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...

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Bibliographic Details
Published inThe Journal of biological chemistry Vol. 269; no. 40; pp. 24621 - 24626
Main Authors Fitzpatrick, V D, Vandlen, R L
Format Journal Article
LanguageEnglish
Published United States American Society for Biochemistry and Molecular Biology 07.10.1994
Subjects
Amino Acid Sequence
Animals
Base Sequence
Guanosine Triphosphate - pharmacology
Mice
Molecular Sequence Data
Peptides, Cyclic - metabolism
Receptors, Somatostatin - analysis
Receptors, Somatostatin - chemistry
Somatostatin - agonists
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Summary: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.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
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ISSN:0021-9258
1083-351X
DOI:10.1016/S0021-9258(17)31437-0