Crystal structure of the vitamin D nuclear receptor ligand binding domain in complex with a locked side chain analog of calcitriol. - Archive ouverte HAL Access content directly
Journal Articles Archives of Biochemistry and Biophysics Year : 2007

Crystal structure of the vitamin D nuclear receptor ligand binding domain in complex with a locked side chain analog of calcitriol.

Abstract

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.

Dates and versions

hal-00189973 , version 1 (22-11-2007)

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Cite

Natacha Rochel, Shinji Hourai, Xenxo Pérez-García, Antonio Rumbo, Antonio Mourino, et al.. Crystal structure of the vitamin D nuclear receptor ligand binding domain in complex with a locked side chain analog of calcitriol.. Archives of Biochemistry and Biophysics, 2007, 460 (2), pp.172-6. ⟨10.1016/j.abb.2007.01.031⟩. ⟨hal-00189973⟩
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