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Science 31 August 1979:
Vol. 205. no. 4409, pp. 917 - 919
DOI: 10.1126/science.224455
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Articles

Science, Vol 205, Issue 4409, 917-919
Copyright © 1979 by American Association for the Advancement of Science

articles

Digitalis genin activity: side-group carbonyl oxygen position is a major determinant

DS Fullerton, K Yoshioka, DC Rohrer, AH From, and K Ahmed

The Na+,k+-adenosine triphosphatase-inhibiting activity of digitalis genins and their analogs is a function of side-group carbonyl (C = O) oxygen position. For each 2.2 angstroms that this oxygen is displaced from its position in digitoxigenin, activity drops by one order of magnitude. This quantitative relation resolves previously proposed models which have attempted to describe the molecular basis of genin activity. A multidisciplinary (crystallographic, conformational energy, synthetic, biological) approach to structure-activity relations is described.


THIS ARTICLE HAS BEEN CITED BY OTHER ARTICLES:
Three-dimensional molecular modeling and drug design.
P Gund, J. Andose, J. Rhodes, and G. Smith (1980)
Science 208, 1425-1431
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