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Page 1
A novel insulin secretagogue is a phosphodiesterase inhibitor.
Leibowitz MD, Biswas C, Brady EJ, Conti M, Cullinan CA, Hayes NS, Manganiello VC, Saperstein R, Wang LH, Zafian PT, et al. Leibowitz MD, et al. Among authors: zafian pt. Diabetes. 1995 Jan;44(1):67-74. doi: 10.2337/diab.44.1.67. Diabetes. 1995. PMID: 7813816
Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor.
Duffy JL, Kirk BA, Konteatis Z, Campbell EL, Liang R, Brady EJ, Candelore MR, Ding VD, Jiang G, Liu F, Qureshi SA, Saperstein R, Szalkowski D, Tong S, Tota LM, Xie D, Yang X, Zafian P, Zheng S, Chapman KT, Zhang BB, Tata JR. Duffy JL, et al. Bioorg Med Chem Lett. 2005 Mar 1;15(5):1401-5. doi: 10.1016/j.bmcl.2005.01.003. Bioorg Med Chem Lett. 2005. PMID: 15713396
Engineering Glucose Responsiveness Into Insulin.
Kaarsholm NC, Lin S, Yan L, Kelly T, van Heek M, Mu J, Wu M, Dai G, Cui Y, Zhu Y, Carballo-Jane E, Reddy V, Zafian P, Huo P, Shi S, Antochshuk V, Ogawa A, Liu F, Souza SC, Seghezzi W, Duffy JL, Erion M, Nargund RP, Kelley DE. Kaarsholm NC, et al. Diabetes. 2018 Feb;67(2):299-308. doi: 10.2337/db17-0577. Epub 2017 Nov 2. Diabetes. 2018. PMID: 29097375
Discovery of Insulin Receptor Partial Agonists MK-5160 and MK-1092 as Novel Basal Insulins with Potential to Improve Therapeutic Index.
Pissarnitski DA, Kekec A, Yan L, Zhu Y, Feng DD, Huo P, Madsen-Duggan C, Moyes CR, Nargund RP, Kelly T, Zhang X, Carballo-Jane E, Gorski J, Zafian P, Qatanani M, Kaarsholm N, Meng F, Jia X, Lee KJ, Wang W, Xu S, Hohn MJ, Iammarino MJ, McCoy MA, Okoh GA, Liang Y, Hollingsworth SA, Erion MD, Kelley DE, Garbaccio RM, Zhang A, Mu J, Lin S. Pissarnitski DA, et al. J Med Chem. 2022 Apr 14;65(7):5593-5605. doi: 10.1021/acs.jmedchem.1c02073. Epub 2022 Mar 17. J Med Chem. 2022. PMID: 35298158
Erratum. Engineering Glucose Responsiveness Into Insulin. Diabetes 2018;67:299-308.
Kaarsholm NC, Lin S, Yan L, Kelly T, van Heek M, Mu J, Wu M, Dai G, Cui Y, Zhu Y, Carballo-Jane E, Reddy V, Zafian P, Huo P, Shi S, Antochshuk V, Ogawa A, Liu F, Souza SC, Seghezzi W, Duffy JL, Erion M, Nargund RP, Kelley DE. Kaarsholm NC, et al. Diabetes. 2018 May;67(5):1030. doi: 10.2337/db18-er05a. Epub 2018 Feb 27. Diabetes. 2018. PMID: 29487114 Free PMC article. No abstract available.
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. Nat Commun. 2022 Feb 17;13(1):942. doi: 10.1038/s41467-022-28561-9. Nat Commun. 2022. PMID: 35177603 Free PMC article.
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