Somatostatin receptors.
Somatostatin induces its biological actions by activating a family of receptor subtypes. The recent cloning of five somatostatin receptor subtypes has led to the development of subtype-selective agonists. These compounds are revealing distinct functions of the individual receptor subtypes. Mutagenesis studies have revealed domains of several of the receptors involved in specific recognition of somatostatin analogues. Molecular modeling of both of these ligand-binding domains and the constrained somatostatin analogues that they interact with may lead to the development of nonpeptide somatostatin drugs that could be useful in the treatment of tumors and various metabolic, gastrointestinal, and central nervous system disorders.
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Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104.
D000818:Animals; D003001:Cloning, Molecular; D019204:GTP-Binding Proteins / Q000378:metabolism; D006801:Humans; D008024:Ligands; D017481:Receptors, Somatostatin / Q000235:genetics / Q000502:physiology*; D013329:Structure-Activity Relationship
D008024:Ligands; D017481:Receptors, Somatostatin; D019204:GTP-Binding Proteins