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Discovery of novel intracellular receptor modulating drugs
Authors:Todd K. Jones   Charles Pathirana   Mark E. Goldman   Lawrence G. Hamann   Luc J. Farmer   Teodoro Ianiro   Michael G. Johnson   Steven L. Bender   Dale E. Mais  Robert B. Stein
Affiliation:

Ligand Pharmaceuticals, Inc., 9393 Towne Centre Drive, San Diego, CA 92121, U.S.A.

Abstract:Utilizing the co-transfection assay as a guide to determining structure activity relationships, we have been pursuing the discovery of non-steroidal hPR modulators. Small molecule, non-steroidal lead structures have been identified. Optimization of these structures has yielded more potent hPR modulators. Improved cross-reactivity profiles with other intracellular receptors are a feature of these compounds owing to their non-steroidal nature.
Keywords:
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