ATP Non-Competitive Ser/Thr Kinase Inhibitors as Potential Anticancer Agents

被引：15

作者：

Cozza, Giorgio ^{[1
,2
]}

Bortolato, Andrea ^{[1
]}

Menta, Ernesto ^{[3
]}

Cavalletti, Ennio ^{[3
]}

Spinelli, Silvano ^{[3
]}

Moro, Stefano ^{[1
]}

机构：

[1] Univ Padua, Dipartimento Sci Farmaceut, MMS, I-35131 Padua, Italy

[2] Univ Padua, Dipartimento Chim Biol, I-35121 Padua, Italy

[3] Eth Oncol Sci SpA, I-20121 Milan, Italy

来源：

ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY | 2009年 / 9卷 / 07期

关键词：

Ser/Thr kinase inhibitors; ATP non-competitive; anticancer drugs; drug discovery; 2,3,5-TRISUBSTITUTED PYRIDINE-DERIVATIVES; ORAL MEK INHIBITOR; MAP KINASE; IN-VITRO; PROTEIN; ACTIVATION; DISCOVERY; CI-1040; JNK; IDENTIFICATION;

D O I：

10.2174/187152009789056930

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

Protein kinases are one of the largest known families of enzyme characterized by having a well conserved ATP binding pocket. Most of the synthetic kinase inhibitors are ATP-competitive, but display some potential problems, like selectivity, discrepancy between the in vitro and in vivo inhibition assays and an high risk of developing mutation inside the ATP-binding pocket. Recently some new inhibitors with a non-competitive mechanism of action were reported, with intresting results both in vitro and in vivo.

引用

页码：778 / 786

页数：9

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