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Page 1
GPR40 partial agonist MK-2305 lower fasting glucose in the Goto Kakizaki rat via suppression of endogenous glucose production.
Miller C, Pachanski MJ, Kirkland ME, Kosinski DT, Mane J, Bunzel M, Cao J, Souza S, Thomas-Fowlkes B, Di Salvo J, Weinglass AB, Li X, Myers RW, Knagge K, Carrington PE, Hagmann WK, Trujillo ME. Miller C, et al. Among authors: pachanski mj. PLoS One. 2017 May 23;12(5):e0176182. doi: 10.1371/journal.pone.0176182. eCollection 2017. PLoS One. 2017. PMID: 28542610 Free PMC article.
GPR40 reduces food intake and body weight through GLP-1.
Gorski JN, Pachanski MJ, Mane J, Plummer CW, Souza S, Thomas-Fowlkes BS, Ogawa AM, Weinglass AB, Di Salvo J, Cheewatrakoolpong B, Howard AD, Colletti SL, Trujillo ME. Gorski JN, et al. Among authors: pachanski mj. Am J Physiol Endocrinol Metab. 2017 Jul 1;313(1):E37-E47. doi: 10.1152/ajpendo.00435.2016. Epub 2017 Mar 14. Am J Physiol Endocrinol Metab. 2017. PMID: 28292762 Free article.
GPR40 partial agonists and AgoPAMs: Differentiating effects on glucose and hormonal secretions in the rodent.
Pachanski MJ, Kirkland ME, Kosinski DT, Mane J, Cheewatrakoolpong B, Xue J, Szeto D, Forrest G, Miller C, Bunzel M, Plummer CW, Chobanian HR, Miller MW, Souza S, Thomas-Fowlkes BS, Ogawa AM, Weinglass AB, Di Salvo J, Li X, Feng Y, Tatosian DA, Howard AD, Colletti SL, Trujillo ME. Pachanski MJ, et al. PLoS One. 2017 Oct 20;12(10):e0186033. doi: 10.1371/journal.pone.0186033. eCollection 2017. PLoS One. 2017. PMID: 29053717 Free PMC article.
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
Pio B, Chobanian HR, Guo Y, Josien H, Hagmann WK, Miller M, Trujillo ME, Kirkland M, Kosinski D, Mane J, Pachanski M, Cheewatrakoolpong B, Ashley E, Orr R, Wright MJ, Bugianesi R, Souza S, Zhang X, Di Salvo J, Weinglass AB, Tschirret-Guth R, Samuel K, Chen Q, Shang J, Lamca J, Ehrhart J, Nargund R, Howard AD, Colletti SL. Pio B, et al. Among authors: pachanski m. Bioorg Med Chem Lett. 2019 Jul 15;29(14):1842-1848. doi: 10.1016/j.bmcl.2019.04.050. Epub 2019 May 2. Bioorg Med Chem Lett. 2019. PMID: 31109791
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. 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 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.
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: pachanski m. 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.
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
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. 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.
15 results