6agonist selectivity determinants in somatostatin receptor subtypes I and II.
The biological activities of the peptide hormone somatostatin are mediated through a recently identified family of G-protein-linked receptors. A number of somatostatin analogs have been characterized with selective affinities for particular somatostatin receptor subtypes. Using one such molecule (MK-678), we have delineated receptor regions that determine analog selectivity in the murine Type 1 and Type 2 somatostatin receptors. We find that the regions about the second and third extracellular loops of these two receptors contain the determinants for MK-678 selectivity and affinity.
Fitzpatrick
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Department of Protein Chemistry, Genentech, Inc., South San Francisco, California 94080.
Vandlen
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D000595:Amino Acid Sequence; D000818:Animals; D001483:Base Sequence; D006160:Guanosine Triphosphate / Q000494:pharmacology; D051379:Mice; D008969:Molecular Sequence Data; D010456:Peptides, Cyclic / Q000378:metabolism; D017481:Receptors, Somatostatin / Q000032:analysis / Q000737:chemistry*; D013004:Somatostatin / Q000819:agonists*
D010456:Peptides, Cyclic; D017481:Receptors, Somatostatin; D013004:Somatostatin; C040968:seglitide; D006160:Guanosine Triphosphate