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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: kohlmann a. 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.
Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.
Huang WS, Liu S, Zou D, Thomas M, Wang Y, Zhou T, Romero J, Kohlmann A, Li F, Qi J, Cai L, Dwight TA, Xu Y, Xu R, Dodd R, Toms A, Parillon L, Lu X, Anjum R, Zhang S, Wang F, Keats J, Wardwell SD, Ning Y, Xu Q, Moran LE, Mohemmad QK, Jang HG, Clackson T, Narasimhan NI, Rivera VM, Zhu X, Dalgarno D, Shakespeare WC. Huang WS, et al. Among authors: kohlmann a. J Med Chem. 2016 May 26;59(10):4948-64. doi: 10.1021/acs.jmedchem.6b00306. Epub 2016 May 12. J Med Chem. 2016. PMID: 27144831
Fragment growing and linking lead to novel nanomolar lactate dehydrogenase inhibitors.
Kohlmann A, Zech SG, Li F, Zhou T, Squillace RM, Commodore L, Greenfield MT, Lu X, Miller DP, Huang WS, Qi J, Thomas RM, Wang Y, Zhang S, Dodd R, Liu S, Xu R, Xu Y, Miret JJ, Rivera V, Clackson T, Shakespeare WC, Zhu X, Dalgarno DC. Kohlmann A, et al. J Med Chem. 2013 Feb 14;56(3):1023-40. doi: 10.1021/jm3014844. Epub 2013 Jan 9. J Med Chem. 2013. PMID: 23302067
Ponatinib inhibits polyclonal drug-resistant KIT oncoproteins and shows therapeutic potential in heavily pretreated gastrointestinal stromal tumor (GIST) patients.
Garner AP, Gozgit JM, Anjum R, Vodala S, Schrock A, Zhou T, Serrano C, Eilers G, Zhu M, Ketzer J, Wardwell S, Ning Y, Song Y, Kohlmann A, Wang F, Clackson T, Heinrich MC, Fletcher JA, Bauer S, Rivera VM. Garner AP, et al. Among authors: kohlmann a. Clin Cancer Res. 2014 Nov 15;20(22):5745-5755. doi: 10.1158/1078-0432.CCR-14-1397. Epub 2014 Sep 19. Clin Cancer Res. 2014. PMID: 25239608 Free PMC article.
Discovery of Novel, Potent Inhibitors of Hydroxy Acid Oxidase 1 (HAO1) Using DNA-Encoded Chemical Library Screening.
Lee ECY, McRiner AJ, Georgiadis KE, Liu J, Wang Z, Ferguson AD, Levin B, von Rechenberg M, Hupp CD, Monteiro MI, Keefe AD, Olszewski A, Eyermann CJ, Centrella P, Liu Y, Arora S, Cuozzo JW, Zhang Y, Clark MA, Huguet C, Kohlmann A. Lee ECY, et al. Among authors: kohlmann a. J Med Chem. 2021 May 27;64(10):6730-6744. doi: 10.1021/acs.jmedchem.0c02271. Epub 2021 May 6. J Med Chem. 2021. PMID: 33955740
Bispecific Estrogen Receptor α Degraders Incorporating Novel Binders Identified Using DNA-Encoded Chemical Library Screening.
Disch JS, Duffy JM, Lee ECY, Gikunju D, Chan B, Levin B, Monteiro MI, Talcott SA, Lau AC, Zhou F, Kozhushnyan A, Westlund NE, Mullins PB, Yu Y, von Rechenberg M, Zhang J, Arnautova YA, Liu Y, Zhang Y, McRiner AJ, Keefe AD, Kohlmann A, Clark MA, Cuozzo JW, Huguet C, Arora S. Disch JS, et al. Among authors: kohlmann a. J Med Chem. 2021 Apr 22;64(8):5049-5066. doi: 10.1021/acs.jmedchem.1c00127. Epub 2021 Apr 12. J Med Chem. 2021. PMID: 33844532
160 results