recent publications

• academic article

  • 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
  • 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
  • Han, C., Chatterjee, A., Noetzel, M. J., Panarese, J. D., Smith, E., Chase, P., Hodder, P., Niswender, C., Conn, P. J., Lindsley, C. W., Stauffer, S. R. Discovery and SAR of muscarinic receptor subtype 1 (M-1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-Dibenzyl-2H-pyrazolo 4,3-c quinolin-3(5H)-ones as positive allosteric modulators Bioorganic & Medicinal Chemistry Letters  2015 25:384-388  DOI:10.1016/j.bmcl.2014.11.011  PMID:25435150  PMCID:PMC4278958
  • 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
  • Gentry, P. R., Kokubo, M., Bridges, T. M., Noetzel, M. J., Cho, H. P., Lamsal, A., Smith, E., Chase, P., Hodder, P. S., Niswender, C. M., Daniels, J. S., Conn, P. J., et al. Development of a highly potent, novel M(5) positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)pipe ridine-4-carboxamide (ML380) Journal of Medicinal Chemistry  2014 57:7804-7810  DOI:10.1021/jm500995y  PMID:25147929  PMCID:PMC4175000
  • Gentry, P. R., Kokubo, M., Bridges, T. M., Cho, H. P., Smith, E., Chase, P., Hodder, P. S., Utley, T. J., Rajapakse, A., Byers, F., Niswender, C. M., Morrison, R. D., et al. Discovery, synthesis and characterization of a highly muscarinic acetylcholine receptor (mAChR)-selective M5-orthosteric antagonist, VU0488130 (ML381): a novel molecular probe ChemMedChem  2014 9:1677-1682  DOI:10.1002/cmdc.201402051  PMID:24692176  PMCID:PMC4116439
  • 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
  • Yan, F., Yu, Y., Chow, D. C., Palzkill, T., Madoux, F., Hodder, P., Chase, P., Griffin, P. R., O'Malley, B. W., Lonard, D. M. Identification of verrucarin a as a potent and selective steroid receptor coactivator-3 small molecule inhibitor PLoS One  2014 9:e95243  DOI:10.1371/journal.pone.0095243  PMID:24743578  PMCID:PMC3990629
  • Lewallen, D. M., Bicker, K. L., Madoux, F., Chase, P., Anguish, L., Coonrod, S., Hodder, P., Thompson, P. R. A FluoPol-ABPP PAD2 high-throughput screen identifies the first calcium site inhibitor targeting the PADs ACS Chemical Biology  2014 9:913-921  DOI:10.1021/cb400841k  PMID:24467619  PMCID:PMC4108211
  • Wang, Y., Lonard, D. M., Yu, Y., Chow, D. C., Palzkill, T. G., Wang, J., Qi, R., Matzuk, A. J., Song, X., Madoux, F., Hodder, P., Chase, P., et al. Bufalin is a potent small-molecule inhibitor of the steroid receptor coactivators SRC-3 and SRC-1 Cancer Research  2014 74:1506-1517  DOI:10.1158/0008-5472.can-13-2939  PMID:24390736  PMCID:PMC3947477
  • Lewallen, D. M., Sreelatha, A., Dharmarajan, V., Madoux, F., Chase, P., Griffin, P. R., Orth, K., Hodder, P., Thompson, P. R. Inhibiting AMPylation: a novel screen to identify the first small molecule inhibitors of protein AMPylation ACS Chemical Biology  2014 9:433-442  DOI:10.1021/cb4006886  PMID:24274060  PMCID:PMC3944102
  • Gentry, P. R., Kokubo, M., Bridges, T. M., Kett, N. R., Harp, J. M., Cho, H. P., Smith, E., Chase, P., Hodder, P. S., Niswender, C. M., Daniels, J. S., Conn, P. J., et al. Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375) Journal of Medicinal Chemistry  2013 56:9351-9355  DOI:10.1021/jm4013246  PMID:24164599  PMCID:PMC3876027
  • Turlington, M., Chun, A., Tomar, S., Eggler, A., Grum-Tokars, V., Jacobs, J., Daniels, J. S., Dawson, E., Saldanha, A., Chase, P., Baez-Santos, Y. M., Lindsley, C. W., et al. Discovery of N-(benzo 1,2,3 triazol-1-yl)-N-(benzyl)acetamido)phenyl) carboxamides as severe acute respiratory syndrome coronavirus (SARS-CoV) 3CLpro inhibitors: Identification of ML300 and noncovalent nanomolar inhibitors with an induced-fit binding Bioorganic & Medicinal Chemistry Letters  2013 23:6172-6177  DOI:10.1016/j.bmcl.2013.08.112  PMID:24080461  PMCID:PMC3878165
  • Gentry, P. R., Bridges, T. M., Lamsal, A., Vinson, P. N., Smith, E., Chase, P., Hodder, P. S., Engers, J. L., Niswender, C. M., Daniels, J. S., Conn, P. J., Wood, M. R., et al. Discovery of ML326: The first sub-micromolar, selective M-5 PAM Bioorganic & Medicinal Chemistry Letters  2013 23:2996-3000  DOI:10.1016/j.bmcl.2013.03.032  PMID:23562060  PMCID:PMC3634896
  • 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
  • Qin, Q., Knapinska, A., Dobri, N., Madoux, F., Chase, P., Hodder, P., Petrukhin, K. In pursuit of synthetic modulators for the orphan retina-specific nuclear receptor NR2E3 Journal of Ocular Pharmacology and Therapeutics  2013 29:298-309  DOI:10.1089/jop.2012.0135  PMID:23098562  PMCID:PMC3613967
  • Jacobs, J., Grum-Tokars, V., Zhou, Y., Turlington, M., Saldanha, S. A., Chase, P., Eggler, A., Dawson, E. S., Baez-Santos, Y. M., Tomar, S., Mielech, A. M., Baker, S. C., et al. Discovery, synthesis, and structure-based optimization of a series of n-(tert-butyl)-2-(n-arylamido)-2-(pyridin-3-yl) acetamides (ml188) as potent noncovalent small molecule inhibitors of the severe acute respiratory syndrome coronavirus (sars-cov) 3cl protease Journal of Medicinal Chemistry  2013 56:534-546  DOI:10.1021/jm301580n  PMID:23231439  PMCID:PMC3569073
  • 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
  • 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
  • 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
  • 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., 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
  • Madoux, F., Simanski, S., Chase, P., Mishra, J. K., Roush, W. R., Ayad, N. G., Hodder, P. An ultra-high throughput cell-based screen for wee1 degradation inhibitors Journal of Biomolecular Screening  2010 15:907-917  DOI:10.1177/1087057110375848  PMID:20660794  PMCID:PMC3082437
  • 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
  • Grimm, C., Jors, S., Saldanha, S. A., Obukhov, A. G., Pan, B. F., Oshima, K., Cuajungco, M. P., Chase, P., Hodder, P., Heller, S. Small molecule activators of TRPML3 Chemistry & Biology  2010 17:135-148  DOI:10.1016/j.chembiol.2009.12.016  PMID:20189104  PMCID:PMC2834294
  • Tanaka, K., Koresawa, M., Iida, M., Fukasawa, K., Stec, E., Cassaday, J., Chase, P., Rickert, K., Hodder, P., Takagi, T., Komatani, H. Multiplexed random peptide library and phospho-specific antibodies facilitate human polo-like kinase 1 inhibitor screen Assay and Drug Development Technologies  2010 8:47-62  DOI:10.1089/adt.2009.0212  PMID:20085455  PMCID:PMC3532019
  • 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
  • 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
  • Madoux, F., Li, X. L., Chase, P., Zastrow, G., Cameron, M. D., Conkright, J. J., Griffin, P. R., Thacher, S., Hodder, P. Potent, selective and cell penetrant inhibitors of SF-1 by functional ultra-high-throughput screening Molecular Pharmacology  2008 73:1776-1784  DOI:10.1124/mol.108.045963  PMID:18334597  PMCID:PMC3228235
  • 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
  • Zuck, P., O'Donnell, G. T., Cassaday, J., Chase, P., Hodder, P., Strulovici, B., Ferrer, M. Miniaturization of absorbance assays using the fluorescent properties of white microplates Analytical Biochemistry  2005 342:254-259  DOI:10.1016/j.ab.2005.04.029  PMID:15949786

• report

  • 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
  • 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
  • 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