STRUCTURAL BASIS FOR THE DIFFERENTIAL RXR AND RAR ACTIVITY OF STILBENE RETINOID ANALOGS

被引：35
作者：
BEARD, RL
GIL, DW
MARLER, DK
HENRY, E
COLON, DF
GILLETT, SJ
AREFIEG, T
BREEN, TS
KRAUSS, H
DAVIES, PJA
CHANDRARATNA, RAS
机构：
[1] ALLERGAN PHARMACEUT INC,DEPT CHEM,RETINOID RES,IRVINE,CA 92715
[2] ALLERGAN PHARMACEUT INC,DEPT BIOL,IRVINE,CA 92715
[3] UNIV TEXAS,SCH MED,DEPT PHARMACOL,HOUSTON,TX 77225
[4] UNIV TEXAS,SCH MED,DEPT MED,HOUSTON,TX 77225
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 12期
关键词：
D O I：
10.1016/S0960-894X(01)80511-4
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Retinoids elicit their biological actions by activating nuclear receptors that regulate gene transcription. There are six known retinoid receptors which belong to the retinoic acid receptor (RAR) and retinoid X receptor (RXR) families. We report RXR-active stilbene retinoid analogs and discuss the structural features that impart RAR and RXR activation properties to compounds of this class.
引用
收藏
页码：1447 / 1452
页数：6
相关论文
共 44 条
[1]  
AGNISH ND, 1992, RETINOIDS CLIN PRACT, P47
[2]   A NEW RETINOIC ACID RECEPTOR IDENTIFIED FROM A HEPATOCELLULAR-CARCINOMA [J].
BENBROOK, D ;
LERNHARDT, E ;
PFAHL, M .
NATURE, 1988, 333 (6174) :669-672
[3]   SYNTHESIS OF HIGH SPECIFIC ACTIVITY [H-3] 9-CIS-RETINOIC ACID AND ITS APPLICATION FOR IDENTIFYING RETINOIDS WITH UNUSUAL BINDING-PROPERTIES [J].
BOEHM, MF ;
MCCLURG, MR ;
PATHIRANA, C ;
MANGELSDORF, D ;
WHITE, SK ;
HEBERT, J ;
WINN, D ;
GOLDMAN, ME ;
HEYMAN, RA .
JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (03) :408-414
[4]   IDENTIFICATION OF A 2ND HUMAN RETINOIC ACID RECEPTOR [J].
BRAND, N ;
PETKOVICH, M ;
KRUST, A ;
CHAMBON, P ;
DETHE, H ;
MARCHIO, A ;
TIOLLAIS, P ;
DEJEAN, A .
NATURE, 1988, 332 (6167) :850-853
[5]   DEVELOPMENTAL BIOLOGY - READING THE RETINOID SIGNALS [J].
BROCKES, J .
NATURE, 1990, 345 (6278) :766-768
[6]   RXR-ALPHA, A PROMISCUOUS PARTNER OF RETINOIC ACID AND THYROID-HORMONE RECEPTORS [J].
BUGGE, TH ;
POHL, J ;
LONNOY, O ;
STUNNENBERG, HG .
EMBO JOURNAL, 1992, 11 (04) :1409-1418
[7]  
DAVIES PA, UNPUB
[8]  
Dawson M. I., 1990, CHEM BIOL SYNTHETIC, DOI [10.1201/9781351070638, DOI 10.1201/9781351070638]
[9]   THE STEROID AND THYROID-HORMONE RECEPTOR SUPERFAMILY [J].
EVANS, RM .
SCIENCE, 1988, 240 (4854) :889-895
[10]   INHIBITION OF HUMAN NON-PANCREATIC PHOSPHOLIPASES-A2 BY RETINOIDS AND FLAVONOIDS - MECHANISM OF ACTION [J].
FAWZY, AA ;
VISHWANATH, BS ;
FRANSON, RC .
AGENTS AND ACTIONS, 1988, 25 (3-4) :394-400
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