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Page 1
The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes.
He S, Ye Z, Truong Q, Shah S, Du W, Guo L, Dobbelaar PH, Lai Z, Liu J, Jian T, Qi H, Bakshi RK, Hong Q, Dellureficio J, Pasternak A, Feng Z, deJesus R, Yang L, Reibarkh M, Bradley SA, Holmes MA, Ball RG, Ruck RT, Huffman MA, Wong F, Samuel K, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Wu M, Shao Q, Trujillo ME, Eiermann GJ, Li C, Zhang BB, Howard AD, Zhou YP, Nargund RP, Hagmann WK. He S, et al. Among authors: yang l. ACS Med Chem Lett. 2012 May 7;3(6):484-9. doi: 10.1021/ml300063m. eCollection 2012 Jun 14. ACS Med Chem Lett. 2012. PMID: 24900499 Free PMC article.
Stimulation of Glucose-Dependent Insulin Secretion by a Potent, Selective sst3 Antagonist.
Pasternak A, Feng Z, de Jesus R, Ye Z, He S, Dobbelaar P, Bradley SA, Chicchi GG, Tsao KL, Trusca D, Eiermann GJ, Li C, Feng Y, Wu M, Shao Q, Zhang BB, Nargund R, Mills SG, Howard AD, Yang L, Zhou YP. Pasternak A, et al. Among authors: yang l. ACS Med Chem Lett. 2012 Feb 27;3(4):289-93. doi: 10.1021/ml200272z. eCollection 2012 Apr 12. ACS Med Chem Lett. 2012. PMID: 24900466 Free PMC article.
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: yang l. 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
Design and synthesis of a new class of malonyl-CoA decarboxylase inhibitors with anti-obesity and anti-diabetic activities.
Tang H, Yan Y, Feng Z, de Jesus RK, Yang L, Levorse DA, Owens KA, Akiyama TE, Bergeron R, Castriota GA, Doebber TW, Ellsworth KP, Lassman ME, Li C, Wu MS, Zhang BB, Chapman KT, Mills SG, Berger JP, Pasternak A. Tang H, et al. Among authors: yang l. Bioorg Med Chem Lett. 2010 Oct 15;20(20):6088-92. doi: 10.1016/j.bmcl.2010.08.047. Epub 2010 Aug 20. Bioorg Med Chem Lett. 2010. PMID: 20832306
3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists.
Walsh SP, Severino A, Zhou C, He J, Liang GB, Tan CP, Cao J, Eiermann GJ, Xu L, Salituro G, Howard AD, Mills SG, Yang L. Walsh SP, et al. Among authors: yang l. Bioorg Med Chem Lett. 2011 Jun 1;21(11):3390-4. doi: 10.1016/j.bmcl.2011.03.114. Epub 2011 Apr 8. Bioorg Med Chem Lett. 2011. PMID: 21514824
Discovery of Selective Small Molecule ROMK Inhibitors as Potential New Mechanism Diuretics.
Tang H, Walsh SP, Yan Y, de Jesus RK, Shahripour A, Teumelsan N, Zhu Y, Ha S, Owens KA, Thomas-Fowlkes BS, Felix JP, Liu J, Kohler M, Priest BT, Bailey T, Brochu R, Alonso-Galicia M, Kaczorowski GJ, Roy S, Yang L, Mills SG, Garcia ML, Pasternak A. Tang H, et al. Among authors: yang l. ACS Med Chem Lett. 2012 Mar 28;3(5):367-72. doi: 10.1021/ml3000066. eCollection 2012 May 10. ACS Med Chem Lett. 2012. PMID: 24900480 Free PMC article.
Discovery of MK-7145, an Oral Small Molecule ROMK Inhibitor for the Treatment of Hypertension and Heart Failure.
Tang H, Zhu Y, Teumelsan N, Walsh SP, Shahripour A, Priest BT, Swensen AM, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Pai LY, Hampton C, Corona A, Hernandez M, Metzger J, Forrest M, Zhou X, Owens K, Tong V, Parmee E, Roy S, Kaczorowski GJ, Yang L, Alonso-Galicia M, Garcia ML, Pasternak A. Tang H, et al. Among authors: yang l. ACS Med Chem Lett. 2016 May 12;7(7):697-701. doi: 10.1021/acsmedchemlett.6b00122. eCollection 2016 Jul 14. ACS Med Chem Lett. 2016. PMID: 27437080 Free PMC article.
Discovery of a potent and selective ROMK inhibitor with improved pharmacokinetic properties based on an octahydropyrazino[2,1-c][1,4]oxazine scaffold.
Zhu Y, de Jesus RK, Tang H, Walsh SP, Jiang J, Gu X, Teumelsan N, Shahripour A, Pio B, Ding FX, Ha S, Priest BT, Swensen AM, Alonso-Galicia M, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Zhou X, Pai LY, Hampton C, Hernandez M, Owens K, Ehrhart J, Roy S, Kaczorowski GJ, Yang L, Parmee ER, Sullivan K, Garcia ML, Pasternak A. Zhu Y, et al. Among authors: yang l. Bioorg Med Chem Lett. 2016 Dec 1;26(23):5695-5702. doi: 10.1016/j.bmcl.2016.10.064. Epub 2016 Oct 24. Bioorg Med Chem Lett. 2016. PMID: 27839686
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