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

Ben E. Evans, Mark G. Bock, Kenneth E. Rittle, Robert M. DiPardo, Willie L. Whitter, Daniel F. Veber, Paul S. Anderson and Roger M. Freidinger
Proceedings of the National Academy of Sciences of the United States of America
Vol. 83, No. 13 (Jul. 1, 1986), pp. 4918-4922
Stable URL: http://www.jstor.org/stable/27621
Page Count: 5
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Since scans are not currently available to screen readers, please contact JSTOR User Support for access. We'll provide a PDF copy for your screen reader.
Design of Potent, Orally Effective, Nonpeptidal Antagonists of the Peptide Hormone Cholecystokinin
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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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