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首页> 外文期刊>Combinatorial Chemistry & High Throughput Screening >Creating Chemical Diversity to Target Protein Kinases
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Creating Chemical Diversity to Target Protein Kinases

机译:建立化学多样性以靶向蛋白质激酶

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摘要

Protein kinases play crucial roles in regulating virtually every cellular process and are currently attracting tremendous interest as drug targets from the pharmaceutical industry. The major challenges facing the development of the potential kinase inhibitor drugs are: selectivity, physical properties (solubility, molecular weight), and pharmacological properties (bioavailability, half life, toxicity, etc.) This review focuses on how selective protein kinase inhibitors that target the ATP and allosteric binding sites are currently being identified and optimized.
机译:蛋白激酶在调节几乎每个细胞过程中都起着至关重要的作用,目前作为制药行业的药物靶标引起了人们极大的兴趣。潜在激酶抑制剂药物的开发面临的主要挑战是:选择性,物理性质(溶解度,分子量)和药理性质(生物利用度,半衰期,毒性等)。这篇综述着重于如何针对性地选择蛋白激酶抑制剂目前正在确定和优化ATP和变构结合位点。

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