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GPR139, an Orphan Receptor Highly Enriched in the Habenula and Septum, Is Activated by the Essential Amino Acids L-Tryptophan and L-Phenylalanine.
Liu C, Bonaventure P, Lee G, Nepomuceno D, Kuei C, Wu J, Li Q, Joseph V, Sutton SW, Eckert W, Yao X, Yieh L, Dvorak C, Carruthers N, Coate H, Yun S, Dugovic C, Harrington A, Lovenberg TW. Liu C, et al. Among authors: coate h. Mol Pharmacol. 2015 Nov;88(5):911-25. doi: 10.1124/mol.115.100412. Epub 2015 Sep 8. Mol Pharmacol. 2015. PMID: 26349500
Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor.
Dvorak CA, Coate H, Nepomuceno D, Wennerholm M, Kuei C, Lord B, Woody D, Bonaventure P, Liu C, Lovenberg T, Carruthers NI. Dvorak CA, et al. Among authors: coate h. ACS Med Chem Lett. 2015 Jul 20;6(9):1015-8. doi: 10.1021/acsmedchemlett.5b00247. eCollection 2015 Sep 10. ACS Med Chem Lett. 2015. PMID: 26396690 Free PMC article.
Pharmacology of JNJ-28583113: A novel TRPM2 antagonist.
Fourgeaud L, Dvorak C, Faouzi M, Starkus J, Sahdeo S, Wang Q, Lord B, Coate H, Taylor N, He Y, Qin N, Wickenden A, Carruthers N, Lovenberg TW, Penner R, Bhattacharya A. Fourgeaud L, et al. Among authors: coate h. Eur J Pharmacol. 2019 Jun 15;853:299-307. doi: 10.1016/j.ejphar.2019.03.043. Epub 2019 Apr 6. Eur J Pharmacol. 2019. PMID: 30965058
Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793.
Préville C, Bonaventure P, Koudriakova T, Lord B, Nepomuceno D, Rizzolio M, Mani N, Coe KJ, Ndifor A, Dugovic C, Dvorak CA, Coate H, Pippel DJ, Fitzgerald A, Allison B, Lovenberg TW, Carruthers NI, Shireman BT. Préville C, et al. Among authors: coate h. ACS Med Chem Lett. 2020 Apr 27;11(10):2002-2009. doi: 10.1021/acsmedchemlett.0c00085. eCollection 2020 Oct 8. ACS Med Chem Lett. 2020. PMID: 33062185 Free PMC article.
Discovery of a Series of Substituted 1H-((1,2,3-Triazol-4-yl)methoxy)pyrimidines as Brain Penetrants and Potent GluN2B-Selective Negative Allosteric Modulators.
Gelin CF, Stenne B, Coate H, Hiscox A, Soyode-Johnson A, Wall JL, Lord B, Schoellerman J, Coe KJ, Wang K, Alcázar J, Chrovian CC, Dvorak CA, Carruthers NI, Koudriakova T, Balana B, Letavic MA. Gelin CF, et al. Among authors: coate h. J Med Chem. 2023 Feb 23;66(4):2877-2892. doi: 10.1021/acs.jmedchem.2c01916. Epub 2023 Feb 9. J Med Chem. 2023. PMID: 36757100
Development of small molecule inhibitors of natural killer group 2D receptor (NKG2D).
Wang J, Nakafuku KM, Ziff J, Gelin CF, Gholami H, Thompson AA, Karpowich NK, Limon L, Coate HR, Damm-Ganamet KL, Shih AY, Grant JC, Côte M, Mak PA, Pascual HA, Rives ML, Edwards JP, Venable JD, Venkatesan H, Shi Z, Allen SJ, Sharma S, Kung PP, Shireman BT. Wang J, et al. Among authors: coate hr. Bioorg Med Chem Lett. 2023 Nov 15;96:129492. doi: 10.1016/j.bmcl.2023.129492. Epub 2023 Sep 29. Bioorg Med Chem Lett. 2023. PMID: 37778428
Pharmacological blockade of the DP2 receptor inhibits cigarette smoke-induced inflammation, mucus cell metaplasia, and epithelial hyperplasia in the mouse lung.
Stebbins KJ, Broadhead AR, Baccei CS, Scott JM, Truong YP, Coate H, Stock NS, Santini AM, Fagan P, Prodanovich P, Bain G, Stearns BA, King CD, Hutchinson JH, Prasit P, Evans JF, Lorrain DS. Stebbins KJ, et al. Among authors: coate h. J Pharmacol Exp Ther. 2010 Mar;332(3):764-75. doi: 10.1124/jpet.109.161919. Epub 2009 Dec 8. J Pharmacol Exp Ther. 2010. PMID: 19996299
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.
Stearns BA, Baccei C, Bain G, Broadhead A, Clark RC, Coate H, Evans JF, Fagan P, Hutchinson JH, King C, Lee C, Lorrain DS, Prasit P, Prodanovich P, Santini A, Scott JM, Stock NS, Truong YP. Stearns BA, et al. Among authors: coate h. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4647-51. doi: 10.1016/j.bmcl.2009.06.085. Epub 2009 Jun 25. Bioorg Med Chem Lett. 2009. PMID: 19608418
13 results