Design of Potent, Orally Effective, Nonpeptidal Antagonists of the Peptide Hormone Cholecystokinin

Overview

Journal Proc Natl Acad Sci U S A

Specialty Science

Date 1986 Jul 1

PMID 3014519

Citations 39

Authors

B E Evans

M G Bock

K E Rittle

R M DiPardo

W L Whitter

D F Veber

P S Anderson

R M Freidinger

Affiliations

Soon will be listed here.

Abstract

We describe the design and synthesis of nonpeptidal antagonists of the peptide hormone cholecystokinin. Several of these compounds have high specificity and nanomolar binding affinity and are active after oral administration. To our knowledge, the design of such agents has not previously been accomplished for any peptide hormone. The structural similarities between these synthetic compounds and the anxiolytic 1,4-benzodiazepines are noted, and the potential of this structural feature for future design of ligands for other peptide hormone receptors is discussed.

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