This basic science study demonstrates that non-conserved residues across species are more critical for subtype-selective ligand recognition than for dual receptor ligands on AT receptors.
Warrants caution extrapolating amphibian-mammalian AT receptor data; leaves open non-conserved residues as targets for subtype-selective ligand design.
Site-directed interspecies amino acid exchange was used to compare the binding determinants of a novel dual endothelial-angiotensin receptor ligand, L-746,072, with type-1 angiotensin receptor (AT1) selective antagonists on AT receptors expressed in COS cells. These studies suggest that residues on AT receptors which are non-conserved between amphibian and mammalian species play a greater role in subtype selective ligand recognition than for dual receptor ligands. These data also support the hypothesis that a common non-peptide binding site exists within transmembrane domains on peptidergic receptors.
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Dascal et al. (1998) studied this question.
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