학술논문
Rapid Identification of Subtype-Selective Agonists of the Somatostatin Receptor Through Combinatorial Chemistry
Document Type
Academic Journal
Author
Rohrer, Susan P.; Birzin, Elizabeth T.; Mosley, Ralph T.; Berk, Scott C.; Hutchins, Steven M.; Shen, Dong-Ming; Xiong, Yusheng; Hayes, Edward C.; Parmar, Rupa M.; Foor, Forrest; Mitra, Sudha W.; Degrado, Sylvia J.; Shu, Min; Klopp, John M.; Cai, Sheng-Jian; Blake, Allan; Chan, Wanda W. S.; Pasternak, Alex; Yang, Lihu; Patchett, Arthur A.; Smith, Roy G.; Chapman, Kevin T.; Schaeffer, James M.
Source
Science. Oct 23, 1998 282(5389):737-740
Subject
Language
English
ISSN
0036-8075
Abstract
Nonpeptide agonists of each of the five somatostatin receptors were identified in combinatorial libraries constructed on the basis of molecular modeling of known peptide agonists.In vitro experiments using these selective compounds demonstrated the role of the somatostatin subtype-2 receptor in inhibition of glucagon release from mouse pancreatic alpha cells and the somatostatin subtype-5 receptor as a mediator of insulin secretion from pancreatic beta cells. Both receptors regulated growth hormone release from the rat anterior pituitary gland. The availability of high-affinity, subtype-selective agonists for each of the somatostatin receptors provides a direct approach to defining their physiological functions.