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., Lawrence B. Hendry.

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 8 , Issue 12 , 2008

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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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Article Details

Year: 2008
Page: [1252 - 1264]
Pages: 13
DOI: 10.2174/138955708786140972
Price: $58

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