Allele-specific activation of genetically engineered receptors.

摘要: The binding of agonists and antagonists to the beta-adrenergic receptor (beta AR) is postulated involve an ionic interaction between amine group ligand carboxylate side chain Asp113 in third hydrophobic domain receptor. To explore importance this ligands beta AR, a Ser residue was substituted for Asp113, ability mutant respond compounds which could potentially interact with hydroxyl assessed. fully activated by catechol-containing esters ketones, did not activate wild-type AR. demonstration that molecular substitution single amino acid can alter specificity AR provides evidence chemical nature critical determinant recognition site Further, modify replacement acids at demonstrates potential rational design drugs function specifically genetically engineered receptors.