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Petrassi, Mike

Vice President, Medicinal Chemistry, Calibr

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  • Bakowski, M. A., Shiroodi, R. K., Liu, R., Olejniczak, J., Yang, B., Gagaring, K., Guo, H., White, P. M., Chappell, L., Debec, A., Landmann, F., Dubben, B., et al. Discovery of short-course antiwolbachial quinazolines for elimination of filarial worm infections Science Translational Medicine  2019 11  DOI:10.1126/scitranslmed.aav3523  PMID:31068442
  • Janes, J., Young, M. E., Chen, E., Rogers, N. H., Burgstaller-Muehlbacher, S., Hughes, L. D., Love, M. S., Hull, M. V., Kuhen, K. L., Woods, A. K., Joseph, S. B., Petrassi, H. M., et al. The ReFRAME library as a comprehensive drug repurposing library and its application to the treatment of cryptosporidiosis Proceedings of the National Academy of Sciences of the United States of America  2018 115:10750-10755  DOI:10.1073/pnas.1810137115  PMID:30282735  PMCID:PMC6196526
  • Huang, L., Kushner, N. L., Theriault, M. E., Pisu, D., Tan, S. M., McNamara, C. W., Petrassi, H. M., Russell, D. G., Brown, A. C. The deconstructed granuloma: a complex high-throughput drug screening platform for the discovery of host-directed therapeutics against tuberculosis Frontiers in Cellular and Infection Microbiology  2018 8  DOI:10.3389/fcimb.2018.00275  PMID:30155446  PMCID:PMC6102409
  • Harbut, M. B., Yang, B., Liu, R., Yano, T., Vilcheze, C., Cheng, B., Lockner, J. W., Guo, H., Yu, C., Franzblau, S. G., Petrassi, H. M., Jacobs, W. R., et al. Small molecules targeting mycobacterium tuberculosis type II NADH dehydrogenase exhibit antimycobacterial activity Angewandte Chemie-International Edition  2018 57:3478-3482  DOI:10.1002/anie.201800260  PMID:29388301
  • Choi, S. H., Mahankali, M., Lee, S. J., Hull, M., Petrassi, H. M., Chatterjee, A. K., Schultz, P. G., Jones, K. A., Shen, W. Targeted disruption of Myc-Max oncoprotein complex by a small molecule ACS Chemical Biology  2017 12:2715-2719  DOI:10.1021/acschembio.7b00799  PMID:28976731
  • Brand, M. D., Goncalves, R. L. S., Orr, A. L., Vargas, L., Gerencser, A. A., Jensen, M. B., Wang, Y. T., Melov, S., Turk, C. N., Matzen, J. T., Dardov, V. J., Petrassi, H. M., et al. Suppressors of superoxide-H2O2 production at site I-Q of mitochondrial complex I protect against stem cell hyperplasia and ischemia-reperfusion injury Cell Metabolism  2016 24:582-592  DOI:10.1016/j.cmet.2016.08.012  PMID:27667666  PMCID:PMC5061631
  • Orr, D. L., Vargas, L., Turk, C. N., Baaten, J. E., Matzen, J. T., Dardov, V. J., Attle, S. J., Li, J., Quackenbush, D. C., Goncalves, R. L. S., Perevoshchikova, I. V., Petrassi, H. M., et al. Suppressors of superoxide production from mitochondrial complex III Nature Chemical Biology  2015 11:834-U36  DOI:10.1038/nchembio.1910  PMID:26368590  PMCID:PMC4618194
  • Syeda, R., Xu, J., Dubin, A. E., Coste, B., Mathur, J., Huynh, T., Matzen, J., Lao, J., Tully, D. C., Engels, I. H., Petrassi, H. M., Schumacher, A. M., et al. Chemical activation of the mechanotransduction channel Piezo1 Elife  2015 4:e07369  DOI:10.7554/eLife.07369  PMID:26001275  PMCID:PMC4456433
  • Rooney, L., Vidal, A., D'Souza, A. M., Devereux, N., Masick, B., Boissel, V., West, R., Head, V., Stringer, R., Lao, J., Petrus, M. J., Patapoutian, A., et al. Discovery, optimization, and biological evaluation of 5-(2-(trifluoromethyl)phenyl)indazoles as a novel class of transient receptor potential A1 (TRPA1) antagonists Journal of Medicinal Chemistry  2014 57:5129-5140  DOI:10.1021/jm401986p  PMID:24884675
  • Liu, B., Lee, Y., Zou, J., Petrassi, H. M., Joseph, R. W., Chao, W., Michelotti, E. L., Bukhtiyarova, M., Springman, E. B., Dorsey, B. D. Discovery and SAR of a series of 4,6-diamino-1,3,5-triazin-2-ol as novel non-nucleoside reverse transcriptase inhibitors of HIV-1 Bioorganic & Medicinal Chemistry Letters  2010 20:6592-6596  DOI:10.1016/j.bmcl.2010.09.034  PMID:20888224
  • Li, J., Petrassi, H. M., Tumanut, C., Masick, B. T., Trussell, C., Harris, J. L. Substrate optimization for monitoring cathepsin C activity in live cells Bioorganic & Medicinal Chemistry  2009 17:1064-1070  DOI:10.1016/j.bmc.2008.02.002  PMID:18313933
  • Tully, D. C., Vidal, A., Chatterjee, A. K., Williams, J. A., Roberts, M. J., Petrassi, H. M., Spraggon, G., Bursulaya, B., Pacoma, R., Shipway, A., Schumacher, A. M., Danahay, H., et al. Discovery of inhibitors of the channel-activating protease prostasin (CAP1/PRSS8) utilizing structure-based design Bioorganic & Medicinal Chemistry Letters  2008 18:5895-5899  DOI:10.1016/j.bmcl.2008.08.029  PMID:18752942
  • Petrassi, H. M., Williams, J. A., Li, J., Tumanut, C., Ek, J., Nakai, T., Masick, B., Backes, B. J., Harris, J. L. A strategy to profile prime and non-prime proteolytic substrate specificity Bioorganic & Medicinal Chemistry Letters  2005 15:3162-3166  DOI:10.1016/j.bmcl.2005.04.019  PMID:15878267
  • Petrassi, H. M., Johnson, S. M., Purkey, H. E., Chiang, K. P., Walkup, T., Jiang, X., Powers, E. T., Kelly, J. W. Potent and selective structure-based dibenzofuran inhibitors of transthyretin amyloidogenesis: Kinetic stabilization of the native state Journal of the American Chemical Society  2005 127:6662-6671  DOI:10.1021/ja044351f  PMID:15869287
  • Johnson, S. M., Petrassi, H. M., Palaninathan, S. K., Mohamedmohaideen, N. N., Purkey, H. E., Nichols, C., Chiang, K. P., Walkup, T., Sacchettini, J. C., Sharpless, K. B., Kelly, J. W. Bisaryloxime ethers as potent inhibitors of transthyretin amyloid fibril formation Journal of Medicinal Chemistry  2005 48:1576-1587  DOI:10.1021/jm049274d  PMID:15743199
  • McCammon, M. G., Scott, D. J., Keetch, C. A., Greene, L. H., Purkey, H. E., Petrassi, H. M., Kelly, J. W., Robinson, C. V. Screening transthyretin amyloid fibril inhibitors: Characterization of novel multiprotein, multiligand complexes by mass spectrometry Structure  2002 10:851-863  DOI:10.1016/s0969-2126(02)00771-2  PMID:12057199
  • Oza, V. B., Smith, C., Raman, P., Koepf, E. K., Lashuel, H. A., Petrassi, H. M., Chiang, K. P., Powers, E. T., Sachettinni, J., Kelly, J. W. Synthesis, structure, and activity of diclofenac analogues as transthyretin amyloid fibril formation inhibitors Journal of Medicinal Chemistry  2002 45:321-332  DOI:10.1021/jm010257n  PMID:11784137
  • Jiang, X., Smith, C. S., Petrassi, H. M., Hammarstrom, P., White, J. T., Sacchettini, J. C., Kelly, J. W. An engineered transthyretin monomer that is nonamyloidogenic, unless it is partially denatured Biochemistry  2001 40:11442-11452  DOI:10.1021/bi011194d  PMID:11560492
  • Petrassi, H. M., Sharpless, K. B., Kelly, J. W. The copper-mediated cross coupling of phenylboronic acids and N-hydroxyphthalimide at room temperature: synthesis of aryloxyamines Organic Letters  2001 3:139-142  DOI:10.1021/ol0003533  PMID:11429858
  • Petrassi, H. M., Klabunde, T., Sacchettini, J., Kelly, J. W. Structure-based design of N-phenyl phenoxazine transthyretin amyloid fibril inhibitors Journal of the American Chemical Society  2000 122:2178-2192  DOI:10.1021/ja993309v
  • Klabunde, T., Petrassi, H. M., Oza, V. B., Raman, P., Kelly, J. W., Sacchettini, J. C. Rational design of potent human transthyretin amyloid disease inhibitors Nature Structural Biology  2000 7:312-321  DOI:10.1038/74082  PMID:10742177
  • Koepf, E. K., Petrassi, H. M., Ratnaswamy, G., Huff, M. E., Sudol, M., Kelly, J. W. Characterization of the structure and function of W -> F WW domain variants: identification of a natively unfolded protein that folds upon ligand binding Biochemistry  1999 38:14338-14351  DOI:10.1021/bi991105l  PMID:10572009
  • Koepf, E. K., Petrassi, H. M., Sudol, M., Kelly, J. W. WW: An isolated three-stranded antiparallel β-sheet domain that unfolds and refolds reversibly; evidence for a structured hydrophobic cluster in urea and GdnHCl and a disordered thermal unfolded state Protein Science  1999 8:841-853  DOI:10.1110/ps.8.4.841  PMID:10211830  PMCID:PMC2144315
  • Oza, V. B., Petrassi, H. M., Purkey, H. E., Kelly, J. W. Synthesis and evaluation of anthranilic acid-based transthyretin amyloid fibril inhibitors Bioorganic & Medicinal Chemistry Letters  1999 9:1-6  DOI:10.1016/s0960-894x(98)00696-9  PMID:9990446
  • Kabza, K. G., Gestwicki, J. E., McGrath, J. L., Petrassi, H. M. Effect off microwave radiation on copper(II) 2,2'-bipyridyl-mediated hydrolysis of bis(p-nitrophenyl) phosphodiester and enzymatic hydrolysis of carbohydrates Journal of Organic Chemistry  1996 61:9599-9602  DOI:10.1021/jo961357h

Background

education and training

• Ph.D. in Chemistry, Scripps Research 1997 - 2001
• Texas A&M University , Chemistry 1996 - 1997
• B.S. in Chemistry, State University of New York College at Fredonia 1994 - 1996

advisee of

• graduate advising relationship

  • Kelly, Jeffery, Ph.D.  candidacy, 1998 - 2001

Contact

full name

• Hank Michael James Petrassi

geographic location

• Scripps California