Division of Radiation and Cancer Biology, Department of Radiation Oncology, Center for Clinical Sciences Research, Stanford University, Stanford, California 94305-5152, USA.
Cancer Res. 2010 Oct 1;70(19):7570-9. doi: 10.1158/0008-5472.CAN-10-1267. Epub 2010 Sep 21.
The receptor tyrosine kinase AXL is thought to play a role in metastasis; however, the therapeutic efficacy of an AXL-targeting agent remains largely untested in metastatic disease. In this study, we defined AXL as a therapeutic target for metastatic ovarian cancer. AXL is primarily expressed in metastases and advanced-stage human ovarian tumors but not in normal ovarian epithelium. Genetic inhibition of AXL in human metastatic ovarian tumor cells is sufficient to prevent the initiation of metastatic disease in vivo. Mechanistically, inhibition of AXL signaling in animals with metastatic disease results in decreased invasion and matrix metalloproteinase activity. Most importantly, soluble human AXL receptors that imposed a specific blockade of the GAS6/AXL pathway had a profound inhibitory effect on progression of established metastatic ovarian cancer without normal tissue toxicity. These results offer the first genetic validation of GAS6/AXL targeting as an effective strategy for inhibition of metastatic tumor progression in vivo. Furthermore, this study defines the soluble AXL receptor as a therapeutic candidate agent for treatment of metastatic ovarian cancer, for which current therapies are ineffective.
受体酪氨酸激酶 AXL 被认为在转移中起作用;然而,AXL 靶向药物在转移性疾病中的治疗效果在很大程度上仍未经测试。在这项研究中,我们将 AXL 定义为转移性卵巢癌的治疗靶点。AXL 主要在转移和晚期人类卵巢肿瘤中表达,但不在正常卵巢上皮中表达。在体内,对人类转移性卵巢肿瘤细胞中的 AXL 进行遗传抑制足以阻止转移性疾病的发生。从机制上讲,在患有转移性疾病的动物中抑制 AXL 信号会导致侵袭和基质金属蛋白酶活性降低。最重要的是,可溶性人 AXL 受体对 GAS6/AXL 途径施加了特异性阻断,对已建立的转移性卵巢癌的进展具有深远的抑制作用,而对正常组织没有毒性。这些结果首次在体内遗传验证了 GAS6/AXL 靶向作为抑制转移性肿瘤进展的有效策略。此外,这项研究将可溶性 AXL 受体定义为治疗转移性卵巢癌的治疗候选药物,目前的治疗方法对此无效。