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Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties.
Bridges TM, Brady AE, Kennedy JP, Daniels RN, Miller NR, Kim K, Breininger ML, Gentry PR, Brogan JT, Jones CK, Conn PJ, Lindsley CW. Bridges TM, et al. Among authors: gentry pr. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5439-42. doi: 10.1016/j.bmcl.2008.09.023. Epub 2008 Sep 10. Bioorg Med Chem Lett. 2008. PMID: 18805692 Free PMC article.
Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS).
Engers DW, Gentry PR, Williams R, Bolinger JD, Weaver CD, Menon UN, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Engers DW, et al. Among authors: gentry pr. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5175-8. doi: 10.1016/j.bmcl.2010.07.007. Epub 2010 Jul 8. Bioorg Med Chem Lett. 2010. PMID: 20667732 Free PMC article.
Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM.
Bridges TM, Kennedy JP, Cho HP, Breininger ML, Gentry PR, Hopkins CR, Conn PJ, Lindsley CW. Bridges TM, et al. Among authors: gentry pr. Bioorg Med Chem Lett. 2010 Jan 15;20(2):558-62. doi: 10.1016/j.bmcl.2009.11.089. Epub 2009 Nov 22. Bioorg Med Chem Lett. 2010. PMID: 20004578 Free PMC article.
Drugs for allosteric sites on receptors.
Wenthur CJ, Gentry PR, Mathews TP, Lindsley CW. Wenthur CJ, et al. Among authors: gentry pr. Annu Rev Pharmacol Toxicol. 2014;54:165-84. doi: 10.1146/annurev-pharmtox-010611-134525. Epub 2013 Oct 2. Annu Rev Pharmacol Toxicol. 2014. PMID: 24111540 Free PMC article. Review.
Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy.
Gogliotti RD, Engers DW, Garcia-Barrantes PM, Panarese JD, Gentry PR, Blobaum AL, Morrison RD, Daniels JS, Thompson AD, Jones CK, Conn PJ, Niswender CM, Lindsley CW, Hopkins CR. Gogliotti RD, et al. Among authors: gentry pr. Bioorg Med Chem Lett. 2016 Jun 15;26(12):2915-2919. doi: 10.1016/j.bmcl.2016.04.041. Epub 2016 Apr 19. Bioorg Med Chem Lett. 2016. PMID: 27131990 Free PMC article.
Identification of a Novel Allosteric Site at the M5 Muscarinic Acetylcholine Receptor.
Burger WAC, Gentry PR, Berizzi AE, Vuckovic Z, van der Westhuizen ET, Thompson G, Yeasmin M, Lindsley CW, Sexton PM, Langmead CJ, Tobin AB, Christopoulos A, Valant C, Thal DM. Burger WAC, et al. Among authors: gentry pr. ACS Chem Neurosci. 2021 Aug 18;12(16):3112-3123. doi: 10.1021/acschemneuro.1c00383. Epub 2021 Aug 5. ACS Chem Neurosci. 2021. PMID: 34351123
92 results