A molecular guidance system based upon target genes, nuclear receptors and ligands applied to drug discovery and prediction of toxicity.
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.
Institute of Molecular Medicine and Genetics, Medical College of Georgia, Augusta GA 30912, USA. vmahesh@mail.mcg.edu
Virendra B
VB
Mahesh
Neil
N
Sidell
Douglas E
DE
Ewing
Edwin D
ED
Bransome
Lawrence B
LB
Hendry
D002467:Cell Nucleus / Q000378:metabolism*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D004247:DNA / Q000737:chemistry; D055808:Drug Discovery; D004958:Estradiol / Q000737:chemistry; D006728:Hormones / Q000737:chemistry; D006801:Humans; D008024:Ligands; D008956:Models, Chemical; D008968:Molecular Conformation; D011487:Protein Conformation; D018160:Receptors, Cytoplasmic and Nuclear / Q000378:metabolism*; D020218:Response Elements; D012984:Software; D013256:Steroids / Q000737:chemistry
D006728:Hormones; D008024:Ligands; D018160:Receptors, Cytoplasmic and Nuclear; D013256:Steroids; D004958:Estradiol; D004247:DNA