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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

A Molecular Guidance System Based Upon Target Genes, Nuclear Receptors and Ligands Applied to Drug Discovery and Prediction of Toxicity

Author(s): Virendra B. Mahesh, Neil Sidell, Douglas E. Ewing, Edwin D. Bransome Jr. and Lawrence B. Hendry

Volume 8 , Issue 12 , 2008

Page: [1252 - 1264] Pages: 13

DOI: 10.2174/138955708786140972

Price: $65


A molecular guidance system useful in drug design is described in which nuclear receptors position ligands in intercalation sites in responsive genes. Evidence is based upon positions of agonists in receptors and the transcriptional activity of a designed estrogen that is 3 times more potent than the steroid hormone estradiol.

Keywords: Nuclear receptors, intercalators, DNA unwinding, steroid hormones, hormone response elements, computer modeling, transcription, drug design

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