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Page 1
Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors.
Lau CK, Bayly CI, Gauthier JY, Li CS, Therien M, Asante-Appiah E, Cromlish W, Boie Y, Forghani F, Desmarais S, Wang Q, Skorey K, Waddleton D, Payette P, Ramachandran C, Kennedy BP, Scapin G. Lau CK, et al. Among authors: scapin g. Bioorg Med Chem Lett. 2004 Feb 23;14(4):1043-8. doi: 10.1016/j.bmcl.2003.11.076. Bioorg Med Chem Lett. 2004. PMID: 15013020
Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro)methyl]phosphonic acid, a potent and orally active small molecule PTP1B inhibitor.
Han Y, Belley M, Bayly CI, Colucci J, Dufresne C, Giroux A, Lau CK, Leblanc Y, McKay D, Therien M, Wilson MC, Skorey K, Chan CC, Scapin G, Kennedy BP. Han Y, et al. Among authors: scapin g. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3200-5. doi: 10.1016/j.bmcl.2008.04.064. Epub 2008 Apr 29. Bioorg Med Chem Lett. 2008. PMID: 18477508
Cerastecins inhibit membrane lipooligosaccharide transport in drug-resistant Acinetobacter baumannii.
Wang H, Ishchenko A, Skudlarek J, Shen P, Dzhekieva L, Painter RE, Chen YT, Bukhtiyarova M, Leithead A, Tracy R, Babaoglu K, Bahnck-Teets C, Buevich A, Cabalu TD, Labroli M, Lange H, Lei Y, Li W, Liu J, Mann PA, Meng T, Mitchell HJ, Mulhearn J, Scapin G, Sha D, Shaw AW, Si Q, Tong L, Wu C, Wu Z, Xiao JC, Xu M, Zhang LK, McKenney D, Miller RR, Black TA, Cooke A, Balibar CJ, Klein DJ, Raheem I, Walker SS. Wang H, et al. Among authors: scapin g. Nat Microbiol. 2024 May;9(5):1244-1255. doi: 10.1038/s41564-024-01667-0. Epub 2024 Apr 22. Nat Microbiol. 2024. PMID: 38649414
Structure Guided Discovery of Novel Pan Metallo-β-Lactamase Inhibitors with Improved Gram-Negative Bacterial Cell Penetration.
Dong S, Zhao Z, Tang H, Li G, Pan J, Gu X, Jiang J, Xiao L, Scapin G, Hunter DN, Yang D, Huang Y, Bennett F, Yang SW, Mandal M, Tang H, Su J, Tudge C, deJesus RK, Ding FX, Lombardo M, Hicks JD, Fischmann T, Mirza A, Dayananth P, Painter RE, Villafania A, Garlisi CG, Zhang R, Mayhood TW, Si Q, Li N, Amin RP, Bhatt B, Chen F, Regan CP, Regan H, Lin X, Wu J, Leithead A, Pollack SR, Scott JD, Nargund RP, Therien AG, Black T, Young K, Pasternak A. Dong S, et al. Among authors: scapin g. J Med Chem. 2024 Mar 14;67(5):3400-3418. doi: 10.1021/acs.jmedchem.3c01614. Epub 2024 Feb 22. J Med Chem. 2024. PMID: 38387069
Author Correction: Functionally selective signaling and broad metabolic benefits by novel insulin receptor partial agonists.
Wu M, Carballo-Jane E, Zhou H, Zafian P, Dai G, Liu M, Lao J, Kelly T, Shao D, Gorski J, Pissarnitski D, Kekec A, Chen Y, Previs SF, Scapin G, Gomez-Llorente Y, Hollingsworth SA, Yan L, Feng D, Huo P, Walford G, Erion MD, Kelley DE, Lin S, Mu J. Wu M, et al. Among authors: scapin g. Nat Commun. 2024 Jan 23;15(1):688. doi: 10.1038/s41467-024-44938-4. Nat Commun. 2024. PMID: 38263326 Free PMC article. No abstract available.
Rapid Evolution of a Fragment-like Molecule to Pan-Metallo-Beta-Lactamase Inhibitors: Initial Leads toward Clinical Candidates.
Mandal M, Xiao L, Pan W, Scapin G, Li G, Tang H, Yang SW, Pan J, Root Y, de Jesus RK, Yang C, Prosise W, Dayananth P, Mirza A, Therien AG, Young K, Flattery A, Garlisi C, Zhang R, Chu D, Sheth P, Chu I, Wu J, Markgraf C, Kim HY, Painter R, Mayhood TW, DiNunzio E, Wyss DF, Buevich AV, Fischmann T, Pasternak A, Dong S, Hicks JD, Villafania A, Liang L, Murgolo N, Black T, Hagmann WK, Tata J, Parmee ER, Weber AE, Su J, Tang H. Mandal M, et al. Among authors: scapin g. J Med Chem. 2022 Dec 22;65(24):16234-16251. doi: 10.1021/acs.jmedchem.2c00766. Epub 2022 Dec 7. J Med Chem. 2022. PMID: 36475645
Functionally selective signaling and broad metabolic benefits by novel insulin receptor partial agonists.
Wu M, Carballo-Jane E, Zhou H, Zafian P, Dai G, Liu M, Lao J, Kelly T, Shao D, Gorski J, Pissarnitski D, Kekec A, Chen Y, Previs SF, Scapin G, Gomez-Llorente Y, Hollingsworth SA, Yan L, Feng D, Huo P, Walford G, Erion MD, Kelley DE, Lin S, Mu J. Wu M, et al. Among authors: scapin g. Nat Commun. 2022 Feb 17;13(1):942. doi: 10.1038/s41467-022-28561-9. Nat Commun. 2022. PMID: 35177603 Free PMC article.
105 results