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Application of conformationally restricted peptidomimetics to modeling the bound conformation of peptide antagonists with the IL-1 receptor |
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| Authors: | Gary A. Flynn Ann L. Akeson Ram Dharanipragada Michael J. Genin J. Antony Malikayil Richard Pottorf Jeffery S. Sabol Herman Schreuder Ron Tomlinson Phil Waid Ron Barrett Jeff Jacobs Steve Yanofsky |
| Affiliation: | (1) Selectide Corporation, 1580 East Hanley Boulevard, Tucson, AZ, 85737, U.S.A.;(2) Hoechst Marion Roussel Inc., 2110 E. Galgraith Road, Cincinnati, OH, 45215, U.S.A.;(3) Affymax Research Institute, 4001 Miranda Drive, Palo Alto, CA, 94302, U.S.A. |
| Abstract: | A collection of complementary peptide caricatures that closely mimic low-energy (presumably highly populated) conformations of amino acids of interest would constitute a valuable tool set to study the interactions of small peptide ligands with their biological targets. Our general strategy for the design, synthesis and application of peptidomimetics is presented. An illustration of how structural information from mimetics combined with cutting edge biophysical data can be used to derive a model for the bound conformation of an 11-mer peptide antagonist with the IL-1 receptor is given. |
| Keywords: | complementary constrained low-energy molecular modeling scaffold |
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