Article
CCK-B/Gastrin receptor transmembrane domain mutations selectively alter synthetic agonist efficacy without affecting the activity of endogenous peptides.
Molecular pharmacology - 1 Aug 2000
Bläker M, Ren Y, Seshadri L, McBride E W, Beinborn M, Kopin A S
Abstract excerpt
Recent efforts have focused on identifying small nonpeptide molecules that can mimic the activity of endogenous peptide hormones. Understanding the molecular basis of ligand-induced receptor activation by these divergent classes of ligands should expedite the process of drug development. Using the cholecystokinin-B/gastrin receptor (CCK-BR) as a model system, we have recently shown that both affinity and efficacy...
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