Department of Radiation Oncology, Mayo Clinic, Rochester, MN 55905, United States.
Department of Oncology, Mayo Clinic, Rochester, MN 55905, United States.
Drug Resist Updat. 2024 May;74:101085. doi: 10.1016/j.drup.2024.101085. Epub 2024 Apr 16.
Enhanced DNA repair is an important mechanism of inherent and acquired resistance to DNA targeted therapies, including poly ADP ribose polymerase (PARP) inhibition. Spleen associated tyrosine kinase (Syk) is a non-receptor tyrosine kinase acknowledged for its regulatory roles in immune cell function, cell adhesion, and vascular development. This study presents evidence indicating that Syk expression in high-grade serous ovarian cancer and triple-negative breast cancers promotes DNA double-strand break resection, homologous recombination (HR), and subsequent therapeutic resistance. Our investigations reveal that Syk is activated by ATM following DNA damage and is recruited to DNA double-strand breaks by NBS1. Once localized to the break site, Syk phosphorylates CtIP, a pivotal mediator of resection and HR, at Thr-847 to promote repair activity, particularly in Syk-expressing cancer cells. Inhibition of Syk or its genetic deletion impedes CtIP Thr-847 phosphorylation and overcomes the resistant phenotype. Collectively, our findings suggest a model wherein Syk fosters therapeutic resistance by promoting DNA resection and HR through a hitherto uncharacterized ATM-Syk-CtIP pathway. Moreover, Syk emerges as a promising tumor-specific target to sensitize Syk-expressing tumors to PARP inhibitors, radiation and other DNA-targeted therapies.
增强的 DNA 修复是固有和获得性对 DNA 靶向治疗(包括聚 ADP 核糖聚合酶(PARP)抑制)的抗性的重要机制。脾相关酪氨酸激酶(Syk)是一种非受体酪氨酸激酶,其在免疫细胞功能、细胞黏附和血管发育中的调节作用已得到认可。本研究提供了证据表明,Syk 在高级别浆液性卵巢癌和三阴性乳腺癌中的表达促进了 DNA 双链断裂切除、同源重组(HR)和随后的治疗耐药性。我们的研究表明,Syk 在 DNA 损伤后被 ATM 激活,并通过 NBS1 募集到 DNA 双链断裂处。一旦定位于断裂部位,Syk 就会磷酸化 CtIP,这是切除和 HR 的关键介质,在 Thr-847 处促进修复活性,特别是在表达 Syk 的癌细胞中。Syk 的抑制或其基因缺失会阻碍 CtIP Thr-847 的磷酸化,并克服耐药表型。总的来说,我们的研究结果表明了一种模型,即 Syk 通过促进迄今为止尚未表征的 ATM-Syk-CtIP 途径的 DNA 切除和 HR,促进治疗耐药性。此外,Syk 作为一种有前途的肿瘤特异性靶点,可以使表达 Syk 的肿瘤对 PARP 抑制剂、辐射和其他 DNA 靶向治疗敏感。