The development of protein kinase inhibitors (PKIs) has gained significance owing to their therapeutic potential for diseases like cancer. In addition, there has been a rise in refining kinase activity assays, each possessing unique biological and analytical characteristics crucial for PKI development. However, the PKI development pipeline experiences high attrition rates and approved PKIs exhibit unexploited potential because of variable patient responses. Enhancing PKI development efficiency involves addressing challenges related to understanding the PKI mechanism of action and employing biomarkers for precision medicine. Selecting appropriate kinase activity assays for these challenges can overcome these attrition rate issues. This review delves into the current obstacles in kinase inhibitor development and elucidates kinase activity assays that can provide solutions.

中文翻译：

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测量激酶活性的创新策略，以加速下一波新型激酶抑制剂的开发


蛋白激酶抑制剂（PKIs）的开发因其对癌症等疾病的治疗潜力而具有重要意义。此外，激酶活性检测的精炼也在不断增加，每种检测都具有对 PKI 开发至关重要的独特生物学和分析特性。然而，PKI 开发渠道的流失率很高，并且由于患者反应各异，已批准的 PKI 表现出未开发的潜力。提高 PKI 开发效率涉及解决与了解 PKI 作用机制和利用生物标志物进行精准医疗相关的挑战。针对这些挑战选择适当的激酶活性测定可以克服这些损耗率问题。本综述深入探讨了激酶抑制剂开发中当前的障碍，并阐明了可以提供解决方案的激酶活性测定。