Recent progress towards the identification of selective inhibitors of serine/threonine protein kinases.
Recent progress towards the identification of selective inhibitors of serine/threonine protein kinases.
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发表时间：
1999-03
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通讯作者：
J. Adams;D. Lee
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文献类型：
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作者：
J. Adams;D. Lee
蛋白质丝氨酸/苏氨酸激酶在制药工业目前追求的分子靶标中占有突出地位。鉴于哺乳动物激酶超家族保守的三级结构和催化机制，发现选择性抑制剂被证明是困难的，这并不奇怪。然而，在过去的两年中，进展加速，靶向ATP结合位点和反义RNA的方法已经成熟到将化合物推进临床试验的程度。为理解p38 MAP激酶抑制剂的吡啶基咪唑类的选择性的结构基础的发展是这一领域的主要进展。
Protein serine/threonine kinases figure prominently among the molecular targets currently being pursued by the pharmaceutical industry. Given the conserved tertiary structure and catalytic mechanism of the mammalian kinase superfamily, it is not surprising that the discovery of selective inhibitors has proven to be difficult. However, in the last two years, progress has accelerated and approaches that target the ATP binding site and antisense RNA have matured to the point of advancing compounds into clinical trials. The development of a structural basis for understanding the selectivity of the pyridinylimidazole class of p38 MAP kinase inhibitors has been a major advance in this area.