University Medical Center Hamburg - Eppendorf, Hubertus Wald University Cancer Center Hamburg, Department of Oncology/Hematology with Sections BMT and Pneumology, Hamburg, Germany.
Anticancer Agents Med Chem. 2011 Sep;11(7):593-9. doi: 10.2174/187152011796817727.
Since its first description Focal Adhesion Kinase (FAK), a cytoplasmatic tyrosine kinase, has been implicated in the formation and progression of solid and liquid malignant tumors. Therefore orally available selective small molecule inhibitors of FAK have been developed, three of them (PF-562-271, PF-04554878 and GSK2256098) are already in clinical testing. This review discusses the recent data obtained from these Phase 1 trials. We also discuss available data on the mechanisms of action of these inhibitors in carcinogenesis and demonstrate that FAK plays an important role in neoangiogenesis which is a crucial step in cancer growth.
自首次描述以来，黏着斑激酶（FAK）作为一种细胞质酪氨酸激酶，已被牵涉到实体瘤和液体恶性肿瘤的形成和进展中。因此，已经开发出了几种可口服的 FAK 选择性小分子抑制剂，其中三种（PF-562-271、PF-04554878 和 GSK2256098）已经在临床试验中进行了测试。这篇综述讨论了从这些 I 期试验中获得的最新数据。我们还讨论了这些抑制剂在致癌作用中的作用机制的现有数据，并证明 FAK 在新血管生成中发挥重要作用，新血管生成是癌症生长的关键步骤。
