Nonpeptidic SH2 inhibitors of the tyrosine kinase ZAP-70

被引:20
|
作者
Vu, CB [1 ]
Corpuz, EG [1 ]
Pradeepan, SG [1 ]
Violette, S [1 ]
Bartlett, C [1 ]
Sawyer, TK [1 ]
机构
[1] ARIAD Pharmaceut Inc, Cambridge, MA 02139 USA
关键词
D O I
10.1016/S0960-894X(99)00524-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of a series of 1,2,4-oxadiazole analogs is discussed along with their ZAP-70 SH2 inhibitory activity. The tyrosine moiety in the original series has been replaced with nonpeptidic functional groups without a substantial loss of binding affinity. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:3009 / 3014
页数:6
相关论文
共 50 条
  • [1] Discovery of potent and selective SH2 inhibitors of the tyrosine kinase ZAP-70
    Vu, CB
    Corpuz, EG
    Merry, TJ
    Pradeepan, SG
    Bartlett, C
    Bohacek, RS
    Botfield, MC
    Eyermann, CJ
    Lynch, BA
    MacNeil, IA
    Ram, MK
    van Schravendijk, MR
    Violette, S
    Sawyer, TK
    JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (20) : 4088 - 4098
  • [2] INTERACTION OF HUMAN P56LCK SH2 DOMAIN WITH THE ZAP-70 TYROSINE KINASE
    ACUTO, O
    DUPLAY, P
    THOME, M
    HERVE, F
    JOURNAL OF CELLULAR BIOCHEMISTRY, 1994, : 394 - 394
  • [3] LOCALIZATION OF ZAP-70 TO THE TCR IS MEDIATED BY BINDING OF TYROSINE-PHOSPHORYLATED TAMS TO THE TANDEM SH2 DOMAINS OF ZAP-70
    WANGE, RL
    ISAKOV, N
    WATTS, JD
    AEBERSOLD, R
    SAMELSON, LE
    FASEB JOURNAL, 1994, 8 (07): : A1228 - A1228
  • [4] THE PROTEIN-TYROSINE KINASE ZAP-70 CAN ASSOCIATE WITH THE SH2 DOMAIN OF PROTO-VAV
    KATZAV, S
    SUTHERLAND, M
    PACKHAM, G
    YI, TL
    WEISS, A
    JOURNAL OF BIOLOGICAL CHEMISTRY, 1994, 269 (51) : 32579 - 32585
  • [5] ZAP-70 protein tyrosine kinase is constitutively targeted to the T cell cortex independently of its SH2 domains
    Huby, RDJ
    Iwashima, M
    Weiss, A
    Ley, SC
    JOURNAL OF CELL BIOLOGY, 1997, 137 (07): : 1639 - 1649
  • [6] Recent advances in the design and synthesis of SH2 inhibitors of Src Grb2 and ZAP-70
    Vu, CB
    CURRENT MEDICINAL CHEMISTRY, 2000, 7 (10) : 1081 - 1100
  • [7] Structural basis for the inhibition of tyrosine kinase activity of ZAP-70
    Deindl, Sebastian
    Kadlecek, Theresa A.
    Brdicka, Tomas
    Cao, Xiaoxian
    Weiss, Arthur
    Kuriyan, John
    CELL, 2007, 129 (04) : 735 - 746
  • [8] Antagonists of the Src homology 2 (SH2) domains of Grb2, Src, Lck and ZAP-70
    García-Echeverría, C
    CURRENT MEDICINAL CHEMISTRY, 2001, 8 (13) : 1589 - 1604
  • [9] ZAP-70 BINDING-SPECIFICITY TO T-CELL RECEPTOR TYROSINE-BASED ACTIVATION MOTIFS - THE TANDEM SH2 DOMAINS OF ZAP-70 BIND DISTINCT TYROSINE-BASED ACTIVATION MOTIFS WITH VARYING AFFINITY
    ISAKOV, N
    WANGE, RL
    BURGESS, WH
    WATTS, JD
    AEBERSOLD, R
    SAMELSON, LE
    JOURNAL OF EXPERIMENTAL MEDICINE, 1995, 181 (01): : 375 - 380
  • [10] Structural Basis for Activation of ZAP-70 by Phosphorylation of the SH2-Kinase Linker
    Yan, Qingrong
    Barros, Tiago
    Visperas, Patrick R.
    Deindl, Sebastian
    Kadlecek, Theresa A.
    Weiss, Arthur
    Kuriyan, John
    MOLECULAR AND CELLULAR BIOLOGY, 2013, 33 (11) : 2188 - 2201