Single mutations at Asn295 and Leu305 in the cytoplasmic half of transmembrane alpha-helix domain 7 of the AT1 receptor induce promiscuous agonist specificity for angiotensin II fragments: a pseudo-constitutive activity.

Abstract excerpt

The most striking feature of a G protein-coupled receptor (GPCR) is its highly exclusive agonist specificity. This feature guarantees that a GPCR recognizes only its specific native agonist(s). In this study, we showed that two point mutations of N295S and L305Q enabled the AT(1) receptors to recognize multiple Ang II fragments. Similar to the well established constitutively active AT(1) mutant receptor N111G,...

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