Article
Rational design of vitamin D3 analogues which selectively restore activity to a vitamin D receptor mutant associated with rickets.
Organic letters - 31 Oct 2002
Swann Steve L, Bergh Joel J, Farach-Carson M Cindy, Koh John T
Abstract excerpt
[formula: see text] Vitamin D3-resistant rickets (VDRR) is associated with mutations to the Vitamin D receptor (VDR) which effect ligand-dependent transactivation. Some VDRR associated mutants directly disrupt ligand binding. Using the reported VDR-1,25-dihydroxy vitamin D3 (1,25(OH)2D3) cocrystal structure, three 1,25(OH)2D3 analogues were designed to uniquely complement the rickets associated mutant...
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