Article
Novel vitamin D receptor ligands having a carboxyl group as an anchor to arginine 274 in the ligand-binding domain.
The Journal of steroid biochemistry and molecular biology - 1 Jul 2010
Fujishima Toshie, Tsuji Genichiro, Tanaka Chika, Harayama Hiroshi
Abstract excerpt
Vitamin D3 is metabolized into the hormonally active form, 1alpha,25-dihydroxyvitamin D3 (1), via 25-hydroxyvitamin D3 (2) which is the most abundant circulating metabolite. Introduction of the 1alpha-hydroxyl group into 25-hydroxyvitamin D3 (2) to produce 1alpha,25-dihydroxyvitamin D3 (1) increases the VDR binding affinity by approximately 1000-fold. The X-ray crystal structure of human VDR in complex with...
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