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Discovery of Nanomolar DCAF1 Small Molecule Ligands.
Li ASM, Kimani S, Wilson B, Noureldin M, González-Álvarez H, Mamai A, Hoffer L, Guilinger JP, Zhang Y, von Rechenberg M, Disch JS, Mulhern CJ, Slakman BL, Cuozzo JW, Dong A, Poda G, Mohammed M, Saraon P, Mittal M, Modh P, Rathod V, Patel B, Ackloo S, Santhakumar V, Szewczyk MM, Barsyte-Lovejoy D, Arrowsmith CH, Marcellus R, Guié MA, Keefe AD, Brown PJ, Halabelian L, Al-Awar R, Vedadi M. Li ASM, et al. Among authors: zhang y. J Med Chem. 2023 Apr 13;66(7):5041-5060. doi: 10.1021/acs.jmedchem.2c02132. Epub 2023 Mar 22. J Med Chem. 2023. PMID: 36948210 Free PMC article.
Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas.
Vaswani RG, Gehling VS, Dakin LA, Cook AS, Nasveschuk CG, Duplessis M, Iyer P, Balasubramanian S, Zhao F, Good AC, Campbell R, Lee C, Cantone N, Cummings RT, Normant E, Bellon SF, Albrecht BK, Harmange JC, Trojer P, Audia JE, Zhang Y, Justin N, Chen S, Wilson JR, Gamblin SJ. Vaswani RG, et al. Among authors: zhang y. J Med Chem. 2016 Nov 10;59(21):9928-9941. doi: 10.1021/acs.jmedchem.6b01315. Epub 2016 Oct 28. J Med Chem. 2016. PMID: 27739677 Free PMC article.
Discovery of cofactor-specific, bactericidal Mycobacterium tuberculosis InhA inhibitors using DNA-encoded library technology.
Soutter HH, Centrella P, Clark MA, Cuozzo JW, Dumelin CE, Guie MA, Habeshian S, Keefe AD, Kennedy KM, Sigel EA, Troast DM, Zhang Y, Ferguson AD, Davies G, Stead ER, Breed J, Madhavapeddi P, Read JA. Soutter HH, et al. Among authors: zhang y. Proc Natl Acad Sci U S A. 2016 Dec 6;113(49):E7880-E7889. doi: 10.1073/pnas.1610978113. Epub 2016 Nov 18. Proc Natl Acad Sci U S A. 2016. PMID: 27864515 Free PMC article.
Structure Based Design of Non-Natural Peptidic Macrocyclic Mcl-1 Inhibitors.
Johannes JW, Bates S, Beigie C, Belmonte MA, Breen J, Cao S, Centrella PA, Clark MA, Cuozzo JW, Dumelin CE, Ferguson AD, Habeshian S, Hargreaves D, Joubran C, Kazmirski S, Keefe AD, Lamb ML, Lan H, Li Y, Ma H, Mlynarski S, Packer MJ, Rawlins PB, Robbins DW, Shen H, Sigel EA, Soutter HH, Su N, Troast DM, Wang H, Wickson KF, Wu C, Zhang Y, Zhao Q, Zheng X, Hird AW. Johannes JW, et al. Among authors: zhang y. ACS Med Chem Lett. 2016 Dec 27;8(2):239-244. doi: 10.1021/acsmedchemlett.6b00464. eCollection 2017 Feb 9. ACS Med Chem Lett. 2016. PMID: 28197319 Free PMC article.
Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action.
Fernández-Montalván AE, Berger M, Kuropka B, Koo SJ, Badock V, Weiske J, Puetter V, Holton SJ, Stöckigt D, Ter Laak A, Centrella PA, Clark MA, Dumelin CE, Sigel EA, Soutter HH, Troast DM, Zhang Y, Cuozzo JW, Keefe AD, Roche D, Rodeschini V, Chaikuad A, Díaz-Sáez L, Bennett JM, Fedorov O, Huber KVM, Hübner J, Weinmann H, Hartung IV, Gorjánácz M. Fernández-Montalván AE, et al. Among authors: zhang y. ACS Chem Biol. 2017 Nov 17;12(11):2730-2736. doi: 10.1021/acschembio.7b00708. Epub 2017 Oct 24. ACS Chem Biol. 2017. PMID: 29043777 Free PMC article.
Correction to "Structure Based Design of Non-Natural Peptidic Macrocyclic Mcl-1 Inhibitors".
Johannes JW, Bates S, Beigie C, Belmonte MA, Breen J, Cao S, Centrella PA, Clark MA, Cuozzo JW, Dumelin CE, Ferguson AD, Habeshian S, Hargreaves D, Joubran C, Kazmirski S, Keefe AD, Lamb ML, Lan H, Li Y, Ma H, Mlynarski S, Packer MJ, Rawlins PB, Robbins DW, Shen H, Sigel EA, Soutter HH, Su N, Troast DM, Wang H, Wickson KF, Wu C, Zhang Y, Zhao Q, Zheng X, Hird AW. Johannes JW, et al. Among authors: zhang y. ACS Med Chem Lett. 2017 Oct 18;8(11):1204. doi: 10.1021/acsmedchemlett.7b00397. eCollection 2017 Nov 9. ACS Med Chem Lett. 2017. PMID: 29152055 Free PMC article.
Agonists and Antagonists of Protease-Activated Receptor 2 Discovered within a DNA-Encoded Chemical Library Using Mutational Stabilization of the Target.
Brown DG, Brown GA, Centrella P, Certel K, Cooke RM, Cuozzo JW, Dekker N, Dumelin CE, Ferguson A, Fiez-Vandal C, Geschwindner S, Guié MA, Habeshian S, Keefe AD, Schlenker O, Sigel EA, Snijder A, Soutter HT, Sundström L, Troast DM, Wiggin G, Zhang J, Zhang Y, Clark MA. Brown DG, et al. Among authors: zhang j, zhang y. SLAS Discov. 2018 Jun;23(5):429-436. doi: 10.1177/2472555217749847. Epub 2018 Jan 9. SLAS Discov. 2018. PMID: 29316408 Free article.
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