期刊
ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS
卷 460, 期 2, 页码 172-176出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.abb.2007.01.031
关键词
vitamin D nuclear receptor; 1 alpha,25(OH)(2)D-3; 21-nor-calcitriol-20(22),23-diyne; crystal structure
The crystal structures of vitamin D nuclear receptor (VDR) have revealed that all compounds are anchored by the same residues to the ligand binding pocket (LBP). Based on this observation, a synthetic analog with a locked side chain (21-nor-calcitriol-20(22),23-diyne) has been synthesized in order to gain in entropy energy with a predefined active side chain conformation. The crystal structure of VDR LBD bound to this locked side chain analogue while confirming the docking provides a structural basis for the activity of this compound. (c) 2007 Elsevier Inc. All rights reserved.
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