ON THE SIDE-CHAIN CONFORMATION OF 1-ALPHA,25-DIHYDROXYVITAMIN D-3 RESPONSIBLE FOR BINDING TO THE RECEPTOR

被引：22

作者：

YAMAMOTO, K

OHTA, M

DELUCA, HF

YAMADA, S

机构：

[1] TOKYO MED & DENT UNIV,INST MED & DENT ENGN,CHIYODA KU,TOKYO 101,JAPAN

[2] CHIGAI PHARMACEUT CO LTD,FUJI GOTEMBA RES LABS,GOTEMBA,SHIZUOKA 412,JAPAN

[3] UNIV WISCONSIN,DEPT BIOCHEM,MADISON,WI 53706

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 09期

关键词：

D O I：

10.1016/0960-894X(95)00142-G

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Side chain mobility of 1,25(OH)(2)D-3 (1) and its 20-epimer (2) was analyzed and shown in a three-dimensional dot map that indicates the two distinct spatial regions accessible by the terminal 25-hydroxyl group for each vitamin. The biological activities of two analogs (3 and 4) of 1, which possess restricted side chain flexibility, were tested and the results suggest the spatial region of 1 responsible for binding to VDR and DBP.

引用

页码：979 / 984

页数：6

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