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A novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptors.
Cho HP, Engers DW, Venable DF, Niswender CM, Lindsley CW, Conn PJ, Emmitte KA, Rodriguez AL. Cho HP, et al. Among authors: engers dw. ACS Chem Neurosci. 2014 Jul 16;5(7):597-610. doi: 10.1021/cn5000343. Epub 2014 May 15. ACS Chem Neurosci. 2014. PMID: 24798819 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. 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.
Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats.
Engers DW, Field JR, Le U, Zhou Y, Bolinger JD, Zamorano R, Blobaum AL, Jones CK, Jadhav S, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Engers DW, et al. J Med Chem. 2011 Feb 24;54(4):1106-10. doi: 10.1021/jm101271s. Epub 2011 Jan 19. J Med Chem. 2011. PMID: 21247167 Free PMC article.
Selective inhibition of the K(ir)2 family of inward rectifier potassium channels by a small molecule probe: the discovery, SAR, and pharmacological characterization of ML133.
Wang HR, Wu M, Yu H, Long S, Stevens A, Engers DW, Sackin H, Daniels JS, Dawson ES, Hopkins CR, Lindsley CW, Li M, McManus OB. Wang HR, et al. Among authors: engers dw. ACS Chem Biol. 2011 Aug 19;6(8):845-56. doi: 10.1021/cb200146a. Epub 2011 Jun 13. ACS Chem Biol. 2011. PMID: 21615117 Free PMC article.
Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)) with oral efficacy in an antiparkinsonian animal model.
Jones CK, Engers DW, Thompson AD, Field JR, Blobaum AL, Lindsley SR, Zhou Y, Gogliotti RD, Jadhav S, Zamorano R, Bogenpohl J, Smith Y, Morrison R, Daniels JS, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Jones CK, et al. Among authors: engers dw. J Med Chem. 2011 Nov 10;54(21):7639-47. doi: 10.1021/jm200956q. Epub 2011 Oct 19. J Med Chem. 2011. PMID: 21966889 Free PMC article.
The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease.
Jones CK, Bubser M, Thompson AD, Dickerson JW, Turle-Lorenzo N, Amalric M, Blobaum AL, Bridges TM, Morrison RD, Jadhav S, Engers DW, Italiano K, Bode J, Daniels JS, Lindsley CW, Hopkins CR, Conn PJ, Niswender CM. Jones CK, et al. Among authors: engers dw. J Pharmacol Exp Ther. 2012 Feb;340(2):404-21. doi: 10.1124/jpet.111.187443. Epub 2011 Nov 16. J Pharmacol Exp Ther. 2012. PMID: 22088953 Free PMC article.
78 results