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Page 1
Discovery of Novel UDP-N-Acetylglucosamine Acyltransferase (LpxA) Inhibitors with Activity against Pseudomonas aeruginosa.
Ryan MD, Parkes AL, Corbett D, Dickie AP, Southey M, Andersen OA, Stein DB, Barbeau OR, Sanzone A, Thommes P, Barker J, Cain R, Compper C, Dejob M, Dorali A, Etheridge D, Evans S, Faulkner A, Gadouleau E, Gorman T, Haase D, Holbrow-Wilshaw M, Krulle T, Li X, Lumley C, Mertins B, Napier S, Odedra R, Papadopoulos K, Roumpelakis V, Spear K, Trimby E, Williams J, Zahn M, Keefe AD, Zhang Y, Soutter HT, Centrella PA, Clark MA, Cuozzo JW, Dumelin CE, Deng B, Hunt A, Sigel EA, Troast DM, DeJonge BLM. Ryan MD, et al. Among authors: sigel ea. J Med Chem. 2021 Oct 14;64(19):14377-14425. doi: 10.1021/acs.jmedchem.1c00888. Epub 2021 Sep 27. J Med Chem. 2021. PMID: 34569791
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: sigel ea. 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: sigel ea. 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: sigel ea. 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: sigel ea. 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: sigel ea. SLAS Discov. 2018 Jun;23(5):429-436. doi: 10.1177/2472555217749847. Epub 2018 Jan 9. SLAS Discov. 2018. PMID: 29316408 Free article.
Machine Learning on DNA-Encoded Libraries: A New Paradigm for Hit Finding.
McCloskey K, Sigel EA, Kearnes S, Xue L, Tian X, Moccia D, Gikunju D, Bazzaz S, Chan B, Clark MA, Cuozzo JW, Guié MA, Guilinger JP, Huguet C, Hupp CD, Keefe AD, Mulhern CJ, Zhang Y, Riley P. McCloskey K, et al. Among authors: sigel ea. J Med Chem. 2020 Aug 27;63(16):8857-8866. doi: 10.1021/acs.jmedchem.0c00452. Epub 2020 Jun 11. J Med Chem. 2020. PMID: 32525674
14 results