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首页> 外文期刊>Expert opinion on therapeutic targets >Targeting Pyk2 for therapeutic intervention.
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Targeting Pyk2 for therapeutic intervention.

机译：靶向Pyk2进行治疗干预。

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IMPORTANCE OF THE FIELD: The focal adhesion tyrosine kinases FAK and Pyk2 are uniquely situated to act as critical mediators for the activation of signaling pathways that regulate cell migration, proliferation and survival. By coordinating adhesion and cytoskeletal dynamics with survival and growth signaling, FAK and Pyk2 represent molecular therapeutic targets in cancer as malignant cells often exhibit defects in these processes. AREAS COVERED IN THIS REVIEW: This review examines the structure and function of the focal adhesion kinase Pyk2 and intends to provide a rationale for the employment of modulating strategies that include both catalytic and extra-catalytic approaches that have been developed in the last 3 - 5 years. WHAT THE READER WILL GAIN: Targeting tyrosine kinases in oncology has focused on the ATP binding pocket as means to inhibit catalytic activity and downregulate pathways involved in tumor invasion. This review discusses the available catalytic inhibitors and compares them to the alternative approach of targeting protein-protein interactions that regulate kinase activity. TAKE HOME MESSAGE: Development of specific catalytic inhibitors of the focal adhesion kinases has improved but significant challenges remain. Thus, approaches that inhibit the effector function of Pyk2 by targeting regulatory modules can increase specificity and will be a welcome asset to the therapeutic arena.
机译：领域的重要性：黏着斑酪氨酸激酶FAK和Pyk2的位置独特，可充当激活调节细胞迁移，增殖和存活的信号通路的关键介体。通过协调粘附和细胞骨架动力学与生存和生长信号，FAK和Pyk2代表了癌症中的分子治疗靶标，因为恶性细胞通常在这些过程中表现出缺陷。这篇综述中涵盖的领域：这篇综述检查了粘着斑激酶Pyk2的结构和功能，旨在为采用调节策略提供理论依据，这些策略包括最近3-5中开发的催化方法和超催化方法年份。读者所能获得的收益：肿瘤学中靶向酪氨酸激酶的研究重点放在ATP结合口袋上，以抑制催化活性并下调与肿瘤浸润有关的途径。这篇综述讨论了可用的催化抑制剂，并将它们与靶向调节激酶活性的蛋白相互作用的另一种方法进行了比较。温馨提示：粘着斑激酶特异性催化抑制剂的开发有所改善，但仍然存在重大挑战。因此，通过靶向调节模块来抑制Pyk2的效应子功能的方法可以提高特异性，将成为治疗领域的一项受欢迎的资产。

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