3-alkyl-2-(alkylimino)thiazolidin-4-o ne chemotype Bioorganic & Medicinal Chemistry Letters 2011 21:6739-6745 DOI:10.1016/j.bmcl.2011.09.049 PMID:21982495 PMCID:PMC3209756
- Teijaro, J. R., Walsh, K. B., Cahalan, S., Fremgen, D. M., Roberts, E., Scott, F., Martinborough, E., Peach, R., Oldstone, M. B. A., Rosen, H. Endothelial cells are central orchestrators of cytokine amplification during influenza virus infection Cell 2011 146:979-990 DOI:10.1016/j.cell.2011.08.015 PMID:21925319 PMCID:PMC3176439
- Rillahan, C. D., Brown, S. J., Register, A. C., Rosen, H., Paulson, J. C. High-throughput screening for inhibitors of sialyl- and fucosyltransferases Angewandte Chemie-International Edition 2011 50:12534-12537 DOI:10.1002/anie.201105065 PMID:22095645 PMCID:PMC3245354
- Marsolais, D., Yagi, S., Kago, T., Leaf, N., Rosen, H. Modulation of chemokines and allergic airway inflammation by selective local sphingosine-1-phosphate receptor 1 agonism in lungs Molecular Pharmacology 2011 79:61-68 DOI:10.1124/mol.110.066811 PMID:20935081 PMCID:PMC3014274
- Tsuboi, K., Bachovchin, D. A., Speers, A. E., Spicer, T. P., Fernandez-Vega, V., Hodder, P., Rosen, H., Cravatt, B. F. Potent and selective inhibitors of glutathione S-transferase omega 1 that impair cancer drug resistance Journal of the American Chemical Society 2011 133:16605-16616 DOI:10.1021/ja2066972 PMID:21899313 PMCID:PMC3226709
- Walsh, K. B., Teijaro, J. R., Rosen, H., Oldstone, M. B. A. Quelling the storm: Utilization of sphingosine-1-phosphate receptor signaling to ameliorate influenza virus-induced cytokine storm Immunologic Research 2011 51:15-25 DOI:10.1007/s12026-011-8240-z PMID:21901448
- Chou, T. F., Brown, S. J., Minond, D., Nordin, B. E., Li, K. L., Jones, A. C., Chase, P., Porubsky, P. R., Stoltz, B. M., Schoenen, F. J., Patricelli, M. P., Hodder, P., et al. Reversible inhibitor of p97, dbeq, impairs both ubiquitin-dependent and autophagic protein clearance pathways Proceedings of the National Academy of Sciences of the United States of America 2011 108:4834-4839 DOI:10.1073/pnas.1015312108 PMID:21383145 PMCID:PMC3064330
- Urbano, M., Guerrero, M., Zhao, J., Velaparthi, S., Schaeffer, M. T., Brown, S., Rosen, H., Roberts, E. Sar analysis of innovative selective small molecule antagonists of sphingosine-1-phosphate 4 (s1p(4)) receptor Bioorganic & Medicinal Chemistry Letters 2011 21:5470-5474 DOI:10.1016/j.bmcl.2011.06.132 PMID:21783362 PMCID:PMC3159836
- Walsh, K. B., Teijaro, J. R., Wilker, P. R., Jatzek, A., Fremgen, D. M., Das, S. C., Watanabe, T., Hatta, M., Shinya, K., Suresh, M., Kawaoka, Y., Rosen, H., et al. Suppression of cytokine storm with a sphingosine analog provides protection against pathogenic influenza virus Proceedings of the National Academy of Sciences of the United States of America 2011 108:12018-12023 DOI:10.1073/pnas.1107024108 PMID:21715659 PMCID:PMC3142000
- Knuckley, B., Jones, J. E., Bachovchin, D. A., Slack, J., Causey, C. P., Brown, S. J., Rosen, H., Cravatt, B. F., Thompson, P. R. A fluopol-ABPP HTS assay to identify PAD inhibitors Chemical Communications 2010 46:7175-7177 DOI:10.1039/c0cc02634d PMID:20740228 PMCID:PMC2943038
- Gianni, D., Taulet, N., Zhang, H., DerMardirossian, C., Kister, J., Martinez, L., Roush, W. R., Brown, S. J., Bokoch, G. M., Rosen, H. A novel and specific NADPH oxidase-1 (Nox1) small-molecule inhibitor blocks the formation of functional invadopodia in human colon cancer cells ACS Chemical Biology 2010 5:981-993 DOI:10.1021/cb100219n PMID:20715845 PMCID:PMC2955773
- Bachovchin, D. A., Wolfe, M. R., Masuda, K., Brown, S. J., Spicer, T. P., Fernandez-Vega, V., Chase, P., Hodder, P. S., Rosen, H., Cravatt, B. F. Oxime esters as selective, covalent inhibitors of the serine hydrolase retinoblastoma-binding protein 9 (RBBP9) Bioorganic & Medicinal Chemistry Letters 2010 20:2254-2258 DOI:10.1016/j.bmcl.2010.02.011 PMID:20207142 PMCID:PMC2843764
- Walsh, K. B., Marsolais, D., Welch, M. J., Rosen, H., Oldstone, M. B. A. Treatment with a sphingosine analog does not alter the outcome of a persistent virus infection Virology 2010 397:260-269 DOI:10.1016/j.virol.2009.08.043 PMID:19962171 PMCID:PMC2821988
- Cahalan, S., Rosen, H. S1P1 signaling just keeps going and going and going Nature Chemical Biology 2009 5:377-378 DOI:10.1038/nchembio0609-377 PMID:19448604
- Goldsmith, M., Avni, D., Levy-Rimler, G., Mashiach, R., Ernst, O., Levi, M., Webb, B., Meijler, M. M., Gray, N. S., Rosen, H., Zor, T. A ceramide-1-phosphate analogue, pcera-1, simultaneously suppresses tumour necrosis factor-alpha and induces interleukin-10 production in activated macrophages Immunology 2009 127:103-115 DOI:10.1111/j.1365-2567.2008.02928.x PMID:18793216 PMCID:PMC2678186
- Marsolais, D., Hahm, B., Walsh, K. B., Edelmann, K. H., McGavern, D., Hatta, Y., Kawaoka, Y., Rosen, H., Oldstone, M. B. A. A critical role for the sphingosine analog aal-r in dampening the cytokine response during influenza virus infection Proceedings of the National Academy of Sciences of the United States of America 2009 106:1560-1565 DOI:10.1073/pnas.0812689106 PMID:19164548 PMCID:PMC2635800
- Don, A. S., Rosen, H. A lipid binding domain in sphingosine kinase 2 Biochemical and Biophysical Research Communications 2009 380:87-92 DOI:10.1016/j.bbrc.2009.01.075 PMID:19168031 PMCID:PMC2657340
- Marsolais, D., Rosen, H. Chemical modulators of sphingosine-1-phosphate receptors as barrier-oriented therapeutic molecules Nature Reviews Drug Discovery 2009 8:297-307 DOI:10.1038/nrd2356 PMID:19300460 PMCID:PMC4455967
- Brown, S. J., Rosen, H., Cravatt, B. F. Identification of selective inhibitors of uncharacterized enzymes by high-throughput screening with fluorescent activity-based probes Nature Biotechnology 2009 27:387-394 DOI:10.1038/nbt.1531 PMID:19329999 PMCID:PMC2709489
- Avni, D., Goldsmith, M., Ernst, O., Mashiach, R., Tuntland, T., Meijler, M. M., Gray, N. S., Rosen, H., Zor, T. Modulation of tnf alpha, il-10 and il-12p40 levels by a ceramide-1-phosphate analog, pcera-1, in vivo and ex vivo in primary macrophages Immunology Letters 2009 123:1-8 DOI:10.1016/j.imlet.2008.12.011 PMID:19185589
- Nakai, R., Salisbury, C. M., Rosen, H., Cravatt, B. F. Ranking the selectivity of pubchem screening hits by activity-based protein profiling: MMP13 as a case study Bioorganic & Medicinal Chemistry 2009 17:1101-1108 DOI:10.1016/j.bmc.2008.03.018 PMID:18364257 PMCID:PMC2661618
- Fazilleau, N., McHeyzer-Williams, L. J., Rosen, H., McHeyzer-Williams, M. G. The function of follicular helper t cells is regulated by the strength of t cell antigen receptor binding Nature Immunology 2009 10:375-384 DOI:10.1038/ni.1704 PMID:19252493 PMCID:PMC2712297
- Don, A. S., Rosen, H. A fluorescent plate reader assay for ceramide kinase Analytical Biochemistry 2008 375:265-271 DOI:10.1016/j.ab.2007.12.024 PMID:18206978 PMCID:PMC2516974
- Niessen, F., Schaffner, F., Furlan-Freguia, C., Pawlinski, R., Bhattacharjee, G., Chun, J., Derian, C. K., Andrade-Gordon, P., Rosen, H., Ruf, W. Dendritic cell PAR1-S1P3 signalling couples coagulation and inflammation Nature 2008 452:654-658 DOI:10.1038/nature06663 PMID:18305483
- Gonzalez-Cabrera, P. J., Jo, E., Sanna, M. G., Brown, S., Leaf, N., Marsolais, D., Schaeffer, M. T., Chapman, J., Cameron, M., Guerrero, M., Roberts, E., Rosen, H. Full pharmacological efficacy of a novel S1P1 agonist that does not require S1P-like headgroup interactions Molecular Pharmacology 2008 74:1308-1318 DOI:10.1124/mol.108.049783 PMID:18708635 PMCID:PMC2575047
- Schurer, S. C., Brown, S. J., Gonzalez-Cabrera, P. J., Schaeffer, M. T., Chapman, J., Jo, E., Chase, P., Spicer, T., Hodder, P., Rosen, H. Ligand-binding pocket shape differences between sphingosine 1-phosphate (S1P) receptors S1P1 and S1P3 determine efficiency of chemical probe identification by ultrahigh-throughput screening ACS Chemical Biology 2008 3:486-498 DOI:10.1021/cb800051m PMID:18590333 PMCID:PMC2597349
- Marsolais, D., Hahm, B., Edelmann, K. H., Walsh, K. B., Guerrero, M., Hatta, Y., Kawaoka, Y., Roberts, E., Oldstone, M. B. A., Rosen, H. Local not systemic modulation of dendritic cell s1p receptors in lung blunts virus-specific immune responses to influenza Molecular Pharmacology 2008 74:896-903 DOI:10.1124/mol.108.048769 PMID:18577684 PMCID:PMC2574812
- Rosen, H., Gonzalez-Cabrera, P., Marsolais, D., Cahalan, S., Don, A. S., Sanna, M. G. Modulating tone: The overture of s1p receptor immunotherapeutics Immunological Reviews 2008 223:221-235 DOI:10.1111/j.1600-065X.2008.00645.x PMID:18613839
- Lee, H. K., Brown, S. J., Rosen, H., Tobias, P. S. Application of beta-lactamase enzyme complementation to the high-throughput screening of toll-like receptor signaling inhibitors Molecular Pharmacology 2007 72:868-875 DOI:10.1124/mol.107.038349 PMID:17615244
- Don, A. S., Martinez-Lamenca, C., Webb, W. R., Proia, R. L., Roberts, E., Rosen, H. Essential requirement for sphingosine kinase 2 in a sphingolipid apoptosis pathway activated by FTY720 analogues Journal of Biological Chemistry 2007 282:15833-15842 DOI:10.1074/jbc.M609124200 PMID:17400555
- Gonzalez-Cabrera, P. J., Hla, T., Rosen, H. Mapping pathways downstream of sphingosine 1-phosphate subtype 1 by differential chemical perturbation and proteomics Journal of Biological Chemistry 2007 282:7254-7264 DOI:10.1074/jbc.M610581200 PMID:17218309
- Tsukada, Y. T., Sanna, M. G., Rosen, H., Gottlieb, R. A. S1p1-selective agonist sew2871 exacerbates reperfusion arrhythmias Journal of Cardiovascular Pharmacology 2007 50:660-669 PMID:18091583
- Rosen, H., Sanna, M. G., Cahalan, S. M., Gonzalez-Cabrera, P. J. Tipping the gatekeeper: S1p regulation of endothelial barrier function Trends in Immunology 2007 28:102-107 DOI:10.1016/j.it.2007.01.007 PMID:17276731
- Alfonso, C., McHeyzer-Williams, M. G., Rosen, H. Cd69 down-modulation and inhibition of thymic egress by short- and long-term selective chemical agonism of sphingosine 1-phosphate receptors European Journal of Immunology 2006 36:149-159 DOI:10.1002/eji.200535127 PMID:16342326
- Sanna, M. G., Wang, S. K., Gonzalez-Cabrera, P. J., Don, A., Marsolais, D., Matheu, M. P., Wei, S. H., Parker, I., Jo, E. J., Cheng, W. C., Cahalan, M. D., Wong, C. H., et al. Enhancement of capillary leakage and restoration of lymphocyte egress by a chiral S1P(1) antagonist in vivo Nature Chemical Biology 2006 2:434-441 DOI:10.1038/nchembio804 PMID:16829954
- Chun, J., Rosen, H. Lysophospholipid receptors as potential drug targets in tissue transplantation and autoimmune diseases Current Pharmaceutical Design 2006 12:161-171 DOI:10.2174/138161206775193109 PMID:16454733
- Martinez, X., Kreuwel, H. T. C., Redmond, W. L., Trenney, R., Hunter, K., Rosen, H., Sarvetnick, N., Wicker, L. S., Sherman, L. A. CD8+ T cell tolerance in nonobese diabetic mice is restored by insulin-dependent diabetes resistance alleles Journal of Immunology 2005 175:1677-1685 PMID:16034108
- Rosen, H. Chemical approaches to the lysophospholipid receptors Prostaglandins & Other Lipid Mediators 2005 77:179-184 DOI:10.1016/j.prostaglandins.2004.09.011 PMID:16099402
- Li, Z., Chen, W. R., Hale, J. J., Lynch, C. L., Mills, S. G., Hajdu, R., Keohane, C. A., Rosenbach, M. J., Milligan, J. A., Shei, G. J., Chrebet, G., Parent, S. A., et al. Discovery of potent 3,5-diphenyl-1,2,4-oxadiazole sphingosine-1-phosphate-1 (s1p(1)) receptor agonists with exceptional selectivity against s1p(2) and s1p(3) Journal of Medicinal Chemistry 2005 48:6169-6173 DOI:10.1021/jm0503244 PMID:16190743
- Gong, Q., Ou, Q. L., Ye, S. M., Lee, W. P., Cornelius, J., Diehl, L., Lin, W. Y., Hu, Z. L., Lu, Y. M., Chen, Y. M., Wu, Y., Meng, Y. G., et al. Importance of cellular microenvironment and circulatory dynamics in b cell immunotherapy Journal of Immunology 2005 174:817-826 PMID:15634903
- Jo, E. J., Sanna, G., Gonzalez-Cabrera, P. J., Thangada, S., Tigyi, G., Osborne, D. A., Hla, T., Parrill, A. L., Rosen, H. S1p(1)-selective in vivo-active agonists from high-throughput screening: Off-the-shelf chemical probes of receptor interactions, signaling, and fate Chemistry & Biology 2005 12:703-715 DOI:10.1016/j.chembiol.2005.04.019 PMID:15975516
- Rosen, H., Goetzl, E. J. Sphingosine 1-phosphate and its receptors: An autocrine and paracrine network Nature Reviews Immunology 2005 5:560-570 DOI:10.1038/nri1650 PMID:15999095
- Wei, S. H., Rosen, H., Matheu, M. P., Sanna, M. G., Wang, S. K., Jo, E. J., Wong, C. H., Parker, I., Cahalan, M. D. Sphingosine 1-phosphate type 1 receptor agonism inhibits transendothelial migration of medullary t cells to lymphatic sinuses Nature Immunology 2005 6:1228-1235 DOI:10.1038/ni1269 PMID:16273098
- Hale, J. J., Lynch, C. L., Neway, W., Mills, S. G., Hajdu, R., Keohane, C. A., Rosenbach, M. J., Milligan, J. A., Shei, G. J., Parent, S. A., Chrebet, G., Bergstrom, J., et al. A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists Journal of Medicinal Chemistry 2004 47:6662-6665 DOI:10.1021/jm0492507 PMID:15615513
- Yan, L., Hale, J. J., Lynch, C. L., Budhu, R., Gentry, A., Mills, S. G., Hajdu, R., Keohane, C. A., Rosenbach, M. J., Milligan, J. A., Shei, G. J., Chrebet, G., et al. Design and synthesis of conformationally constrained 3-(n-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (s1p) receptors Bioorganic & Medicinal Chemistry Letters 2004 14:4861-4866 DOI:10.1016/j.bmcl.2004.07.049 PMID:15341940
- Forrest, M., Sun, S. Y., Hajdu, R., Bergstrom, J., Card, D., Doherty, G., Hale, J., Keohane, C., Meyers, C., Milligan, J., Mills, S., Nomura, N., et al. Immune cell regulation and cardiovascular effects of sphingosine 1-phosphate receptor agonists in rodents are mediated via distinct receptor subtypes Journal of Pharmacology and Experimental Therapeutics 2004 309:758-768 DOI:10.1124/jpet.103.062828 PMID:14747617
- Hale, J. J., Neway, W., Mills, S. G., Hajdu, R., Keohane, C. A., Rosenbach, M., Milligan, J., Shei, G. J., Chrebet, G., Bergstrom, J., Card, D., Koo, G. C., et al. Potent s1p receptor agonists replicate the pharmacologic actions of the novel immune modulator fty720 Bioorganic & Medicinal Chemistry Letters 2004 14:3351-3355 DOI:10.1016/j.bmcl.2004.02.106 PMID:15149705
- Goetzl, E. J., Rosen, H. Regulation of immunity by lysosphingolipids and their g protein - coupled receptors Journal of Clinical Investigation 2004 114:1531-1537 DOI:10.1172/jci200423704 PMID:15578083
- Hale, J. J., Doherty, G., Toth, L., Mills, S. G., Hajdu, R., Keohane, C. A., Rosenbach, M., Milligan, J., Shei, G. J., Chrebet, G., Bergstrom, J., Card, D., et al. Selecting against s1p(3) enhances the acute cardiovascular tolerability of 3-(n-benzyl)aminopropylphosphonic acid s1p receptor agonists Bioorganic & Medicinal Chemistry Letters 2004 14:3501-3505 DOI:10.1016/j.bmcl.2004.04.070 PMID:15177461
- Sanna, M. G., Liao, J. Y., Jo, E. J., Alfonso, C., Ahn, M. Y., Peterson, M. S., Webb, B., Lefebvre, S., Chun, J., Gray, N., Rosen, H. Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate Journal of Biological Chemistry 2004 279:13839-13848 DOI:10.1074/jbc.M311743200 PMID:14732717
- Hale, J. J., Yan, L., Neway, W. E., Hajdu, R., Bergstrom, J. D., Milligan, J. A., Shei, G. J., Chrebet, G. L., Thornton, R. A., Card, D., Rosenbach, M., Rosen, H., et al. Synthesis, stereochemical determination and biochemical characterization of the enantiomeric phosphate esters of the novel immunosuppressive agent fty720 Bioorganic & Medicinal Chemistry 2004 12:4803-4807 DOI:10.1016/j.bmc.2004.07.020 PMID:15336258
- Hale, J. J., Doherty, G., Toth, L., Li, Z., Mills, S. G., Hajdu, R., Keohane, C. A., Rosenbach, M., Milligan, J., Shei, G. J., Chrebet, G., Bergstrom, J., et al. The discovery of 3-(n-alkyl)aminopropylphosphonic acids as potent s1p receptor agonists Bioorganic & Medicinal Chemistry Letters 2004 14:3495-3499 DOI:10.1016/j.bmcl.2004.04.069 PMID:15177460
- Ferrer, M., Kolodin, G. D., Zuck, P., Peltier, R., Berry, K., Mandala, S. M., Rosen, H., Ota, H., Ozaki, S., Inglese, J., Strulovici, B. A fully automated s-35 gtp gamma s scintillation proximity assay for the high-throughput screening of g(i)-linked g protein-coupled receptors Assay and Drug Development Technologies 2003 1:261-273 DOI:10.1089/15406580360545071 PMID:15090191
- Rosen, H., Sanna, G., Alfonso, C. Egress: A receptor-regulated step in lymphocyte trafficking Immunological Reviews 2003 195:160-177 DOI:10.1034/j.1600-065X.2003.00068.x PMID:12969317
- Rosen, H., Alfonso, C., Surh, C. D., McHeyzer-Williams, M. G. Rapid induction of medullary thymocyte phenotypic maturation and egress inhibition by nanomolar sphingosine 1-phosphate receptor agonist Proceedings of the National Academy of Sciences of the United States of America 2003 100:10907-10912 DOI:10.1073/pnas.1832725100 PMID:12954982 PMCID:PMC196901
- Rosen, H., Liao, J. Y. Sphingosine 1-phosphate pathway therapeutics: A lipid ligand-receptor paradigm Current Opinion in Chemical Biology 2003 7:461-468 DOI:10.1016/s1367-5931(03)00085-1 PMID:12941420
- Xie, J. H., Nomura, N., Koprak, S. L., Quackenbush, E. J., Forrest, M. J., Rosen, H. Sphingosine-1-phosphate receptor agonism impairs the efficiency of the local immune response by altering trafficking of naive and antigen-activated cd4(+) t cells Journal of Immunology 2003 170:3662-3670 PMID:12646631
- Mandala, S., Hajdu, R., Bergstrom, J., Quackenbush, E., Xie, J., Milligan, J., Thornton, R., Shei, G. J., Card, D., Keohane, C., Rosenbach, M., Hale, J., et al. Alteration of lymphocyte trafficking by sphingosine-1-phosphate receptor agonists Science 2002 296:346-349 DOI:10.1126/science.1070238 PMID:11923495
- Parent, S. A., Zhang, T., Chrebet, G., Clemas, J. A., Figueroa, D. J., Ky, B., Blevins, R. A., Austin, C. P., Rosen, H. Molecular characterization of the murine signr1 gene encoding a c-type lectin homologous to human dc-sign and dc-signr Gene 2002 293:33-46 DOI:10.1016/s0378-1119(02)00722-9 PMID:12137941
- Bowman, J. C., Hicks, P. S., Kurtz, M. B., Rosen, H., Schmatz, D. M., Liberator, P. A., Douglas, C. M. The antifungal echinocandin caspofungin acetate kills growing cells of aspergillus fumigatus in vitro Antimicrobial Agents and Chemotherapy 2002 46:3001-3012 DOI:10.1128/aac.46.9.3001-3012.2002 PMID:12183260
- Abruzzo, G. K., Gill, C. J., Flattery, A. M., Kong, L., Leighton, C., Smith, J. G., Pikounis, V. B., Bartizal, K., Rosen, H. Efficacy of the echinocandin caspofungin against disseminated aspergillosis and candidiasis in cyclophosphamide-induced immunosuppressed mice Antimicrobial Agents and Chemotherapy 2000 44:2310-2318 DOI:10.1128/aac.44.9.2310-2318.2000 PMID:10952573
- Kohler, J., Dorso, K. L., Young, K., Hammond, G. G., Rosen, H., Kropp, H., Silver, L. L. In vitro activities of the potent, broad-spectrum carbapenem mk-0826 (l-749,345) against broad-spectrum beta-lactamase- and extended-spectrum p-lactamase-producing klebsiella pneumoniae and escherichia coli clinical isolates Antimicrobial Agents and Chemotherapy 1999 43:1170-1176 PMID:10223931 PMCID:PMC89128
- Rosen, H., Hajdu, R., Silver, L., Kropp, H., Dorso, K., Kohler, J., Sundelof, J. G., Huber, J., Hammond, G. G., Jackson, J. J., Gill, C. J., Thompson, R., et al. Reduced immunotoxicity and preservation of antibacterial activity in a releasable side-chain carbapenem antibiotic Science 1999 283:703-706 DOI:10.1126/science.283.5402.703 PMID:9924033
- Gill, C. J., Jackson, J. J., Gerckens, L. S., Pelak, B. A., Thompson, R. K., Sundelof, J. G., Kropp, H., Rosen, H. In vivo activity and pharmacokinetic evaluation of a novel long-acting carbapenem antibiotic, mk-826 (l-749,345) Antimicrobial Agents and Chemotherapy 1998 42:1996-2001 PMID:9687396 PMCID:PMC105722
- Beck, L. A., Dalke, S., Leiferman, K. M., Bickel, C. A., Hamilton, R., Rosen, H., Bochner, B. S., Schleimer, R. P. Cutaneous injection of rantes causes eosinophil recruitment - comparison of nonallergic and allergic human subjects Journal of Immunology 1997 159:2962-2972 PMID:9300720
- Abruzzo, G. K., Flattery, A. M., Gill, C. J., Kong, L., Smith, J. G., Pikounis, V. B., Balkovec, J. M., Bouffard, A. F., Dropinski, J. F., Rosen, H., Kropp, H., Bartizal, K. Evaluation of the echinocandin antifungal mk-0991 (l-743,872): Efficacies in mouse models of disseminated aspergillosis, candidiasis, and cryptococcosis Antimicrobial Agents and Chemotherapy 1997 41:2333-2338 PMID:9371329 PMCID:PMC164124
- Sundelof, J. G., Hajdu, R., Gill, C. J., Thompson, R., Rosen, H., Kropp, H. Pharmacokinetics of l-749,345, a long-acting carbapenem antibiotic, in primates Antimicrobial Agents and Chemotherapy 1997 41:1743-1748 PMID:9257753 PMCID:PMC163997
- Gordon, E. J., Myers, K. J., Dougherty, J. P., Rosen, H., Ron, Y. Both anti-cd11a (lfa-i) and anti-cd11b (mac-1) therapy delay the onset and diminish the severity of experimental autoimmune encephalomyelitis Journal of Neuroimmunology 1995 62:153-160 DOI:10.1016/0165-5728(95)00120-2 PMID:7499503
- Zheng, H., Fletcher, D., Kozak, W., Jiang, M. H., Hofmann, K. J., Conn, C. A., Soszynski, D., Grabiec, C., Trumbauer, M. E., Shaw, A., Kostura, M. J., Stevens, K., et al. Resistance to fever induction and impaired acute-phase response in interleukin-1-beta-deficient mice Immunity 1995 3:9-19 DOI:10.1016/1074-7613(95)90154-x PMID:7621081
- Konteatis, Z. D., Siciliano, S. J., Vanriper, G., Molineaux, C. J., Pandya, S., Fischer, P., Rosen, H., Mumford, R. A., Springer, M. S. Development of c5a receptor antagonists - differential loss of functional-responses Journal of Immunology 1994 153:4200-4205 PMID:7930622
- Vanriper, G., Nicholson, D. W., Scheid, M. P., Fischer, P. A., Springer, M. S., Rosen, H. Induction, characterization, and functional coupling of the high affinity chemokine receptor for RANTES and macrophage inflammatory protein-1 alpha upon differentiation of an eosinophilic HL-60 cell line Journal of Immunology 1994 152:4055-4061 PMID:7511665
- Demartino, J. A., Vanriper, G., Siciliano, S. J., Molineaux, C. J., Konteatis, Z. D., Rosen, H., Springer, M. S. The amino-terminus of the human c5a receptor is required for high-affinity c5a binding and for receptor activation by c5a but not c5a analogs Journal of Biological Chemistry 1994 269:14446-14450 PMID:8182049
- Siciliano, S. J., Rollins, T. E., Demartino, J., Konteatis, Z., Malkowitz, L., Vanriper, G., Bondy, S., Rosen, H., Springer, M. S. Two-site binding of C5a by its receptor: an alternative binding paradigm for G protein-coupled receptors Proceedings of the National Academy of Sciences of the United States of America 1994 91:1214-1218 DOI:10.1073/pnas.91.4.1214 PMID:8108389 PMCID:PMC43127
- Koo, G. C., Rosen, H., Sirotina, A., Ma, X. D., Shultz, L. D. Anti-cd11b antibody prevents immunopathologic changes in viable moth-eaten bone-marrow chimeric mice Journal of Immunology 1993 151:6733-6741 PMID:8258688
- Vanriper, G., Siciliano, S., Fischer, P. A., Meurer, R., Springer, M. S., Rosen, H. Characterization and species distribution of high-affinity gtp-coupled receptors for human rantes and monocyte chemoattractant protein-1 Journal of Experimental Medicine 1993 177:851-856 DOI:10.1084/jem.177.3.851 PMID:7679712
- Cervia, J. S., Rosen, H., Murray, H. W. Effector role of blood monocytes in experimental visceral leishmaniasis Infection and Immunity 1993 61:1330-1333 PMID:8454335 PMCID:PMC281366
- Meurer, R., Vanriper, G., Feeney, W., Cunningham, P., Hora, D., Springer, M. S., Macintyre, D. E., Rosen, H. Formation of eosinophilic and monocytic intradermal inflammatory sites in the dog by injection of human rantes but not human monocyte chemoattractant protein-1, human macrophage inflammatory protein 1-alpha, or human interleukin-8 Journal of Experimental Medicine 1993 178:1913-1921 DOI:10.1084/jem.178.6.1913 PMID:7504053
- Whitcup, S. M., Debarge, L. R., Rosen, H., Nussenblatt, R. B., Chan, C. C. Monoclonal-antibody against cd11b cd18 inhibits endotoxin-induced uveitis Investigative Ophthalmology & Visual Science 1993 34:673-681 PMID:8095493
- Robinson, M. K., Andrew, D., Rosen, H., Brown, D., Ortlepp, S., Stephens, P., Butcher, E. C. Antibody against the leu-cam beta-chain (cd18) promotes both lfa-1-dependent and cr3-dependent adhesion events Journal of Immunology 1992 148:1080-1085 PMID:1371129
- Grau, G. E., Pointaire, P., Piguet, P. F., Vesin, C., Rosen, H., Stamenkovic, I., Takei, F., Vassalli, P. Late administration of monoclonal-antibody to leukocyte function-antigen 1 abrogates incipient murine cerebral malaria European Journal of Immunology 1991 21:2265-2267 DOI:10.1002/eji.1830210939 PMID:1679717
- Heyworth, P. G., Curnutte, J. T., Nauseef, W. M., Volpp, B. D., Pearson, D. W., Rosen, H., Clark, R. A. Neutrophil nicotinamide adenine-dinucleotide phosphate oxidase assembly - translocation of p47-phox and p67-phox requires interaction between p47-phox and cytochrome-b558 Journal of Clinical Investigation 1991 87:352-356 DOI:10.1172/jci114993 PMID:1985107
- Hurst, J. K., Loehr, T. M., Curnutte, J. T., Rosen, H. Resonance raman and electron-paramagnetic resonance structural investigations of neutrophil cytochrome-b558 Journal of Biological Chemistry 1991 266:1627-1634 PMID:1846361
- Blankenstein, T., Qin, Z. H., Uberla, K., Muller, W., Rosen, H., Volk, H. D., Diamantstein, T. Tumor suppression after tumor-cell targeted tumor-necrosis-factor-alpha gene-transfer Journal of Experimental Medicine 1991 173:1047-1052 DOI:10.1084/jem.173.5.1047 PMID:2022919
- Rosen, H., Gordon, S. Adoptive transfer of fluorescence-labeled cells shows that resident peritoneal-macrophages are able to migrate into specialized lymphoid organs and inflammatory sites in the mouse European Journal of Immunology 1990 20:1251-1258 DOI:10.1002/eji.1830200609 PMID:2369918
- Rosen, H. Role of CR3 in induced myelomonocytic recruitment: insights from in vivo monoclonal antibody studies in the mouse Journal of Leukocyte Biology 1990 48:465-469 PMID:2230596
- Rosen, H., Law, S. K. A. The leukocyte cell-surface receptor(s) for the ic3b product of complement Current Topics in Microbiology and Immunology 1990 153:99-122 PMID:2137074
- Rosen, H., Gordon, S. The role of the type-3 complement receptor in the induced recruitment of myelomonocytic cells to inflammatory sites in the mouse American Journal of Respiratory Cell and Molecular Biology 1990 3:3-10 PMID:2141991
- Hutchings, P., Rosen, H., Oreilly, L., Simpson, E., Gordon, S., Cooke, A. Transfer of diabetes in mice prevented by blockade of adhesion-promoting receptor on macrophages Nature 1990 348:639-641 DOI:10.1038/348639a0 PMID:2250718
- Dinauer, M. C., Curnutte, J. T., Rosen, H., Orkin, S. H. A missense mutation in the neutrophil cytochrome-b heavy-chain in cytochrome-positive x-linked chronic granulomatous-disease Journal of Clinical Investigation 1989 84:2012-2016 DOI:10.1172/jci114393 PMID:2556453
- Lunn, E. R., Perry, V. H., Brown, M. C., Rosen, H., Gordon, S. Absence of wallerian degeneration does not hinder regeneration in peripheral-nerve European Journal of Neuroscience 1989 1:27-33 DOI:10.1111/j.1460-9568.1989.tb00771.x PMID:12106171
- Rosen, H., Milon, G., Gordon, S. Antibody to the murine type 3 complement receptor inhibits T lymphocyte-dependent recruitment of myelomonocytic cells in vivo Journal of Experimental Medicine 1989 169:535-548 DOI:10.1084/jem.169.2.535 PMID:2521356 PMCID:PMC2189217
- Rosen, H., Gordon, S. Current status review - adhesion molecules and myelomonocytic cell-endothelial interactions British Journal of Experimental Pathology 1989 70:385-394 PMID:2669925 PMCID:PMC2040576
- Rosen, H., Gordon, S., North, R. J. Exacerbation of murine listeriosis by a monoclonal-antibody specific for the type-3 complement receptor of myelomonocytic cells - absence of monocytes at infective foci allows listeria to multiply in nonphagocytic cells Journal of Experimental Medicine 1989 170:27-37 DOI:10.1084/jem.170.1.27 PMID:2501445
- Cooper, A., Rosen, H., Blackwell, J. M. Monoclonal-antibodies that recognize distinct epitopes of the macrophage type 3 complement receptor differ in their ability to inhibit binding of leishmania promastigotes harvested at different phases of their growth-cycle Immunology 1988 65:511-514 PMID:3065216 PMCID:PMC1385558
- Okamura, N., Malawista, S. E., Roberts, R. L., Rosen, H., Ochs, H. D., Babior, B. M., Curnutte, J. T. Phosphorylation of the oxidase-related k-48 phosphoprotein family in the unusual autosomal cytochrome-negative and x-linked cytochrome-positive types of chronic granulomatous-disease Blood 1988 72:811-816 PMID:3401601
- Rosen, H., Gordon, S. Monoclonal antibody to the murine type 3 complement receptor inhibits adhesion of myelomonocytic cells in vitro and inflammatory cell recruitment in vivo Journal of Experimental Medicine 1987 166:1685-1701 DOI:10.1084/jem.166.6.1685 PMID:2445894 PMCID:PMC2188801
- Rosen, H., Gordon, S. Surface events in polymorphonuclear leukocyte activation - insights from a hydrophobic membrane antigen that triggers the respiratory burst Journal of Cell Science 1987 88:591-601 PMID:2459144
- Berton, G., Rosen, H., Ezekowitz, R. A. B., Bellavite, P., Serra, M. C., Rossi, F., Gordon, S. Monoclonal-antibodies to a particulate superoxide-forming system stimulate a respiratory burst in intact guinea-pig neutrophils Proceedings of the National Academy of Sciences of the United States of America 1986 83:4002-4006 DOI:10.1073/pnas.83.11.4002 PMID:3012541
- Millar, R. P., Rosen, H., Badminton, M., Pasqualini, C., Kerdelhue, B. Luteinizing-hormone-releasing hormone (lh-rh) binding to purified rat pituitary nuclei FEBS Letters 1983 153:382-386 DOI:10.1016/0014-5793(83)80648-6 PMID:6311621
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report
- Kumar, N., Nuhant, P., Solt, L. A., Conkright, J. J., Wang, Y., Istrate, M. A., Busby, S. A., Ruben, D. G. O., Burris, T. P., Cameron, M., Mercer, B. A., Hodder, P., et al. Identification of a novel selective inverse agonist probe and analogs for the Retinoic acid receptor-related Orphan Receptor Alpha (RORalpha) 2010
- Kumar, N., Kamenecka, T., Lyda, B., Khan, P., Chang, M. R., Garcia-Ordonez, R. D., Cameron, M., Ferguson, J., Mercer, B. A., Hodder, P., Rosen, H., Griffin, P. R. Identification of a novel selective inverse agonist probe and analogs for the Retinoic acid receptor-related Orphan Receptor Gamma (RORgamma) 2010
- Hulce, J. J., Joslyn, C., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Cravatt, B. F., Hodder, P., Rosen, H. An in vivo active carbamate-based dual inhibitor of lysophospholipase 1 (LYPLA1) and lysophospholipase 2 (LYPLA2) Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:25506974
- Adibekian, A., Martin, B. R., Chang, J. W., Hsu, K. L., Tsuboi, K., Bachovchin, D. A., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Cravatt, B. F., et al. Characterization of a Selective, Reversible Inhibitor of Lysophospholipase 2 (LYPLA2) Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:24624468
- Adibekian, A., Martin, B. R., Chang, J. W., Hsu, K. L., Tsuboi, K., Bachovchin, D. A., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Cravatt, B. F., et al. Characterization of a selective, reversible inhibitor of lysophospholipase 1 (LYPLA1) Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:24624465
- Schoenen, F. J., Whipple, D., Baillargeon, P., Brown, C. L., Chase, P., Ferguson, J., Fernandez-Vega, V., Hodder, P., Mathew, R., Neuenswander, B., Porubsky, P., Rogers, S., et al. Inhibitors of the Plasmodium falciparum M17 leucine aminopeptidase Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:25506973
- Schoenen, F. J., Weiner, W. S., Baillargeon, P., Brown, C. L., Chase, P., Ferguson, J., Fernandez-Vega, V., Ghosh, P., Hodder, P., Krise, J. P., Matharu, D. S., Neuenswander, B., et al. Inhibitors of the Plasmodium falciparum M18 aspartyl aminopeptidase Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:24479194
- Nagano, J. M. G., Hsu, K. L., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Bahnson, B. J., Cravatt, B. F., Hodder, P., Rosen, H. Optimization and characterization of a carbamate inhibitor for plasma platelet-activating factor acetylhydrolase (pPAFAH) Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23658952
- Dreyton, C. J., Jones, J. E., Knuckley, B. A., Subramanian, V., Anderson, E. D., Brown, S. J., Fernandez-Vega, V., Eberhart, C., Spicer, T., Zuhl, A. M., Ferguson, J., Speers, A. E., et al. Optimization and characterization of a pan protein arginine deiminase (PAD) inhibitor Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23833800
- Adibekian, A., Martin, B. R., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Cravatt, B. F., Hodder, P., Rosen, H. Optimization and characterization of a triazole urea dual inhibitor for lysophospholipase 1 (LYPLA1) and lysophospholipase 2 (LYPLA2) Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23658947
- Adibekian, A., Hsu, K. L., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Cravatt, B. F., Hodder, P., Rosen, H. Optimization and characterization of a triazole urea inhibitor for alpha/beta hydrolase domain-containing protein 11 (ABHD11): anti-probe for LYPLA1/LYPLA2 dual inhibitor ML211 Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23658953
- Hsu, K. L., Tsuboi, K., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Cravatt, B. F., Hodder, P., Rosen, H. Optimization and characterization of a triazole urea inhibitor for diacylglycerol lipase beta (DAGL-beta) Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23658950
- Adibekian, A., Hsu, K. L., Speers, A. E., Monillas, E. S., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Bahnson, B. J., Cravatt, B. F., Hodder, P., Rosen, H. Optimization and characterization of a triazole urea inhibitor for platelet-activating factor acetylhydrolase type 2 (PAFAH2) Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23658960
- Tsuboi, K., Bachovchin, D. A., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Cravatt, B. F., Hodder, P., Rosen, H. Optimization and characterization of an inhibitor for glutathione S-tranferase omega 1 (GSTO1) Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:22834034
- Hsu, K. L., Tsuboi, K., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Cravatt, B. F., Hodder, P., Rosen, H. Optimization and characterization of triazole urea inhibitors for abhydrolase domain containing protein 6 (ABHD6) Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23762934
- Guerrero, M., Poddutoori, R., Pinacho-Crisostomo, F., Schaeffer, M. T., Brown, S. J., Spicer, T., Chase, P., Ferguson, J., Roberts, E., Sanna, G., Hodder, P., Rosen, H. Probe development efforts for an allosteric agonist of the sphingosine 1-phosphate receptor 3 (S1P3) Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23658964
- Zuhl, A. M., Mohr, J. T., Speers, A. E., Bachovchin, D. A., Berlin, J. M., Spicer, T., Fernandez-Vega, V., Brown, S. J., Ferguson, J., Fu, G. C., Cravatt, B. F., Hodder, P., et al. Probe development efforts to identify novel inhibitors of ABHD10 Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23762952
- Bachovchin, D. A., Speers, A. E., Brown, S. J., Spicer, T. P., Fernandez, Vega, Ferguson, J., Mohr, J. T., Murphy, J., Fu, G. C., Cravatt, B. F., Hodder, P. S., Rosen, H. Probe development efforts to identify novel inhibitors of protein phosphatase methylesterase-1 (PME-1) Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:22834039
- Bachovchin, D. A., Speers, A. E., Zuhl, A. M., Brown, S. J., Cravatt, B. F., Fernandez, Vega, Spicer, T., Mercer, B. A., Ferguson, J., Hodder, P., Rosen, H. R. Probe report for PME-1 inhibitors Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:21433379
- Brown, S. J., Bachovchin, D. A., Cravatt, B. F., Fernandez-Vega, V., Spicer, T., Mercer, B. A., Hodder, P., Rosen, H. R. Probe report for RBBP9 inhibitors - Probe 1 Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:21433353
- Bachovchin, D. A., Speers, A. E., Brown, S. J., Cravatt, B. F., Spicer, T., Mercer, B. A., Ferguson, J., Hodder, P., Rosen, H. R. Probe report for RBBP9 inhibitors - Probe 2 Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:21433382
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thesis