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Page 1
GPR120 suppresses adipose tissue lipolysis and synergizes with GPR40 in antidiabetic efficacy.
Satapati S, Qian Y, Wu MS, Petrov A, Dai G, Wang SP, Zhu Y, Shen X, Muise ES, Chen Y, Zycband E, Weinglass A, Di Salvo J, Debenham JS, Cox JM, Lan P, Shah V, Previs SF, Erion M, Kelley DE, Wang L, Howard AD, Shang J. Satapati S, et al. Among authors: howard ad. J Lipid Res. 2017 Aug;58(8):1561-1578. doi: 10.1194/jlr.M075044. Epub 2017 Jun 5. J Lipid Res. 2017. PMID: 28583918 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: howard ad. 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. Among authors: howard ad. 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: howard ad. 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
Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40.
Lu J, Byrne N, Wang J, Bricogne G, Brown FK, Chobanian HR, Colletti SL, Di Salvo J, Thomas-Fowlkes B, Guo Y, Hall DL, Hadix J, Hastings NB, Hermes JD, Ho T, Howard AD, Josien H, Kornienko M, Lumb KJ, Miller MW, Patel SB, Pio B, Plummer CW, Sherborne BS, Sheth P, Souza S, Tummala S, Vonrhein C, Webb M, Allen SJ, Johnston JM, Weinglass AB, Sharma S, Soisson SM. Lu J, et al. Among authors: howard ad. Nat Struct Mol Biol. 2017 Jul;24(7):570-577. doi: 10.1038/nsmb.3417. Epub 2017 Jun 5. Nat Struct Mol Biol. 2017. PMID: 28581512
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: howard ad. 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.
GPR40 (FFAR1) - Combined Gs and Gq signaling in vitro is associated with robust incretin secretagogue action ex vivo and in vivo.
Hauge M, Vestmar MA, Husted AS, Ekberg JP, Wright MJ, Di Salvo J, Weinglass AB, Engelstoft MS, Madsen AN, Lückmann M, Miller MW, Trujillo ME, Frimurer TM, Holst B, Howard AD, Schwartz TW. Hauge M, et al. Among authors: howard ad. Mol Metab. 2014 Oct 24;4(1):3-14. doi: 10.1016/j.molmet.2014.10.002. eCollection 2015 Jan. Mol Metab. 2014. PMID: 25685685 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
153 results