9EZ1

Vitamin D receptor in complex with 1,4a,25-trihydroxyvitamin D3

これはPDB形式変換不可エントリーです。

9EZ1 の概要

• エントリーDOI: 10.2210/pdb9ez1/pdb
• 分子名称: Vitamin D3 receptor A, Nuclear receptor coactivator 2, 1,4a,25-trihydroxyvitamin D3, ... (5 entities in total)
• 機能のキーワード: agonist, vitamin d metabolites, vdr, transcription
• 由来する生物種: Danio rerio (zebrafish); 詳細
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 36130.20

構造登録者

Rochel, N. (登録日: 2024-04-10, 公開日: 2024-06-19)

主引用文献

Peluso-Iltis, C.,Pierrat, N.,Rovito, D.,Osz, J.,Sawada, D.,Kittaka, A.,Laverny, G.,Rochel, N.
4-Hydroxy-1 alpha ,25-Dihydroxyvitamin D 3 : Synthesis and Structure-Function Study.
Biomolecules, 14:-, 2024

PubMed Abstract: The active vitamin D metabolites, 25-hydroxyvitamin D (25D) and 1,25-dihydroxyvitamin D (1,25D), are produced by successive hydroxylation steps and play key roles in several cellular processes. However, alternative metabolic pathways exist, and among them, the 4-hydroxylation of 25D is a major one. This study aims to investigate the structure-activity relationships of 4-hydroxy derivatives of 1,25D. Structural analysis indicates that 1,4α,25(OH)D and 1,4β,25(OH)D maintain the anchoring hydrogen bonds of 1,25D and form additional interactions, stabilizing the active conformation of VDR. In addition, 1,4α,25D and 1,4β,25D are as potent as 1,25D in regulating the expression of VDR target genes in rat intestinal epithelial cells and in the mouse kidney. Moreover, these two 4-hydroxy derivatives promote hypercalcemia in mice at a dose similar to that of the parent compound.

PubMed: 38785958
DOI: 10.3390/biom14050551

実験手法

X-RAY DIFFRACTION (1.95 Å)