3-anilino-4-arylmaleimides: Potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3)

被引:156
作者
Smith, DG [1 ]
Buffet, M [1 ]
Fenwick, AE [1 ]
Haigh, D [1 ]
Ife, RJ [1 ]
Saunders, M [1 ]
Slingsby, BP [1 ]
Stacey, R [1 ]
Ward, RW [1 ]
机构
[1] SmithKline Beecham Pharmaceut, Harlow CM19 5AW, Essex, England
关键词
D O I
10.1016/S0960-894X(00)00721-6
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Potent 3-anilino-4-arylmaleimide glycogen synthase kinase-3 (GSK-3) inhibitors have been prepared using automated array methodology. A number of these are highly selective, having little inhibitory potency against more than 20 other protein kinases. (C) 2001 Elsevier Science Ltd. All rights reserved.
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收藏
页码:635 / 639
页数:5
相关论文
共 36 条
[1]   The protein kinase C inhibitors Ro 318220 and GF 109203X are equally potent inhibitors of MAPKAP kinase-1 beta (Rsk-2) and p70 S6 kinase [J].
Alessi, DR .
FEBS LETTERS, 1997, 402 (2-3) :121-123
[2]   INSULIN RESISTANCE IN SKELETAL-MUSCLES IN PATIENTS WITH NIDDM [J].
BECKNIELSEN, H ;
VAAG, A ;
DAMSBO, P ;
HANDBERG, A ;
NIELSEN, OH ;
HENRIKSEN, JE ;
THYERONN, P .
DIABETES CARE, 1992, 15 (03) :418-429
[3]   CORRELATION BETWEEN MUSCLE GLYCOGEN-SYNTHASE ACTIVITY AND INVIVO INSULIN ACTION IN MAN [J].
BOGARDUS, C ;
LILLIOJA, S ;
STONE, K ;
MOTT, D .
JOURNAL OF CLINICAL INVESTIGATION, 1984, 73 (04) :1185-1190
[4]  
BOSCH F, 1986, J BIOL CHEM, V261, P6927
[5]   The mood-stabilizing agent valproate inhibits the activity of glycogen synthase kinase-3 [J].
Chen, G ;
Huang, LD ;
Jiang, YM ;
Manji, HK .
JOURNAL OF NEUROCHEMISTRY, 1999, 72 (03) :1327-1330
[6]   Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription [J].
Coghlan, MP ;
Culbert, AA ;
Cross, DAE ;
Corcoran, SL ;
Yates, JW ;
Pearce, NJ ;
Rausch, OL ;
Murphy, GJ ;
Carter, PS ;
Cox, LR ;
Mills, D ;
Brown, MJ ;
Haigh, D ;
Ward, RW ;
Smith, DG ;
Murray, KJ ;
Reith, AD ;
Holder, JC .
CHEMISTRY & BIOLOGY, 2000, 7 (10) :793-803
[7]   SEPARATION AND CHARACTERIZATION OF GLYCOGEN-SYNTHASE KINASE-3, GLYCOGEN-SYNTHASE KINASE-4 AND GLYCOGEN-SYNTHASE KINASE-5 FROM RABBIT SKELETAL-MUSCLE [J].
COHEN, P ;
YELLOWLEES, D ;
AITKEN, A ;
DONELLADEANA, A ;
HEMMINGS, BA ;
PARKER, PJ .
EUROPEAN JOURNAL OF BIOCHEMISTRY, 1982, 124 (01) :21-35
[8]  
CROSS DAE, 2001, IN PRESS
[9]   LITHIUM INDUCES APOPTOSIS IN IMMATURE CEREBELLAR GRANULE CELLS BUT PROMOTES SURVIVAL OF MATURE NEURONS [J].
D'MELLO, SR ;
ANELLI, R ;
CALISSANO, P .
EXPERIMENTAL CELL RESEARCH, 1994, 211 (02) :332-338
[10]   Specificity and mechanism of action of some commonly used protein kinase inhibitors [J].
Davies, SP ;
Reddy, H ;
Caivano, M ;
Cohen, P .
BIOCHEMICAL JOURNAL, 2000, 351 (351) :95-105