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Trzupek, John
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Trzupek, John

Graduate Student
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Positions

  • 2018 - Vice President, Head of Corporate Development, KSQ Therapeutics

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  • Doctoral Dissertation
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Publications

recent publications
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  • academic article

    • Schnute, M. E., Wennerstal, M., Alley, J., Bengtsson, M., Blinn, J. R., Bolten, C. W., Braden, T., Bonn, T., Carlsson, B., Caspers, N., Chen, M., Choi, C., et al. Discovery of 3-cyano-N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo 2,3-b pyridin-5-yObenzamide: a potent, selective, and orally bioavailable retinoic acid receptor related orphan receptor C2 inverse agonist Journal of Medicinal Chemistry  2018 61:10415-10439  DOI:10.1021/acs.jmedchern.8b00392  PMID:30130103
    • Vazquez, M. L., Kaila, N., Strohbach, J. W., Trzupek, J. D., Brown, M. F., Flanagan, M. E., Mitton-Fry, M. J., Johnson, T. A., TenBrink, R. E., Arnold, E. P., Basak, A., Heasley, S. E., et al. Identification of N-{cis-3-(methyl(7H-pyrrolo 2,3-d pyrimidin-4-yl)aminolcyclobutyl}propan e-1-sulfonamide (PF-04965842): a selective JAK1 clinical candidate for the treatment of autoimmune diseases Journal of Medicinal Chemistry  2018 61:1130-1152  DOI:10.1021/acs.jmedchem.7b01598  PMID:29298069
    • Lee, K. L., Ambler, C. M., Anderson, D. R., Boscoe, B. P., Bree, A. G., Brodfuehrer, J. I., Chang, J. S., Choi, C., Chung, S., Curran, K. J., Day, J. E., Dehnhardt, C. M., et al. Discovery of clinical candidate 1-{ (2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl methoxy}-7-methoxyi soquinoline-6-carboxamide (PF-06650833), a potent, selective inhibitor of interleukin-1 receptor associated kinase 4 (IRAK4), by fragment -based drug design Journal of Medicinal Chemistry  2017 60:5521-5542  DOI:10.1021/acs.jmedchem.7b00231  PMID:28498658
    • Gerstenberger, B. S., Trzupek, J. D., Tallant, C., Fedorov, O., Filippakopoulos, P., Brennan, P. E., Fedele, V., Martin, S., Picaud, S., Rogers, C., Parikh, M., Taylor, A., et al. Identification of a chemical probe for family VIII bromodomains through optimization of a fragment hit Journal of Medicinal Chemistry  2016 59:4800-4811  DOI:10.1021/acs.jmedchem.6b00012  PMID:27115555  PMCID:PMC5034155
    • Fedorov, O., Castex, J., Tallant, C., Owen, D. R., Martin, S., Aldeghi, M., Monteiro, O., Filippakopoulos, P., Picaud, S., Trzupek, J. D., Gerstenberger, B. S., Bountra, C., et al. Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance Science Advances  2015 1  DOI:10.1126/sciadv.1500723  PMID:26702435  PMCID:PMC4681344
    • Fish, P. V., Filippakopoulos, P., Bish, G., Brennan, P. E., Bunnage, M. E., Cook, A. S., Federov, O., Gerstenberger, B. S., Jones, H., Knapp, S., Marsden, B., Nocka, K., et al. Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit Journal of Medicinal Chemistry  2012 55:9831-9837  DOI:10.1021/jm3010515  PMID:23095041  PMCID:PMC3506127
    • Trzupek, J. D., Li, C., Chan, C., Crowley, B. M., Heimann, A. C., Danishefsky, S. J. Lessons from the total synthesis of (+/-)-phalarine: insights into the mechanism of the Pictet-Spengler reaction Pure and Applied Chemistry  2010 82:1735-1748  DOI:10.1351/pac-con-09-11-14  PMID:20711493  PMCID:PMC2920150
    • Trzupek, J. D., Lee, D., Crowley, B. M., Marathias, V. M., Danishefsky, S. J. Total synthesis of enantiopure phalarine via a stereospecific Pictet-Spengler reaction: traceless transfer of chirality from L-tryptophan Journal of the American Chemical Society  2010 132:8506-8512  DOI:10.1021/ja1030968  PMID:20509657  PMCID:PMC2895623
    • degree-related publication Shimamura, H., Breazzano, S. P., Garfunkle, J., Kimball, F. S., Trzupek, J. D., Boger, D. L. Total synthesis of complestatin: development of a Pd(0)-mediated indole annulation for macrocyclization Journal of the American Chemical Society  2010 132:7776-7783  DOI:10.1021/ja102304p  PMID:20469945  PMCID:PMC2892899
    • degree-related publication Garfunkle, J., Kimball, F. S., Trzupek, J. D., Takizawa, S., Shimamura, H., Tomishima, M., Boger, D. L. Total synthesis of chloropeptin II (complestatin) and chloropeptin I Journal of the American Chemical Society  2009 131:16036-16038  DOI:10.1021/ja907193b  PMID:19839632  PMCID:PMC2783344
    • Kan, C., Trzupek, J. D., Wu, B., Chen, G., Tan, Z., Yuan, Y., Danishefsky, S. J. Toward homogeneous erythropoietin: chemical synthesis of the Ala1-Gly28 glycopeptide domain by "alanine" ligation Journal of the American Chemical Society  2009 131:5438-5443  DOI:10.1021/ja808707w  PMID:19334679  PMCID:PMC2765573
    • degree-related publication Jin, W., Trzupek, J. D., Rayl, T. J., Broward, M. A., Vielhauer, G. A., Weir, S. J., Hwang, I., Boger, D. L. A unique class of duocarmycin and CC-1065 analogues subject to reductive activation Journal of the American Chemical Society  2007 129:15391-15397  DOI:10.1021/ja075398e  PMID:18020335  PMCID:PMC2519901
    • degree-related publication Tichenor, M. S., MacMillan, K. S., Trzupek, J. D., Rayl, T. J., Hwang, I., Boger, D. L. Systematic exploration of the structural features of yatakemycin impacting DNA alkylation and biological activity Journal of the American Chemical Society  2007 129:10858-10869  DOI:10.1021/ja072777z  PMID:17691783  PMCID:PMC2519902
    • degree-related publication Tichenor, M. S., Trzupek, J. D., Kastrinsky, D. B., Shiga, F., Hwang, I., Boger, D. L. Asymmetric total synthesis of (+)- and ent-(-)-yatakemycin and duocarmycin SA: evaluation of yatakemycin key partial structures and its unnatural enantiomer Journal of the American Chemical Society  2006 128:15683-15696  DOI:10.1021/ja064228j  PMID:17147378  PMCID:PMC2515590
    • degree-related publication Trzupek, J. D., Gottesfeld, J. M., Boger, D. L. Alkylation of duplex DNA in nucleosome core particles by duocarmycin SA and yatakemycin Nature Chemical Biology  2006 2:79-82  DOI:10.1038/nchembio761  PMID:16415862
    • Toth, J. L., Trzupek, J. D., Flores, L. V., Kiakos, K., Hartley, J. A., Pennington, W. T., Lee, M. A novel achiral seco-amino-cyclopropylindoline (CI) analog of CC-1065 and the duocarmycins: design, synthesis and biological studies Medicinal Chemistry (Shariqah (United Arab Emirates))  2005 1:13-9  PMID:16789881
    • Trzupek, J. D., Sheppard, T. L. Photochemical generation of ribose abasic sites in RNA oligonucleotides Organic Letters  2005 7:1493-1496  DOI:10.1021/ol050120h  PMID:15816735
    • Kupchinsky, S., Centioni, S., Howard, T., Trzupek, J., Roller, S., Carnahan, V., Townes, H., Purnell, B., Price, C., Handl, H., Summerville, K., Johnson, K., et al. A novel class of achiral seco-analogs of CC-1065 and the duocarmycins: design, synthesis, DNA binding, and anticancer properties Bioorganic & Medicinal Chemistry  2004 12:6221-6236  DOI:10.1016/j.bmc.2004.08.051  PMID:15519165
    • degree-related publication Parrish, J. P., Trzupek, J. D., Hughes, T. V., Hwang, I., Boger, D. L. Synthesis and evaluation of N-aryl and N-alkenyl CBI derivatives Bioorganic & Medicinal Chemistry  2004 12:5845-5856  DOI:10.1016/j.bmc.2004.08.032  PMID:15498660
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Background

education and training

  • M.B.A. in Finance, The University of Chicago , Booth School of Business, high honors 2011 - 2013
  • Ph.D. in Chemistry, Scripps Research 2001 - 2006
  • B.A. in Chemistry, Northwestern University , cum laude and with honors 1997 - 2001

advisee of

  • graduate advising relationship

    • Boger, Dale, Ph.D.  candidacy, 2002 - 2006
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Contact

full name

  • John David Trzupek

geographic location

  • Scripps California 

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