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Review Article

Fak 和 Fak 抑制剂的新见解

卷 28, 期 17, 2021

发表于: 03 November, 2020

页: [3318 - 3338] 页: 21

弟呕挨: 10.2174/0929867327666201103162239

价格: $65

摘要

背景：黏附斑激酶(Focal adhesion kinase, Fak)是一种细胞质蛋白酪氨酸激酶，在不同的实体癌中过表达和激活;它在转移形成、细胞迁移、侵袭和血管生成中发挥了重要作用，因此被认为是癌症治疗的潜在靶点，特别是在转移阶段。近年来，不同的研究强调了新的Fak抑制剂作为潜在抗癌药物的重要性，但其他研究证明了其在与心脏功能或病毒感染相关的不同病理中的作用。 方法：一项广泛的文献研究(104篇参考文献)已经完成了Fak的结构，它在肿瘤发展中的重要性，但也在目前正在研究的其他病理中。因此，目前正在进行临床研究的化合物使用适当的数据库进行处理。最后，对目前临床前研究的主要化学支架进行了分析，重点分析了其分子结构和活性结构关系(SAR)。 结果：目前，只有少数可逆atp竞争抑制剂正在进行临床前研究和临床试验。其他化合物，与不同的化学支架，研究获得更活跃和选择性的Fak抑制剂。这篇综述综述了Fak在癌症和其他病理中的不同功能;今天的临床试验化合物和最近的化学支架(也包括在专利)给出了最有趣的结果进行了研究。此外，还报道了PROTAC分子。 结论：尽管已经从Fak抑制剂和其他不同的抗癌药物之间的关联中获得了有希望的信息，但所有报道的结果表明，需要进行更多的研究来设计和合成新的选择性和更活性的化合物。此外，在核水平和非癌细胞中，其他重要的作用被证明，使这种蛋白质成为药物化学中越来越重要的靶点。

关键词: 病灶粘附激酶，Fak抑制剂，转移，癌症治疗，临床试验，PROTACS

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