recent publications
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academic article
- Grandjean, J. M. D., Madhavan, A., Cech, L., Seguinot, B. O., Paxman, R. J., Smith, E., Scampavia, L., Powers, E. T., Cooley, C. B., Plate, L., Spicer, T. P., Kelly, J. W., et al. Pharmacologic IRE1/XBP1s activation confers targeted ER proteostasis reprogramming Nature Chemical Biology 2020 DOI:10.1038/s41589-020-0584-z PMID:32690944
- Pan, C. H., Otsuka, Y., Sridharan, B., Woo, M., Leiton, C. V., Babu, S., Goncalves, M. T., Kawalerski, R. R., Bai, J. D. K., Chang, D. V. K., Biankin, A. V., Scampavia, L., et al. An unbiased high-throughput drug screen reveals a potential therapeutic vulnerability in the most lethal molecular subtype of pancreatic cancer Molecular Oncology 2020 DOI:10.1002/1878-0261.12743 PMID:32533886
- Otsuka, Y., Airola, M. V., Choi, Y. M., Coant, N., Snider, J., Cariello, C., Saied, E. M., Arenz, C., Bannister, T., Rahaim, R., Hannun, Y. A., Shumate, J., et al. Identification of Small-Molecule Inhibitors of Neutral Ceramidase (nCDase) via Target-Based High-Throughput Screening SLAS Discovery 2020 DOI:10.1177/2472555220945283 PMID:32734807
- Smith, E., Janovick, J. A., Bannister, T. D., Shumate, J., Ganapathy, V., Scampavia, L., Spicer, T. P. Rescue of mutant gonadotropin-releasing hormone receptor function independent of cognate receptor activity Scientific Reports 2020 10 DOI:10.1038/s41598-020-67473-w PMID:32601341 PMCID:PMC7324376
- Wang, L. M., Cheng, C. M., Qin, J., Xu, M. F., Kao, C. Y., Shi, J. J., You, E. L., Gong, W. C., Rosa, L. P., Chase, P., Scampavia, L., Madoux, F., et al. Small-molecule inhibitor targeting orphan nuclear receptor COUP-TFII for prostate cancer treatment Science Advances 2020 6 DOI:10.1126/sciadv.aaz8031 PMID:32494682 PMCID:PMC7190335
- Spicer, T. P. Drug Discovery Targeting COVID-19 SLAS Discovery 2020 25:1095-1096 DOI:10.1177/2472555220970966 PMID:33215959
- Smith, E., Davis-Gardner, M. E., Garcia-Ordonez, R. D., Nguyen, T. T., Hull, M., Chen, E., Baillargeon, P., Scampavia, L., Strutzenberg, T., Griffin, P. R., Farzan, M., Spicer, T. P. High-Throughput Screening for Drugs That Inhibit Papain-Like Protease in SARS-CoV-2 SLAS Discovery 2020 DOI:10.1177/2472555220963667 PMID:33043784 PMCID:PMC7550789
- Smith, E., Dukovski, D., Shumate, J., Scampavia, L., Miller, J. P., Spicer, T. P. Identification of Compounds That Promote Readthrough of Premature Termination Codons in the CFTR SLAS Discovery 2020 DOI:10.1177/2472555220962001 PMID:33016182
- Llamosas, N., Arora, V., Vij, R., Kilinc, M., Bijoch, L., Rojas, C., Reich, A., Sridharan, B., Willems, E., Piper, D. R., Scampavia, L., Spicer, T. P., et al. SYNGAP1 Controls the Maturation of Dendrites, Synaptic Function, and Network Activity in Developing Human Neurons Journal of Neuroscience 2020 40:7980-7994 DOI:10.1523/jneurosci.1367 PMID:32887745 PMCID:PMC7548701
- Baillargeon, P., Spicer, T. P., Scampavia, L. Applications for open source microplate-compatible illumination panels Journal of Visualized Experiments : JoVE 2019 DOI:10.3791/60088 PMID:31633701
- Baillargeon, P., Shumate, J., Hou, S., Fernandez-Vega, V., Marques, N., Souza, G., Seldin, J., Spicer, T. P., Scampavia, L. Automating a magnetic 3D spheroid model technology for high-throughput screening SLAS Technology 2019 24:420-428 DOI:10.1177/2472630319854337 PMID:31225974
- Baillargeon, P., Coss-Flores, K., Singhera, F., Shumate, J., Williams, H., DeLuca, L., Spicer, T. P., Scampavia, L. Design of microplate-compatible illumination panels for a semiautomated benchtop pipetting system SLAS Technology 2019 24:399-407 DOI:10.1177/2472630318822476 PMID:30698997
- Sridharan, B., Hubbs, C., Llamosas, N., Kilinc, M., Singhera, F. U., Willems, E., Piper, D. R., Scampavia, L., Rumbaugh, G., Spicer, T. P. A simple procedure for creating scalable phenotypic screening assays in human neurons Scientific Reports 2019 9 DOI:10.1038/s41598-019-45265-1 PMID:31227747 PMCID:PMC6588600
- 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
- Zhou, W., Yin, Y., Smith, E., Chou, J., Shumate, J., Scampavia, L., Spicer, T. P., Carpino, N., French, J. B. Discovery and characterization of two classes of selective inhibitors of the suppressor of the TCR signaling family of proteins ACS Infectious Diseases 2019 5:250-259 DOI:10.1021/acsinfecdis.8b00238 PMID:30485744 PMCID:PMC6368478
- Spicer, T. P., Gardiner, D. L., Schoenen, F. J., Roy, S., Griffin, P. R., Chase, P., Scampavia, L., Hodder, P., Trenholme, K. R. Identification of antimalarial inhibitors using late-stage gametocytes in a phenotypic live/dead sssay SLAS Discovery 2019 24:38-46 DOI:10.1177/2472555218796410 PMID:30142014
- Shumate, J., Baillargeon, P., Spicer, T. P., Scampavia, L. IoT for real-time measurement of high-throughput liquid dispensing in laboratory environments SLAS Technology 2018 23:440-447 DOI:10.1177/2472630318769454 PMID:29649373
- Janovick, J. A., Spicer, T. P., Bannister, T. D., Smith, E., Ganapathy, V., Scampavia, L. Chemical validation and optimization of pharmacoperones targeting vasopressin type 2 receptor mutant Biochemical Journal 2018 475:2941-2953 DOI:10.1042/bcj20180065 PMID:30068530
- Quereda, V., Hou, S., Madoux, F., Scampavia, L., Spicer, T. P., Duckett, D. A cytotoxic three-dimensional-spheroid, high-throughput assay using patient-derived glioma stem cells SLAS Discovery 2018 23:842-849 DOI:10.1177/2472555218775055 PMID:29750582 PMCID:PMC6102052
- Kota, S., Hou, S., Guerrant, W., Madoux, F., Troutman, S., Fernandez-Vega, V., Alekseeva, N., Madala, N., Scampavia, L., Kissil, J., Spicer, T. P. A novel three-dimensional high-throughput screening approach identifies inducers of a mutant KRAS selective lethal phenotype Oncogene 2018 37:4372-4384 DOI:10.1038/s41388-018-0257-5 PMID:29743592
- Hou, S., Tiriac, H., Sridharan, B. P., Scampavia, L., Madoux, F., Seldin, J., Souza, G. R., Watson, D., Tuveson, D., Spicer, T. P. Advanced development of primary pancreatic organoid tumor models for high-throughput phenotypic drug screening SLAS Discovery 2018 23:574-584 DOI:10.1177/2472555218766842 PMID:29673279 PMCID:PMC6013403
- Nieto, A., Fernandez-Vega, V., Spicer, T. P., Sturchler, E., Adhikari, P., Kennedy, N., Mandat, S., Chase, P., Scampavia, L., Bannister, T., Hodder, P., McDonald, P. H. Identification of Novel, Structurally Diverse, Small Molecule Modulators of GPR119 Assay and Drug Development Technologies 2018 16:278-288 DOI:10.1089/adt.2018.849 PMID:30019946 PMCID:PMC6065524
- Muntean, B. S., Patil, D. N., Madoux, F., Fossetta, J., Scampavia, L., Spicer, T. P., Martemyanov, K. A. A high-throughput time-resolved fluorescence energy transfer assay to screen for modulators of RGS7/Gβ5/R7BP complex Assay and Drug Development Technologies 2018 16:150-161 DOI:10.1089/adt.2017.839 PMID:29658790 PMCID:PMC5906730
- Kong, J., Fang, P., Madoux, F., Spicer, T. P., Scampavia, L., Kim, S., Guo, M. High-throughput screening for protein synthesis inhibitors targeting aminoacyl-tRNA synthetases SLAS Discovery 2018 23:174-182 DOI:10.1177/2472555217734128 PMID:29020503
- Singhera, F., Cooper, E., Scampavia, L., Spicer, T. Using bead injection to model dispensing of 3-D multicellular spheroids into microtiter plates Talanta 2018 177:74-76 DOI:10.1016/j.talanta.2017.09.022 PMID:29108585 PMCID:PMC5683093
- Collia, D., Bannister, T. D., Tan, H., Jin, S., Langaee, T., Shumate, J., Scampavia, L., Spicer, T. P. A rapid phenotypic whole-cell screening approach for the identification of small-molecule inhibitors that counter β-lactamase resistance in pseudomonas aeruginosa SLAS Discovery 2018 23:55-64 DOI:10.1177/2472555217728489 PMID:28850797 PMCID:PMC5743017
- Smith, E., Giuliano, K. A., Shumate, J., Baillargeon, P., McEwan, B., Cullen, M. D., Miller, J. P., Drew, L., Scampavia, L., Spicer, T. P. A homogeneous cell-based halide-sensitive yellow fluorescence protein assay to identify modulators of the cystic fibrosis transmembrane conductance regulator ion channel Assay and Drug Development Technologies 2017 15:395-406 DOI:10.1089/adt.2017.810 PMID:29172645
- Janovick, J. A., Spicer, T. P., Bannister, T. D., Scampavia, L., Conn, P. M. Pharmacoperone rescue of vasopressin 2 receptor mutants reveals unexpected constitutive activity and coupling bias PLoS One 2017 12 DOI:10.1371/journal.pone.0181830 PMID:28767678 PMCID:PMC5540481
- Hou, S., Madoux, F., Scampavia, L., Janovick, J. A., Conn, P. M., Spicer, T. P. Drug library screening for the identification of ionophores that correct the mistrafficking disorder associated with oxalosis kidney disease SLAS Discovery 2017 22:887-896 DOI:10.1177/2472555217689992 PMID:28346094
- Madoux, F., Tanner, A., Vessels, M., Willetts, L., Hou, S., Scampavia, L., Spicer, T. P. A 1536-well 3D viability assay to assess the cytotoxic effect of erugs on spheroids SLAS Discovery 2017 22:516-524 DOI:10.1177/2472555216686308 PMID:28346088
- Wang, J., Fang, P. F., Chase, P., Tshori, S., Razin, E., Spicer, T. P., Scampavia, L., Hodder, P., Guo, M. Development of an HTS-compatible assay for discovery of melanoma-related microphthalmia transcription factor disruptors using AlphaScreen technology SLAS Discovery 2017 22:58-66 DOI:10.1177/1087057116675274 PMID:27827304
- Janovick, J. A., Spicer, T. P., Smith, E., Bannister, T. D., Kenakin, T., Scampavia, L., Conn, P. M. Receptor antagonism/agonism can be uncoupled from pharmacoperone activity Molecular and Cellular Endocrinology 2016 434:176-185 DOI:10.1016/j.mce.2016.07.003 PMID:27389877 PMCID:PMC4983495
- Smith, E., Janovick, J. A., Bannister, T. D., Shumate, J., Scampavia, L., Conn, P. M., Spicer, T. P. Identification of potential pharmacoperones capable of rescuing the functionality of misfolded vasopressin 2 receptor involved in nephrogenic diabetes insipidus Journal of Biomolecular Screening 2016 21:824-831 DOI:10.1177/1087057116653925 PMID:27280550
- 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
- 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
- Jambrina, E., Cerne, R., Smith, E., Scampavia, L., Cuadrado, M., Findlay, J., Krambis, M. J., Wakulchik, M., Chase, P., Brunavs, M., Burris, K. D., Gallagher, P., et al. An integrated approach for screening and identification of positive allosteric modulators of N-methyl-D-aspartate receptors Journal of Biomolecular Screening 2016 21:468-479 DOI:10.1177/1087057116628437 PMID:26838761
- Thenin-Houssier, S., de Vera, I. M. S., Pedro-Rosa, L., Brady, A., Richard, A., Konnick, B., Opp, S., Buffone, C., Fuhrmann, J., Kota, S., Billack, B., Pietka-Ottlik, M., et al. Ebselen, a small-molecule capsid inhibitor of HIV-1 replication Antimicrobial Agents and Chemotherapy 2016 60:2195-2208 DOI:10.1128/aac.02574-15 PMID:26810656 PMCID:PMC4808204
- Chase, P., Enogieru, I., Madoux, F., Bishop, E., Beer, J., Scampavia, L., Spicer, T. An automated miniaturized method to perform and analyze antimicrobial drug synergy assays Assay and Drug Development Technologies 2016 14:58-66 DOI:10.1089/adt.2015.672 PMID:26669516 PMCID:PMC4761817
- Palde, P. B., Bhaskar, A., Rosa, L. E. P., Madoux, F., Chase, P., Gupta, V., Spicer, T., Scampavia, L., Singh, A., Carroll, K. S. First-in-class inhibitors of sulfur metabolism with bactericidal activity against non-replicating M. tuberculosis ACS Chemical Biology 2016 11:172-184 DOI:10.1021/acschembio.5b00517 PMID:26524379 PMCID:PMC4729198
- Smith, E., Chase, P., Niswender, C. M., Utley, T. J., Sheffler, D. J., Noetzel, M. J., Lamsal, A., Wood, M. R., Conn, P. J., Lindsley, C. W., Madoux, F., Acosta, M., et al. Application of parallel multiparametric cell-based FLIPR detection assays for the identification of modulators of the muscarinic acetylcholine receptor 4 (M-4) Journal of Biomolecular Screening 2015 20:858-868 DOI:10.1177/1087057115581770 PMID:25877150 PMCID:PMC4659430
- Conn, P. M., Spicer, T. P., Scampavia, L., Janovick, J. A. Assay strategies for identification of therapeutic leads that target protein trafficking Trends in Pharmacological Sciences 2015 36:498-505 DOI:10.1016/j.tips.2015.05.004 PMID:26067100 PMCID:PMC4532603
- 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
- Ting, P. Y., Damoiseaux, R., Titz, B., Bradley, K. A., Graeber, T. G., Fernandez-Vega, V., Bannister, T. D., Chase, P., Nair, R., Scampavia, L., Hodder, P., Spicer, T. P., et al. Identification of small molecules that disrupt signaling between ABL and its positive regulator RIN1 PLoS One 2015 10:e0121833 DOI:10.1371/journal.pone.0121833 PMID:25811598 PMCID:PMC4374917
- Madoux, F., Janovick, J. A., Smithson, D., Fargue, S., Danpure, C. J., Scampavia, L., Chen, Y. T., Spicer, T. P., Conn, P. M. Development of a phenotypic high-content assay to identify pharmacoperone drugs for the treatment of primary hyperoxaluria type 1 by high-throughput screening Assay and Drug Development Technologies 2015 13:16-24 DOI:10.1089/adt.2014.627 PMID:25710543
- 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
- Pedro-Rosa, L., Buckner, F. S., Ranade, R. M., Eberhart, C., Madoux, F., Gillespie, J. R., Koh, C. Y., Brown, S., Lohse, J., Verlinde, C. L. M., Fan, E., Bannister, T., et al. Identification of potent inhibitors of the Trypanosoma brucei methionyl-tRNA synthetase via high-throughput orthogonal screening Journal of Biomolecular Screening 2015 20:122-130 DOI:10.1177/1087057114548832 PMID:25163684 PMCID:PMC4378865
- Kadakkuzha, B. M., Spicer, T. P., Chase, P., Richman, J. B., Hodder, P., Puthanveettil, S. V. High-throughput screening for small molecule modulators of motor protein Kinesin Assay and Drug Development Technologies 2014 12:470-480 DOI:10.1089/adt.2014.579 PMID:25383721
- Madoux, F., Tredup, C., Scampavia, L., Chase, P. S., Hodder, P. S., Fields, G. B., Becker-Pauly, C., Minond, D., Spicer, T. P. Development of high throughput screening assays and pilot screen for inhibitors of metalloproteases meprin α and β Biopolymers 2014 102:396-406 DOI:10.1002/bip.22527 PMID:25048711 PMCID:PMC4339026
- Spicer, T., Fernandez-Vega, V., Chase, P., Scampavia, L., To, J., Dalton, J. P., Da Silva, F. L., Skinner-Adams, T. S., Gardiner, D. L., Trenholme, K. R., Brown, C. L., Ghosh, P., et al. Identification of potent and selective inhibitors of the plasmodium falciparum M18 aspartyl aminopeptidase (PfM18AAP) of human malaria via high-throughput screening Journal of Biomolecular Screening 2014 19:1107-1115 DOI:10.1177/1087057114525852 PMID:24619116 PMCID:PMC4641816
- Conn, P. M., Smith, E., Spicer, T., Chase, P., Scampavia, L., Janovick, J. A. A phenotypic high throughput screening assay for the identification of pharmacoperones for the gonadotropin releasing hormone receptor Assay and Drug Development Technologies 2014 12:238-246 DOI:10.1089/adt.2014.576 PMID:24831790 PMCID:PMC4025569
- Sturchler, E., Chen, W., Spicer, T., Hodder, P., McDonald, P., Duckett, D. Development of an HTS-compatible assay for the discovery of ASK1 signalosome inhibitors using alphascreen technology Assay and Drug Development Technologies 2014 12:229-237 DOI:10.1089/adt.2013.558 PMID:24831789 PMCID:PMC4025566
- Jiang, J., Taylor, A. B., Choi, J. Y., Hart, P. J., Roush, W. R., Fields, G. B., Hodder, P. S., Minong, D., Spicer, T. P. Characterization of selective exosite-binding inhibitors of matrix metalloproteinase 13 that prevent articular cartilage degradation in vitro Journal of Medicinal Chemistry 2014 57:9598-9611 DOI:10.1021/jm501284e PMID:25330343 PMCID:PMC4255739
- 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
- Richard, D. J., Lena, R., Bannister, T., Blake, N., Pierceall, W. E., Carlson, N. E., Keller, C. E., Koenig, M., He, Y., Minond, D., Mishra, J., Cameron, M., et al. Hydroxyquinoline-derived compounds and analoguing of selective Mcl-1 inhibitors using a functional biomarker Bioorganic & Medicinal Chemistry 2013 21:6642-6649 DOI:10.1016/j.bmc.2013.08.017 PMID:23993674 PMCID:PMC3831274
- Thomas, P. W., Spicer, T., Cammarata, M., Brodbelt, J. S., Hodder, P., Fast, W. An altered zinc-binding site confers resistance to a covalent inactivator of New Delhi metallo-beta-lactamase-1 (NDM-1) discovered by high-throughput screening Bioorganic & Medicinal Chemistry 2013 21:3138-3146 DOI:10.1016/j.bmc.2013.03.031 PMID:23591260 PMCID:PMC3651783
- Karapetyan, Y. E., Sferrazza, G. F., Zhou, M., Ottenberg, G., Spicer, T., Chase, P., Fallahi, M., Hodder, P., Weissmann, C., Lasmezas, C. I. Unique drug screening approach for prion diseases identifies tacrolimus and astemizole as antiprion agents Proceedings of the National Academy of Sciences of the United States of America 2013 110:7044-7049 DOI:10.1073/pnas.1303510110 PMID:23576755 PMCID:PMC3637718
- 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
- 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
- Amundsen, S. K., Spicer, T., Karabulut, A. C., Londono, L. M., Eberhart, C., Vega, V. F., Bannister, T. D., Hodder, P., Smith, G. R. Small-molecule inhibitors of bacterial AddAB and RecBCD helicase-nuclease DNA repair enzymes ACS Chemical Biology 2012 7:879-891 DOI:10.1021/cb300018x PMID:22443934 PMCID:PMC3356449
- Peatey, C. L., Spicer, T. P., Hodder, P. S., Trenholme, K. R., Gardiner, D. L. A high-throughput assay for the identification of drugs against late-stage Plasmodium falciparum gametocytes Molecular and Biochemical Parasitology 2011 180:127-131 DOI:10.1016/j.molbiopara.2011.09.002 PMID:21939693
- Bialkowska, A. B., Crisp, M., Bannister, T., He, Y. J., Chowdhury, S., Schurer, S., Chase, P., Spicer, T., Madoux, F., Tian, C. L., Hodder, P., Zaharevitz, D., et al. Identification of small-molecule inhibitors of the colorectal cancer oncogene Kruppel-like factor 5 expression by ultrahigh-throughput screening Molecular Cancer Therapeutics 2011 10:2043-2051 DOI:10.1158/1535-7163.mct-11-0550 PMID:21885866 PMCID:PMC3213326
- 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
- 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
- Istrate, M. A., Spicer, T. P., Wang, Y., Bernard, J. A., Helvering, L. M., Bocchinfuso, W. P., Richardson, T. I., Zink, R., Kumar, N., Montrose-Rafizadeh, C., Dodge, J., Hodder, P., et al. Development of an HTS-compatible assay for discovery of ROR alpha modulators using AlphaScreen (r) technology Journal of Biomolecular Screening 2011 16:183-191 DOI:10.1177/1087057110389040 PMID:21297105 PMCID:PMC4434603
- Weide, T., Saldanha, S. A., Minond, D., Spicer, T. P., Fotsing, J. R., Spaargaren, M., Frere, J. M., Bebrone, C., Sharpless, K. B., Hodder, P. S., Fokin, V. V. NH-1,2,3-triazole-based inhibitors of the VIM-2 Metallo-beta-Lactamase: synthesis and structure-activity studies ACS Medicinal Chemistry Letters 2010 1:150-154 DOI:10.1021/ml900022q PMID:20625539 PMCID:PMC2901175
- 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
- Kota, S., Scampavia, L., Spicer, T., Beeler, A. B., Takahashi, V., Snyder, J. K., Porco, J. A., Hodder, P., Strosberg, A. D. A time-resolved fluorescence-resonance energy transfer assay for identifying inhibitors of hepatitis C virus core dimerization Assay and Drug Development Technologies 2010 8:96-105 DOI:10.1089/adt.2009.0217 PMID:20035614 PMCID:PMC2971647
- Brothers, S. P., Saldanha, S. A., Spicer, T. P., Cameron, M., Mercer, B. A., Chase, P., McDonald, P., Wahlestedt, C., Hodder, P. S. Selective and brain penetrant neuropeptide y y2 receptor antagonists discovered by whole-cell high-throughput screening Molecular Pharmacology 2010 77:46-57 DOI:10.1124/mol.109.058677 PMID:19837904 PMCID:PMC2802430
- Minond, D., Saldanha, S. A., Subramaniam, P., Spaargaren, M., Spicer, T., Fotsing, J. R., Weide, T., Fokin, V. V., Sharpless, K. B., Galleni, M., Bebrone, C., Lassaux, P., et al. Inhibitors of VIM-2 by screening pharmacologically active and click-chemistry compound libraries Bioorganic & Medicinal Chemistry 2009 17:5027-5037 DOI:10.1016/j.bmc.2009.05.070 PMID:19553129 PMCID:PMC2759276
- 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
- Lauer-Fields, J. L., Spicer, T. P., Chase, P. S., Cudic, M., Burstein, G. D., Nagase, H., Hodder, P., Fields, G. B. Screening of potential a, disintegrin and metalloproteinase with thrombospondin motifs-4 inhibitors using a collagen model fluorescence resonance energy transfer substrate Analytical Biochemistry 2008 373:43-51 DOI:10.1016/j.ab.2007.09.014 PMID:17949675 PMCID:PMC2245870
- Schroeter, T., Minond, D., Weiser, A., Dao, C., Habel, J., Spicer, T., Chase, P., Baillargeon, P., Scampavia, L., Schuerer, S., Chung, C., Mader, C., et al. Comparison of miniaturized time-resolved fluorescence resonance energy transfer and enzyme-coupled luciferase high-throughput screening assays to discover inhibitors of Rho-kinase II (ROCK-II) Journal of Biomolecular Screening 2008 13:17-28 DOI:10.1177/1087057107310806 PMID:18227223
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report
- Minond, D., Saldanha, S. A., Spicer, T., Qin, L., Mercer, B. A., Roush, W. R., Hodder, P. HTS assay for discovery of novel metallo-beta-lactamase (MBL) inhibitors Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:21961119
- 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
- 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
- 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
- Bialkowska, A., Crisp, M., Madoux, F., Spicer, T., Knapinska, A., Mercer, B., Bannister, T. D., He, Y., Chowdhury, S., Cameron, M., Yang, V. W., Hodder, P. ML264: An antitumor agent that potently and selectively inhibits kruppel-like factor five (KLF5) expression: a probe for studying colon cancer development and progression Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23762940
- Spicer, T., Minond, D., Enogieru, I., Saldanha, S. A., Allais, C., Liu, Q., Mercer, B. A., Roush, W. R., Hodder, P. ML302, a novel beta-lactamase (BLA) inhibitor Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23762954
- Bannister, T., Koenig, M., He, Y., Mishra, J., Spicer, T., Minond, D., Saldanha, A., Mercer, B. A., Cameron, M., Lena, R., Carlson, N., Richard, D., et al. ML311: A small molecule that potently and selectively disrupts the protein-protein interaction of Mcl-1 and Bim: a probe for studying lymphoid tumorigenesis Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23762927
- Bannister, T. D., Nair, R., Spicer, T., Fernandez Vega, V., Eberhart, C., Mercer, B. A., Cameron, M., Schurer, S., Amundsen, S. K., Karabulut, A., Londono, L. M., Smith, G. R., et al. ML328: A novel dual inhibitor of bacterial AddAB and RecBCD helicase-nuclease DNA repair enzymes Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23833795
- 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
- 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
- Saldanha, S. A., Brothers, S. P., Spicer, T., Cameron, M., Mercer, B. A., Chase, P., McDonald, P., Wahlestedt, C., Hodder, P. S. Probe report for NPY-Y2 receptor antagonists Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:21433370
- 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