Abstract
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
Mini-Reviews in Medicinal Chemistry
Title: A Molecular Guidance System Based Upon Target Genes, Nuclear Receptors and Ligands Applied to Drug Discovery and Prediction of Toxicity
Volume: 8 Issue: 12
Author(s): Virendra B. Mahesh, Neil Sidell, Douglas E. Ewing, Edwin D. Bransome Jr. and Lawrence B. Hendry
Affiliation:
Keywords: Nuclear receptors, intercalators, DNA unwinding, steroid hormones, hormone response elements, computer modeling, transcription, drug design
Abstract: 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.
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Cite this article as:
Mahesh B. Virendra, Sidell Neil, Ewing E. Douglas, Bransome Jr. D. Edwin and Hendry B. Lawrence, A Molecular Guidance System Based Upon Target Genes, Nuclear Receptors and Ligands Applied to Drug Discovery and Prediction of Toxicity, Mini-Reviews in Medicinal Chemistry 2008; 8 (12) . https://dx.doi.org/10.2174/138955708786140972
DOI https://dx.doi.org/10.2174/138955708786140972 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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