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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: miller c, miller mw. 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 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. 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. 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.
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. 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: miller mw. 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
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: miller mw. 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.
MLi-2, a Potent, Selective, and Centrally Active Compound for Exploring the Therapeutic Potential and Safety of LRRK2 Kinase Inhibition.
Fell MJ, Mirescu C, Basu K, Cheewatrakoolpong B, DeMong DE, Ellis JM, Hyde LA, Lin Y, Markgraf CG, Mei H, Miller M, Poulet FM, Scott JD, Smith MD, Yin Z, Zhou X, Parker EM, Kennedy ME, Morrow JA. Fell MJ, et al. J Pharmacol Exp Ther. 2015 Dec;355(3):397-409. doi: 10.1124/jpet.115.227587. Epub 2015 Sep 25. J Pharmacol Exp Ther. 2015. PMID: 26407721
Discovery of phenyl acetamides as potent and selective GPR119 agonists.
Zhu C, Wang L, Zhu Y, Guo ZZ, Liu P, Hu Z, Szewczyk JW, Kang L, Chicchi G, Ehrhardt A, Woods A, Seo T, Woods M, van Heek M, Dingley KH, Pang J, Salituro GM, Powell J, Terebetski JL, Hornak V, Campeau LC, Orr RK, Ujjainwalla F, Miller M, Stamford A, Wood HB, Kowalski T, Nargund RP, Edmondson SD. Zhu C, et al. Bioorg Med Chem Lett. 2017 Mar 1;27(5):1124-1128. doi: 10.1016/j.bmcl.2017.01.091. Epub 2017 Feb 1. Bioorg Med Chem Lett. 2017. PMID: 28185720
The discovery of N-((2H-tetrazol-5-yl)methyl)-4-((R)-1-((5r,8R)-8-(tert-butyl)-3-(3,5-dichlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl)-4,4-dimethylpentyl)benzamide (SCH 900822): a potent and selective glucagon receptor antagonist.
DeMong D, Dai X, Hwa J, Miller M, Lin SI, Kang L, Stamford A, Greenlee W, Yu W, Wong M, Lavey B, Kozlowski J, Zhou G, Yang DY, Patel B, Soriano A, Zhai Y, Sondey C, Zhang H, Lachowicz J, Grotz D, Cox K, Morrison R, Andreani T, Cao Y, Liang M, Meng T, McNamara P, Wong J, Bradley P, Feng KI, Belani J, Chen P, Dai P, Gauuan J, Lin P, Zhao H. DeMong D, et al. J Med Chem. 2014 Mar 27;57(6):2601-10. doi: 10.1021/jm401858f. Epub 2014 Feb 26. J Med Chem. 2014. PMID: 24527772
Design of Potent and Orally Active GPR119 Agonists for the Treatment of Type II Diabetes.
Liu P, Hu Z, DuBois BG, Moyes CR, Hunter DN, Zhu C, Kar NF, Zhu Y, Garfunkle J, Kang L, Chicchi G, Ehrhardt A, Woods A, Seo T, Woods M, van Heek M, Dingley KH, Pang J, Salituro GM, Powell J, Terebetski JL, Hornak V, Campeau LC, Lamberson J, Ujjainwalla F, Miller M, Stamford A, Wood HB, Kowalski T, Nargund RP, Edmondson SD. Liu P, et al. ACS Med Chem Lett. 2015 Jul 10;6(8):936-41. doi: 10.1021/acsmedchemlett.5b00207. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288697 Free PMC article.
950 results