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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. Among authors: lin s. 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
Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists.
Zhou C, Tang C, Chang E, Ge M, Lin S, Cline E, Tan CP, Feng Y, Zhou YP, Eiermann GJ, Petrov A, Salituro G, Meinke P, Mosley R, Akiyama TE, Einstein M, Kumar S, Berger J, Howard AD, Thornberry N, Mills SG, Yang L. Zhou C, et al. Among authors: lin s. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1298-301. doi: 10.1016/j.bmcl.2009.10.052. Epub 2009 Oct 15. Bioorg Med Chem Lett. 2010. PMID: 20064714
A novel series of indazole-/indole-based glucagon receptor antagonists.
Lin S, Zhang F, Jiang G, Qureshi SA, Yang X, Chicchi GG, Tota L, Bansal A, Brady E, Trujillo M, Salituro G, Miller C, Tata JR, Zhang BB, Parmee ER. Lin S, et al. Bioorg Med Chem Lett. 2015 Oct 1;25(19):4143-7. doi: 10.1016/j.bmcl.2015.08.015. Epub 2015 Aug 8. Bioorg Med Chem Lett. 2015. PMID: 26303893
Glucagon receptor antagonism induces increased cholesterol absorption.
Guan HP, Yang X, Lu K, Wang SP, Castro-Perez JM, Previs S, Wright M, Shah V, Herath K, Xie D, Szeto D, Forrest G, Xiao JC, Palyha O, Sun LP, Andryuk PJ, Engel SS, Xiong Y, Lin S, Kelley DE, Erion MD, Davis HR, Wang L. Guan HP, et al. Among authors: lin s. J Lipid Res. 2015 Nov;56(11):2183-95. doi: 10.1194/jlr.M060897. Epub 2015 Sep 15. J Lipid Res. 2015. PMID: 26373568 Free PMC article.
Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus.
Xu J, Lin S, Myers RW, Addona G, Berger JP, Campbell B, Chen HS, Chen Z, Eiermann GJ, Elowe NH, Farrer BT, Feng W, Fu Q, Kats-Kagan R, Kavana M, Malkani S, McMasters DR, Mitra K, Pachanski MJ, Tong X, Trujillo ME, Xu L, Zhang B, Zhang F, Zhang R, Parmee ER. Xu J, et al. Among authors: lin s. Bioorg Med Chem Lett. 2017 May 1;27(9):2069-2073. doi: 10.1016/j.bmcl.2016.10.085. Epub 2016 Oct 31. Bioorg Med Chem Lett. 2017. PMID: 28284804
Discovery of orally active hepatoselective glucokinase activators for treatment of Type II Diabetes Mellitus.
Xu J, Lin S, Myers RW, Trujillo ME, Pachanski MJ, Malkani S, Chen HS, Chen Z, Campbell B, Eiermann GJ, Elowe N, Farrer BT, Feng W, Fu Q, Kats-Kagan R, Kavana M, McMasters DR, Mitra K, Tong X, Xu L, Zhang F, Zhang R, Addona GH, Berger JP, Zhang B, Parmee ER. Xu J, et al. Among authors: lin s. Bioorg Med Chem Lett. 2017 May 1;27(9):2063-2068. doi: 10.1016/j.bmcl.2016.10.088. Epub 2016 Oct 31. Bioorg Med Chem Lett. 2017. PMID: 28284809
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. Among authors: lin s. Diabetes. 2018 Feb;67(2):299-308. doi: 10.2337/db17-0577. Epub 2017 Nov 2. Diabetes. 2018. PMID: 29097375
A glucose-responsive insulin therapy protects animals against hypoglycemia.
Yang R, Wu M, Lin S, Nargund RP, Li X, Kelly T, Yan L, Dai G, Qian Y, Dallas-Yang Q, Fischer PA, Cui Y, Shen X, Huo P, Feng DD, Erion MD, Kelley DE, Mu J. Yang R, et al. Among authors: lin s. JCI Insight. 2018 Jan 11;3(1):e97476. doi: 10.1172/jci.insight.97476. eCollection 2018 Jan 11. JCI Insight. 2018. PMID: 29321379 Free PMC article.
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