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Mobocertinib (TAK-788): A Targeted Inhibitor of EGFR Exon 20 Insertion Mutants in Non-Small Cell Lung Cancer.
Gonzalvez F, Vincent S, Baker TE, Gould AE, Li S, Wardwell SD, Nadworny S, Ning Y, Zhang S, Huang WS, Hu Y, Li F, Greenfield MT, Zech SG, Das B, Narasimhan NI, Clackson T, Dalgarno D, Shakespeare WC, Fitzgerald M, Chouitar J, Griffin RJ, Liu S, Wong KK, Zhu X, Rivera VM. Gonzalvez F, et al. Among authors: gould ae. Cancer Discov. 2021 Jul;11(7):1672-1687. doi: 10.1158/2159-8290.CD-20-1683. Epub 2021 Feb 25. Cancer Discov. 2021. PMID: 33632773
Discovery of mobocertinib, a potent, oral inhibitor of EGFR exon 20 insertion mutations in non-small cell lung cancer.
Huang WS, Li F, Gong Y, Zhang Y, Youngsaye W, Xu Y, Zhu X, Greenfield MT, Kohlmann A, Taslimi PM, Toms A, Zech SG, Zhou T, Das B, Jang HG, Tugnait M, Ye YE, Gonzalvez F, Baker TE, Nadworny S, Ning Y, Wardwell SD, Zhang S, Gould AE, Hu Y, Lane W, Skene RJ, Zou H, Clackson T, Narasimhan NI, Rivera VM, Dalgarno DC, Shakespeare WC. Huang WS, et al. Among authors: gould ae. Bioorg Med Chem Lett. 2023 Jan 15;80:129084. doi: 10.1016/j.bmcl.2022.129084. Epub 2022 Nov 21. Bioorg Med Chem Lett. 2023. PMID: 36423823 Free article.
Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.
Gould AE, Adams R, Adhikari S, Aertgeerts K, Afroze R, Blackburn C, Calderwood EF, Chau R, Chouitar J, Duffey MO, England DB, Farrer C, Forsyth N, Garcia K, Gaulin J, Greenspan PD, Guo R, Harrison SJ, Huang SC, Iartchouk N, Janowick D, Kim MS, Kulkarni B, Langston SP, Liu JX, Ma LT, Menon S, Mizutani H, Paske E, Renou CC, Rezaei M, Rowland RS, Sintchak MD, Smith MD, Stroud SG, Tregay M, Tian Y, Veiby OP, Vos TJ, Vyskocil S, Williams J, Xu T, Yang JJ, Yano J, Zeng H, Zhang DM, Zhang Q, Galvin KM. Gould AE, et al. J Med Chem. 2011 Mar 24;54(6):1836-46. doi: 10.1021/jm101479y. Epub 2011 Feb 22. J Med Chem. 2011. PMID: 21341678
Identification of Novel Carbocyclic Pyrimidine Cyclic Dinucleotide STING Agonists for Antitumor Immunotherapy Using Systemic Intravenous Route.
Vyskocil S, Cardin D, Ciavarri J, Conlon J, Cullis C, England D, Gershman R, Gigstad K, Gipson K, Gould A, Greenspan P, Griffin R, Gulavita N, Harrison S, Hu Z, Hu Y, Hata A, Huang J, Huang SC, Janowick D, Jones M, Kolev V, Langston SP, Lee HM, Li G, Lok D, Ma L, Mai D, Malley J, Matsuda A, Mizutani H, Mizutani M, Molchanova N, Nunes E, Pusalkar S, Renou C, Rowland S, Sato Y, Shaw M, Shen L, Shi Z, Skene R, Soucy F, Stroud S, Xu H, Xu T, Abu-Yousif AO, Zhang J. Vyskocil S, et al. J Med Chem. 2021 May 27;64(10):6902-6923. doi: 10.1021/acs.jmedchem.1c00374. Epub 2021 May 17. J Med Chem. 2021. PMID: 34000802 Free article.
Optimization of tetrahydronaphthalene inhibitors of Raf with selectivity over hERG.
Huang SC, Adhikari S, Afroze R, Brewer K, Calderwood EF, Chouitar J, England DB, Fisher C, Galvin KM, Gaulin J, Greenspan PD, Harrison SJ, Kim MS, Langston SP, Ma LT, Menon S, Mizutani H, Rezaei M, Smith MD, Zhang DM, Gould AE. Huang SC, et al. Among authors: gould ae. Bioorg Med Chem Lett. 2016 Feb 15;26(4):1156-60. doi: 10.1016/j.bmcl.2016.01.049. Epub 2016 Jan 21. Bioorg Med Chem Lett. 2016. PMID: 26804230
Design of proteasome inhibitors with oral efficacy in vivo against Plasmodium falciparum and selectivity over the human proteasome.
Xie SC, Metcalfe RD, Mizutani H, Puhalovich T, Hanssen E, Morton CJ, Du Y, Dogovski C, Huang SC, Ciavarri J, Hales P, Griffin RJ, Cohen LH, Chuang BC, Wittlin S, Deni I, Yeo T, Ward KE, Barry DC, Liu B, Gillett DL, Crespo-Fernandez BF, Ottilie S, Mittal N, Churchyard A, Ferguson D, Aguiar ACC, Guido RVC, Baum J, Hanson KK, Winzeler EA, Gamo FJ, Fidock DA, Baud D, Parker MW, Brand S, Dick LR, Griffin MDW, Gould AE, Tilley L. Xie SC, et al. Among authors: gould ae. Proc Natl Acad Sci U S A. 2021 Sep 28;118(39):e2107213118. doi: 10.1073/pnas.2107213118. Proc Natl Acad Sci U S A. 2021. PMID: 34548400 Free PMC article.
Novel small-molecule inhibitors of RNA polymerase III.
Wu L, Pan J, Thoroddsen V, Wysong DR, Blackman RK, Bulawa CE, Gould AE, Ocain TD, Dick LR, Errada P, Dorr PK, Parkinson T, Wood T, Kornitzer D, Weissman Z, Willis IM, McGovern K. Wu L, et al. Among authors: gould ae. Eukaryot Cell. 2003 Apr;2(2):256-64. doi: 10.1128/EC.2.2.256-264.2003. Eukaryot Cell. 2003. PMID: 12684375 Free PMC article.
Discovery and optimization of pyrazoline compounds as B-Raf inhibitors.
Duffey MO, Adams R, Blackburn C, Chau RW, Chen S, Galvin KM, Garcia K, Gould AE, Greenspan PD, Harrison S, Huang SC, Kim MS, Kulkarni B, Langston S, Liu JX, Ma LT, Menon S, Nagayoshi M, Rowland RS, Vos TJ, Xu T, Yang JJ, Yu S, Zhang Q. Duffey MO, et al. Among authors: gould ae. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4800-4. doi: 10.1016/j.bmcl.2010.06.113. Epub 2010 Jun 25. Bioorg Med Chem Lett. 2010. PMID: 20634068
Mechanistic study of Uba5 enzyme and the Ufm1 conjugation pathway.
Gavin JM, Hoar K, Xu Q, Ma J, Lin Y, Chen J, Chen W, Bruzzese FJ, Harrison S, Mallender WD, Bump NJ, Sintchak MD, Bence NF, Li P, Dick LR, Gould AE, Chen JJ. Gavin JM, et al. Among authors: gould ae. J Biol Chem. 2014 Aug 15;289(33):22648-22658. doi: 10.1074/jbc.M114.573972. Epub 2014 Jun 25. J Biol Chem. 2014. PMID: 24966333 Free PMC article.
26 results