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Scaffold Morphing Identifies 3-Pyridyl Azetidine Ureas as Inhibitors of Nicotinamide Phosphoribosyltransferase (NAMPT).
Palacios DS, Meredith EL, Kawanami T, Adams CM, Chen X, Darsigny V, Palermo M, Baird D, George EL, Guy C, Hewett J, Tierney L, Thigale S, Wang L, Weihofen WA. Palacios DS, et al. Among authors: darsigny v. ACS Med Chem Lett. 2019 Oct 10;10(11):1524-1529. doi: 10.1021/acsmedchemlett.9b00325. eCollection 2019 Nov 14. ACS Med Chem Lett. 2019. PMID: 31749905 Free PMC article.
A small-molecule inhibitor of C5 complement protein.
Jendza K, Kato M, Salcius M, Srinivas H, De Erkenez A, Nguyen A, McLaughlin D, Be C, Wiesmann C, Murphy J, Bolduc P, Mogi M, Duca J, Namil A, Capparelli M, Darsigny V, Meredith E, Tichkule R, Ferrara L, Heyder J, Liu F, Horton PA, Romanowski MJ, Schirle M, Mainolfi N, Anderson K, Michaud GA. Jendza K, et al. Among authors: darsigny v. Nat Chem Biol. 2019 Jul;15(7):666-668. doi: 10.1038/s41589-019-0303-9. Epub 2019 Jun 17. Nat Chem Biol. 2019. PMID: 31209353
Structure based design of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors from a phenotypic screen.
Palacios DS, Meredith E, Kawanami T, Adams C, Chen X, Darsigny V, Geno E, Palermo M, Baird D, Boynton G, Busby SA, George EL, Guy C, Hewett J, Tierney L, Thigale S, Weihofen W, Wang L, White N, Yin M, Argikar UA. Palacios DS, et al. Among authors: darsigny v. Bioorg Med Chem Lett. 2018 Feb 1;28(3):365-370. doi: 10.1016/j.bmcl.2017.12.037. Epub 2017 Dec 18. Bioorg Med Chem Lett. 2018. PMID: 29275937