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Petrassi, Mike
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Petrassi, Mike

Vice President, Medicinal Chemistry, Calibr
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Publications

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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
    • degree-related publication 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
    • degree-related publication 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
    • degree-related publication 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
    • degree-related publication 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
    • degree-related publication 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
    • degree-related publication 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
    • degree-related publication 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
    • degree-related publication 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
    • degree-related publication 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
    • degree-related publication 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
    • degree-related publication 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
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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
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Contact

full name

  • Hank Michael James Petrassi

geographic location

  • Scripps California 

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