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Page 1
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: pachanski m. 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.
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: pachanski m. 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.
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.
Shah SK, He S, Guo L, Truong Q, Qi H, Du W, Lai Z, Liu J, Jian T, Hong Q, Dobbelaar P, Ye Z, Sherer E, Feng Z, Yu Y, Wong F, Samuel K, Madiera M, Karanam BV, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Feng Y, Wu M, Shao Q, Trujillo ME, Eiermann GJ, Li C, Pachanski M, Fernandez G, Nelson D, Bunting P, Morissette P, Volksdorf S, Kerr J, Zhang BB, Howard AD, Zhou YP, Pasternak A, Nargund RP, Hagmann WK. Shah SK, et al. Among authors: pachanski m. ACS Med Chem Lett. 2015 Mar 18;6(5):513-7. doi: 10.1021/ml500514w. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005524 Free PMC article.
Design, Synthesis, and Evaluation of Novel and Selective G-protein Coupled Receptor 120 (GPR120) Spirocyclic Agonists.
Cox JM, Chu HD, Chelliah MV, Debenham JS, Eagen K, Lan P, Lombardo M, London C, Plotkin MA, Shah U, Sun Z, Vaccaro HM, Venkatraman S, Suzuki T, Wang N, Ashley ER, Crespo A, Madeira M, Leung DH, Alleyne C, Ogawa AM, Souza S, Thomas-Fowlkes B, Di Salvo J, Weinglass A, Kirkland M, Pachanski M, Powles MA, Tozzo E, Akiyama TE, Ujjainwalla F, Tata JR, Sinz CJ. Cox JM, et al. Among authors: pachanski m. ACS Med Chem Lett. 2016 Nov 17;8(1):49-54. doi: 10.1021/acsmedchemlett.6b00360. eCollection 2017 Jan 12. ACS Med Chem Lett. 2016. PMID: 28105274 Free PMC article.
Design and Synthesis of Novel, Selective GPR40 AgoPAMs.
Plummer CW, Clements MJ, Chen H, Rajagopalan M, Josien H, Hagmann WK, Miller M, Trujillo ME, Kirkland M, Kosinski D, Mane J, Pachanski M, Cheewatrakoolpong B, Nolting AF, Orr R, Christensen M, Campeau LC, Wright MJ, Bugianesi R, Souza S, Zhang X, Di Salvo J, Weinglass AB, Tschirret-Guth R, Nargund R, Howard AD, Colletti SL. Plummer CW, et al. Among authors: pachanski m. ACS Med Chem Lett. 2017 Jan 23;8(2):221-226. doi: 10.1021/acsmedchemlett.6b00443. eCollection 2017 Feb 9. ACS Med Chem Lett. 2017. PMID: 28197316 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: pachanski mj. 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: pachanski mj. 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
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: pachanski m. 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
Discovery of Chromane Propionic Acid Analogues as Selective Agonists of GPR120 with in Vivo Activity in Rodents.
Adams GL, Velazquez F, Jayne C, Shah U, Miao S, Ashley ER, Madeira M, Akiyama TE, Di Salvo J, Suzuki T, Wang N, Truong Q, Gilbert E, Zhou D, Verras A, Kirkland M, Pachanski M, Powles M, Yin W, Ujjainwalla F, Venkatraman S, Edmondson SD. Adams GL, et al. Among authors: pachanski m. ACS Med Chem Lett. 2016 Dec 6;8(1):96-101. doi: 10.1021/acsmedchemlett.6b00394. eCollection 2017 Jan 12. ACS Med Chem Lett. 2016. PMID: 28105282 Free PMC article.
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: pachanski m. 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.
15 results