Article
Roof and floor of the muscarinic binding pocket: variations in the binding modes of orthosteric ligands.
Molecular pharmacology - 1 Dec 2007
Goodwin J Alex, Hulme Edward C, Langmead Christopher J, Tehan Ben G
Abstract excerpt
Alanine substitution mutagenesis has been used to investigate residues that make up the roof and floor of the muscarinic binding pocket and regulate ligand access. We mutated the amino acids in the second extracellular loop of the M1 muscarinic acetylcholine receptor that are homologous to the cis-retinal contact residues in rhodopsin, the disulfide-bonded Cys178 and Cys98 that anchor the loop to transmembrane...
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