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Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor.
McClure KF, Jackson M, Cameron KO, Kung DW, Perry DA, Orr ST, Zhang Y, Kohrt J, Tu M, Gao H, Fernando D, Jones R, Erasga N, Wang G, Polivkova J, Jiao W, Swartz R, Ueno H, Bhattacharya SK, Stock IA, Varma S, Bagdasarian V, Perez S, Kelly-Sullivan D, Wang R, Kong J, Cornelius P, Michael L, Lee E, Janssen A, Steyn SJ, Lapham K, Goosen T. McClure KF, et al. Among authors: kong j. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5410-4. doi: 10.1016/j.bmcl.2013.07.044. Epub 2013 Jul 30. Bioorg Med Chem Lett. 2013. PMID: 23953189
Orally active and brain permeable proline amides as highly selective 5HT2c agonists for the treatment of obesity.
Liu KK, Lefker BA, Dombroski MA, Chiang P, Cornelius P, Patterson TA, Zeng Y, Santucci S, Tomlinson E, Gibbons CP, Marala R, Brown JA, Kong JX, Lee E, Werner W, Wenzel Z, Giragossian C, Chen H, Coffey SB. Liu KK, et al. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2365-9. doi: 10.1016/j.bmcl.2010.01.107. Epub 2010 Jan 25. Bioorg Med Chem Lett. 2010. PMID: 20202843
Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate.
Bhattacharya SK, Andrews K, Beveridge R, Cameron KO, Chen C, Dunn M, Fernando D, Gao H, Hepworth D, Jackson VM, Khot V, Kong J, Kosa RE, Lapham K, Loria PM, Londregan AT, McClure KF, Orr ST, Patel J, Rose C, Saenz J, Stock IA, Storer G, VanVolkenburg M, Vrieze D, Wang G, Xiao J, Zhang Y. Bhattacharya SK, et al. Among authors: kong j. ACS Med Chem Lett. 2014 Feb 24;5(5):474-9. doi: 10.1021/ml400473x. eCollection 2014 May 8. ACS Med Chem Lett. 2014. PMID: 24900864 Free PMC article.
Pharmacological characterization of the first in class clinical candidate PF-05190457: a selective ghrelin receptor competitive antagonist with inverse agonism that increases vagal afferent firing and glucose-dependent insulin secretion ex vivo.
Kong J, Chuddy J, Stock IA, Loria PM, Straub SV, Vage C, Cameron KO, Bhattacharya SK, Lapham K, McClure KF, Zhang Y, Jackson VM. Kong J, et al. Br J Pharmacol. 2016 May;173(9):1452-64. doi: 10.1111/bph.13439. Epub 2016 Mar 17. Br J Pharmacol. 2016. PMID: 26784385 Free PMC article.
Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment of Appetite Loss.
Garnsey MR, Smith AC, Polivkova J, Arons AL, Bai G, Blakemore C, Boehm M, Buzon LM, Campion SN, Cerny M, Chang SC, Coffman K, Farley KA, Fonseca KR, Ford KK, Garren J, Kong JX, Koos MRM, Kung DW, Lian Y, Li MM, Li Q, Martinez-Alsina LA, O'Connor R, Ogilvie K, Omoto K, Raymer B, Reese MR, Ryder T, Samp L, Stevens KA, Widlicka DW, Yang Q, Zhu K, Fortin JP, Sammons MF. Garnsey MR, et al. Among authors: kong jx. J Med Chem. 2023 Mar 9;66(5):3195-3211. doi: 10.1021/acs.jmedchem.2c02012. Epub 2023 Feb 19. J Med Chem. 2023. PMID: 36802610
An inverse agonist of orphan receptor GPR61 acts by a G protein-competitive allosteric mechanism.
Lees JA, Dias JM, Rajamohan F, Fortin JP, O'Connor R, Kong JX, Hughes EAG, Fisher EL, Tuttle JB, Lovett G, Kormos BL, Unwalla RJ, Zhang L, Dechert Schmitt AM, Zhou D, Moran M, Stevens KA, Fennell KF, Varghese AE, Maxwell A, Cote EE, Zhang Y, Han S. Lees JA, et al. Among authors: kong jx. Nat Commun. 2023 Sep 23;14(1):5938. doi: 10.1038/s41467-023-41646-3. Nat Commun. 2023. PMID: 37741852 Free PMC article.
4,933 results