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Page 1
Optimization of Preclinical Metabolism for Somatostatin Receptor Subtype 5-Selective Antagonists.
Liu W, Hussain Z, Zang Y, Sweis RF, Romero FA, Finke PE, Moningka R, Bao J, Plotkin MA, Shang J, Dingley KH, Salituro G, Murphy BA, Howard AD, Ujjainwalla F, Wood HB, Duffy JL. Liu W, et al. Among authors: howard ad. ACS Med Chem Lett. 2018 Oct 5;9(11):1088-1093. doi: 10.1021/acsmedchemlett.8b00306. eCollection 2018 Nov 8. ACS Med Chem Lett. 2018. PMID: 30429950 Free PMC article.
Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes.
Guo L, Parker DL, Zang Y, Sweis RF, Liu W, Sherer EC, Buist N, Terebetski J, Kelly T, Bugianesi R, Priest BT, Dingley KH, Li X, Mitelman S, Salituro G, Trujillo ME, Pachanski M, Kirkland M, Powles MA, Eiermann GJ, Feng Y, Shang J, Howard AD, Ujjainwalla F, Sinz CJ, Debenham JS, Edmondson SD, Nargund RP, Hagmann WK, Li D. Guo L, et al. Among authors: howard ad. ACS Med Chem Lett. 2016 Oct 12;7(12):1107-1111. doi: 10.1021/acsmedchemlett.6b00314. eCollection 2016 Dec 8. ACS Med Chem Lett. 2016. PMID: 27994747 Free PMC article.
Discovery and Pharmacology of a Novel Somatostatin Subtype 5 (SSTR5) Antagonist: Synergy with DPP-4 Inhibition.
Liu W, Shao PP, Liang GB, Bawiec J, He J, Aster SD, Wu M, Chicchi G, Wang J, Tsao KL, Shang J, Salituro G, Zhou YP, Li C, Akiyama TE, Metzger DE, Murphy BA, Howard AD, Weber AE, Duffy JL. Liu W, et al. Among authors: howard ad. ACS Med Chem Lett. 2018 Sep 12;9(11):1082-1087. doi: 10.1021/acsmedchemlett.8b00305. eCollection 2018 Nov 8. ACS Med Chem Lett. 2018. PMID: 30429949 Free PMC article.
Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects.
Lombardo M, Bender K, London C, Plotkin MA, Kirkland M, Mane J, Pachanski M, Geissler W, Cummings J, Habulihaz B, Akiyama TE, Di Salvo J, Madeira M, Pols J, Powles MA, Finley MF, Johnson E, Roussel T, Uebele VN, Crespo A, Leung D, Alleyne C, Trusca D, Lei Y, Howard AD, Ujjainwalla F, Tata JR, Sinz CJ. Lombardo M, et al. Among authors: howard ad. Bioorg Med Chem Lett. 2016 Dec 1;26(23):5724-5728. doi: 10.1016/j.bmcl.2016.10.054. Epub 2016 Oct 24. Bioorg Med Chem Lett. 2016. PMID: 27815121
Design of potent and selective GPR119 agonists for type II diabetes.
Szewczyk JW, Acton J, Adams AD, Chicchi G, Freeman S, Howard AD, Huang Y, Li C, Meinke PT, Mosely R, Murphy E, Samuel R, Santini C, Yang M, Zhang Y, Zhao K, Wood HB. Szewczyk JW, et al. Among authors: howard ad. Bioorg Med Chem Lett. 2011 May 1;21(9):2665-9. doi: 10.1016/j.bmcl.2010.12.086. Epub 2010 Dec 22. Bioorg Med Chem Lett. 2011. PMID: 21273063
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: howard ad. 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
Corrigendum to "Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects" [Bioorg. Med. Chem. Lett. 26 (2016) 5724-5728].
Lombardo M, Bender K, London C, Plotkin MA, Kirkland M, Mane J, Pachanski M, Geissler W, Cummings J, Habulihaz B, Akiyama TE, Di Salvo J, Madeira M, Pols J, Powles MA, Finley MF, Johnson E, Roussel T, Uebele VN, Crespo A, Leung D, Alleyne C, Trusca D, Lei Y, Howard AD, Ujjainwalla F, Tata JR, Sinz CJ. Lombardo M, et al. Among authors: howard ad. Bioorg Med Chem Lett. 2017 Mar 1;27(5):1333. doi: 10.1016/j.bmcl.2017.01.082. Epub 2017 Feb 4. Bioorg Med Chem Lett. 2017. PMID: 28169160 No abstract available.
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: howard ad. 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
Diamine Derivatives as Novel Small-Molecule, Potent, and Subtype-Selective Somatostatin SST3 Receptor Agonists.
Li D, Wu Z, Yu Y, Ball RG, Guo L, Sherer E, He S, Hong Q, Lai Z, Qi H, Truong Q, Yang DX, Chicchi GG, Tsao KL, Trusca D, Trujillo M, Pachanski M, Eiermann GJ, Howard AD, Zhou YP, Zhang BB, Nargund RP, Hagmann WK. Li D, et al. Among authors: howard ad. ACS Med Chem Lett. 2014 Apr 24;5(6):690-5. doi: 10.1021/ml500079u. eCollection 2014 Jun 12. ACS Med Chem Lett. 2014. PMID: 24944745 Free PMC article.
Structure-Activity Relationship of Novel and Selective Biaryl-Chroman GPR40 AgoPAMs.
Chen HY, Plummer CW, Xiao D, Chobanian HR, DeMong D, Miller M, Trujillo ME, Kirkland M, Kosinski D, Mane J, Pachanski M, Cheewatrakoolpong B, Di Salvo J, Thomas-Fowlkes B, Souza S, Tatosian DA, Chen Q, Hafey MJ, Houle R, Nolting AF, Orr R, Ehrhart J, Weinglass AB, Tschirret-Guth R, Howard AD, Colletti SL. Chen HY, et al. Among authors: howard ad. ACS Med Chem Lett. 2018 Jun 14;9(7):685-690. doi: 10.1021/acsmedchemlett.8b00149. eCollection 2018 Jul 12. ACS Med Chem Lett. 2018. PMID: 30034601 Free PMC article.
152 results