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New insights into the function of M4 muscarinic acetylcholine receptors gained using a novel allosteric modulator and a DREADD (designer receptor exclusively activated by a designer drug).
Nawaratne V, Leach K, Suratman N, Loiacono RE, Felder CC, Armbruster BN, Roth BL, Sexton PM, Christopoulos A. Nawaratne V, et al. Among authors: felder cc. Mol Pharmacol. 2008 Oct;74(4):1119-31. doi: 10.1124/mol.108.049353. Epub 2008 Jul 15. Mol Pharmacol. 2008. PMID: 18628403
Crystal structures of the M1 and M4 muscarinic acetylcholine receptors.
Thal DM, Sun B, Feng D, Nawaratne V, Leach K, Felder CC, Bures MG, Evans DA, Weis WI, Bachhawat P, Kobilka TS, Sexton PM, Kobilka BK, Christopoulos A. Thal DM, et al. Among authors: felder cc. Nature. 2016 Mar 17;531(7594):335-40. doi: 10.1038/nature17188. Epub 2016 Mar 9. Nature. 2016. PMID: 26958838 Free PMC article.
Bitopic Binding Mode of an M1 Muscarinic Acetylcholine Receptor Agonist Associated with Adverse Clinical Trial Outcomes.
Bradley SJ, Molloy C, Bundgaard C, Mogg AJ, Thompson KJ, Dwomoh L, Sanger HE, Crabtree MD, Brooke SM, Sexton PM, Felder CC, Christopoulos A, Broad LM, Tobin AB, Langmead CJ. Bradley SJ, et al. Among authors: felder cc. Mol Pharmacol. 2018 Jun;93(6):645-656. doi: 10.1124/mol.118.111872. Epub 2018 Apr 25. Mol Pharmacol. 2018. PMID: 29695609 Free PMC article.
Cryptic pocket formation underlies allosteric modulator selectivity at muscarinic GPCRs.
Hollingsworth SA, Kelly B, Valant C, Michaelis JA, Mastromihalis O, Thompson G, Venkatakrishnan AJ, Hertig S, Scammells PJ, Sexton PM, Felder CC, Christopoulos A, Dror RO. Hollingsworth SA, et al. Among authors: felder cc. Nat Commun. 2019 Jul 23;10(1):3289. doi: 10.1038/s41467-019-11062-7. Nat Commun. 2019. PMID: 31337749 Free PMC article.
148 results