Department of Antibody Discovery & Protein Engineering, AstraZeneca plc, Gaithersburg, MD, United States of America.
Department of Clinical Pharmacology & Safety Sciences, AstraZeneca plc, Gaithersburg, MD, United States of America.
PLoS One. 2020 Jun 4;15(6):e0234268. doi: 10.1371/journal.pone.0234268. eCollection 2020.
Annexin A1 (anxA1) is an immunomodulatory protein that has been proposed as a tumor vascular target for antitumor biologic agents, yet to date the vascular expression of anxA1 in specific tumor indications has not been systematically assessed. Attempts to evaluate vascular anxA1 expression by immunohistochemistry are complicated by a lack of available antibodies that are both specific for anxA1 and bind the N-terminal-truncated form of anxA1 that has previously been identified in tumor vasculature. To study the vascular expression pattern of anxA1 in non-small-cell lung carcinoma (NSCLC), we isolated an antibody capable of binding N-terminal-truncated anxA127-346 and employed it in immunohistochemical studies of human lung specimens. Lung tumor specimens evaluated with this antibody revealed vascular (endothelial) anxA1 expression in five of eight tumor samples studied, but no vascular anxA1 expression was observed in normal lung tissue. Tumor microarray analysis further demonstrated positive vascular staining for anxA1 in 30 of 80 NSCLC samples, and positive staining of neoplastic cells was observed in 54 of 80 samples. No correlation was observed between vascular and parenchymal anxA1 expression. Two rodent tumor models, B16-F10 and Py230, were determined to have upregulated anxA1 expression in the intratumoral vasculature. These data validate anxA1 as a potential vascular anti-tumor target in a subset of human lung tumors and identify rodent models which demonstrate anxA1 expression in tumor vasculature.
膜联蛋白 A1(anxA1)是一种免疫调节蛋白,它被提议作为抗肿瘤生物制剂的肿瘤血管靶点,但迄今为止,特定肿瘤适应证中 anxA1 的血管表达尚未得到系统评估。尝试通过免疫组织化学评估血管 anxA1 表达受到缺乏既针对 anxA1 又结合先前在肿瘤血管中鉴定的 anxA1 N 端截断形式的可用抗体的阻碍。为了研究非小细胞肺癌(NSCLC)中 anxA1 的血管表达模式,我们分离出一种能够结合 N 端截断 anxA127-346 的抗体,并将其用于人类肺标本的免疫组织化学研究。用该抗体评估的肺肿瘤标本在研究的 8 个肿瘤样本中的 5 个中显示出血管(内皮)anxA1 表达,但在正常肺组织中未观察到血管 anxA1 表达。肿瘤微阵列分析进一步表明,在 80 个 NSCLC 样本中的 30 个中观察到 anxA1 血管阳性染色,在 80 个样本中的 54 个中观察到肿瘤细胞阳性染色。未观察到血管和实质 anxA1 表达之间的相关性。B16-F10 和 Py230 两种啮齿动物肿瘤模型被确定为肿瘤内血管中 anxA1 表达上调。这些数据验证了 anxA1 作为人类肺肿瘤中一部分的潜在血管抗肿瘤靶点,并确定了在肿瘤血管中显示 anxA1 表达的啮齿动物模型。