Abstract:
:Site-directed mutagenesis has been used to evaluate the roles of the key aspartate and arginine residues in transmembrane domain three of the muscarinic receptors. The results suggest that the formation of an ionic bond between the Asp carboxylate group and the onium headgroup is essential to anchor acetylcholine in its active, bound conformation in both binary agonist-receptor and ternary agonist-receptor-G-protein complexes, but that secondary, non-productive binding modes, promoted by non-polar forces, may contribute to binary complex formation by other ligands. The positive charge of the arginyl side-chain is central to the recognition, and subsequent activation of G-proteins by the agonist-M1 mAChR complex.
journal_name
Life Scijournal_title
Life sciencesauthors
Hulme EC,Curtis CA,Page KM,Jones PGdoi
10.1016/0024-3205(95)00025-2subject
Has Abstractpub_date
1995-01-01 00:00:00pages
891-8issue
11-12eissn
0024-3205issn
1879-0631pii
0024-3205(95)00025-2journal_volume
56pub_type
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