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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
Published by: National Academy of Sciences
Stable URL: http://www.jstor.org/stable/27621
Page Count: 5
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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.
Proceedings of the National Academy of Sciences of the United States of America © 1986 National Academy of Sciences