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Page 1
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: thomas fowlkes b. 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.
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: thomas fowlkes bs. 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 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: thomas fowlkes b. 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.
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: thomas fowlkes bs. 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 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: thomas fowlkes b. PLoS One. 2017 May 23;12(5):e0176182. doi: 10.1371/journal.pone.0176182. eCollection 2017. PLoS One. 2017. PMID: 28542610 Free PMC article.
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: thomas fowlkes b. 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
Improvement of hERG-ROMK index of spirocyclic ROMK inhibitors through scaffold optimization and incorporation of novel pharmacophores.
Dong S, VanGelder K, Shi ZC, Yu Y, Wu Z, Ferguson R, Guo ZZ, Tang H, Frie J, Fu Q, Gu X, Priest BT, Thomas-Fowlkes B, Weinglass A, Margulis M, Liu J, Pai LY, Hampton C, Haimbach RE, Owens K, Tong V, Xu S, Hu M, Zingaro GJ, Morissette P, Ehrhart J, Roy S, Sullivan K, Pasternak A. Dong S, et al. Among authors: thomas fowlkes b. Bioorg Med Chem Lett. 2017 Jun 1;27(11):2559-2566. doi: 10.1016/j.bmcl.2017.03.086. Epub 2017 Mar 30. Bioorg Med Chem Lett. 2017. PMID: 28431879
Discovery of MK-8153, a Potent and Selective ROMK Inhibitor and Novel Diuretic/Natriuretic.
Jiang J, Ding FX, Zhou X, Bateman TJ, Dong S, Gu X, Keh deJesus R, Pio B, Tang H, Chobanian HR, Levorse D, Hu M, Thomas-Fowlkes B, Margulis M, Koehler M, Weinglass A, Gibson J, Houle K, Yudkovitz J, Hampton C, Pai LY, Samuel K, Cutarelli T, Sullivan K, Parmee ER, Davies I, Pasternak A. Jiang J, et al. Among authors: thomas fowlkes b. J Med Chem. 2021 Jun 10;64(11):7691-7701. doi: 10.1021/acs.jmedchem.1c00406. Epub 2021 May 26. J Med Chem. 2021. PMID: 34038119
The design and synthesis of novel spirocyclic heterocyclic sulfone ROMK inhibitors as diuretics.
Chobanian HR, Guo Y, Pio B, Tang H, Teumelsan N, Clements M, Frie J, Ferguson R, Guo Z, Thomas-Fowlkes BS, Felix JP, Liu J, Kohler M, Priest B, Hampton C, Pai LY, Corona A, Metzger J, Tong V, Joshi EM, Xu L, Owens K, Maloney K, Sullivan K, Pasternak A. Chobanian HR, et al. Among authors: thomas fowlkes bs. Bioorg Med Chem Lett. 2017 Feb 15;27(4):1109-1114. doi: 10.1016/j.bmcl.2016.10.032. Epub 2016 Oct 13. Bioorg Med Chem Lett. 2017. PMID: 28111141
Discovery of a Potent and Selective ROMK Inhibitor with Pharmacokinetic Properties Suitable for Preclinical Evaluation.
Walsh SP, Shahripour A, Tang H, Teumelsan N, Frie J, Zhu Y, Priest BT, Swensen AM, Liu J, Margulis M, Visconti R, Weinglass A, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Alonso-Galicia M, Zhou X, Pai LY, Corona A, Hampton C, Hernandez M, Bentley R, Chen J, Shah K, Metzger J, Forrest M, Owens K, Tong V, Ha S, Roy S, Kaczorowski GJ, Yang L, Parmee E, Garcia ML, Sullivan K, Pasternak A. Walsh SP, et al. ACS Med Chem Lett. 2015 May 7;6(7):747-52. doi: 10.1021/ml500440u. eCollection 2015 Jul 9. ACS Med Chem Lett. 2015. PMID: 26191360 Free PMC article.
19 results