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
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
    BENBROOK, D
    LERNHARDT, E
    PFAHL, M
    [J]. 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
    BOEHM, MF
    MCCLURG, MR
    PATHIRANA, C
    MANGELSDORF, D
    WHITE, SK
    HEBERT, J
    WINN, D
    GOLDMAN, ME
    HEYMAN, RA
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (03) : 408 - 414
  • [4] IDENTIFICATION OF A 2ND HUMAN RETINOIC ACID RECEPTOR
    BRAND, N
    PETKOVICH, M
    KRUST, A
    CHAMBON, P
    DETHE, H
    MARCHIO, A
    TIOLLAIS, P
    DEJEAN, A
    [J]. NATURE, 1988, 332 (6167) : 850 - 853
  • [5] DEVELOPMENTAL BIOLOGY - READING THE RETINOID SIGNALS
    BROCKES, J
    [J]. NATURE, 1990, 345 (6278) : 766 - 768
  • [6] RXR-ALPHA, A PROMISCUOUS PARTNER OF RETINOIC ACID AND THYROID-HORMONE RECEPTORS
    BUGGE, TH
    POHL, J
    LONNOY, O
    STUNNENBERG, HG
    [J]. 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
    EVANS, RM
    [J]. SCIENCE, 1988, 240 (4854) : 889 - 895
  • [10] INHIBITION OF HUMAN NON-PANCREATIC PHOSPHOLIPASES-A2 BY RETINOIDS AND FLAVONOIDS - MECHANISM OF ACTION
    FAWZY, AA
    VISHWANATH, BS
    FRANSON, RC
    [J]. AGENTS AND ACTIONS, 1988, 25 (3-4): : 394 - 400