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Discovery of structurally distinct tricyclic M4 positive allosteric modulator (PAM) chemotypes - Part 2.
Long MF, Capstick RA, Spearing PK, Engers JL, Gregro AR, Bollinger SR, Chang S, Luscombe VB, Rodriguez AL, Cho HP, Niswender CM, Bridges TM, Conn PJ, Lindsley CW, Engers DW, Temple KJ. Long MF, et al. Among authors: engers jl. Bioorg Med Chem Lett. 2021 Dec 1;53:128416. doi: 10.1016/j.bmcl.2021.128416. Epub 2021 Oct 26. Bioorg Med Chem Lett. 2021. PMID: 34710625 Free PMC article.
Discovery of the First Selective M4 Muscarinic Acetylcholine Receptor Antagonists with in Vivo Antiparkinsonian and Antidystonic Efficacy.
Moehle MS, Bender AM, Dickerson JW, Foster DJ, Qi A, Cho HP, Donsante Y, Peng W, Bryant Z, Stillwell KJ, Bridges TM, Chang S, Watson KJ, O'Neill JC, Engers JL, Peng L, Rodriguez AL, Niswender CM, Lindsley CW, Hess EJ, Conn PJ, Rook JM. Moehle MS, et al. Among authors: engers jl. ACS Pharmacol Transl Sci. 2021 Aug 2;4(4):1306-1321. doi: 10.1021/acsptsci.0c00162. eCollection 2021 Aug 13. ACS Pharmacol Transl Sci. 2021. PMID: 34423268 Free PMC article.
Discovery of VU6028418: A Highly Selective and Orally Bioavailable M4 Muscarinic Acetylcholine Receptor Antagonist.
Spock M, Carter TR, Bollinger KA, Han C, Baker LA, Rodriguez AL, Peng L, Dickerson JW, Qi A, Rook JM, O'Neill JC, Watson KJ, Chang S, Bridges TM, Engers JL, Engers DW, Niswender CM, Conn PJ, Lindsley CW, Bender AM. Spock M, et al. Among authors: engers jl. ACS Med Chem Lett. 2021 Aug 2;12(8):1342-1349. doi: 10.1021/acsmedchemlett.1c00363. eCollection 2021 Aug 12. ACS Med Chem Lett. 2021. PMID: 34413964 Free PMC article.
Discovery of a novel 3,4-dimethylcinnoline carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping.
Temple KJ, Engers JL, Long MF, Gregro AR, Watson KJ, Chang S, Jenkins MT, Luscombe VB, Rodriguez AL, Niswender CM, Bridges TM, Conn PJ, Engers DW, Lindsley CW. Temple KJ, et al. Among authors: engers jl. Bioorg Med Chem Lett. 2019 Nov 1;29(21):126678. doi: 10.1016/j.bmcl.2019.126678. Epub 2019 Sep 10. Bioorg Med Chem Lett. 2019. PMID: 31537424
Discovery of VU2957 (Valiglurax): An mGlu4 Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease.
Panarese JD, Engers DW, Wu YJ, Bronson JJ, Macor JE, Chun A, Rodriguez AL, Felts AS, Engers JL, Loch MT, Emmitte KA, Castelhano AL, Kates MJ, Nader MA, Jones CK, Blobaum AL, Conn PJ, Niswender CM, Hopkins CR, Lindsley CW. Panarese JD, et al. Among authors: engers jl. ACS Med Chem Lett. 2018 Oct 16;10(3):255-260. doi: 10.1021/acsmedchemlett.8b00426. eCollection 2019 Mar 14. ACS Med Chem Lett. 2018. PMID: 30891122 Free PMC article.
35 results