Department of Biopharmacy, University of Debrecen, 4032 Debrecen, Hungary.
Department of Pathology, University of Debrecen, 4032 Debrecen, Hungary.
Molecules. 2018 Jun 26;23(7):1535. doi: 10.3390/molecules23071535.
Uveal melanoma (UM) is the most common primary intraocular malignancy in adults, with an incidence of 4⁻5 cases per million. The prognosis of UM is very poor. In the present study, our aim was to investigate the expression of mRNA and protein for somatostatin receptor types-1, -2, -3, -4, -5 (SSTR-1⁻5) in human UM tissue samples and in OCM-1 and OCM-3 human UM cell lines by qRT-PCR, western blot and ligand competition assay. The mRNA for SSTR-2 showed markedly higher expression in UM tissues than SSTR-5. The presence of SSTRs was demonstrated in 70% of UM specimens using ligand competition assay and both human UM models displayed specific high affinity SSTRs. Among the five SSTRs, the mRNA investigated for SSTR-2 and SSTR-5 receptors was strongly expressed in both human UM cell lines, SSTR-5 showing the highest expression. The presence of the SSTR-2 and SSTR-5 receptor proteins was confirmed in both cell lines by western blot. In summary, the expression of somatostatin receptors in human UM specimens and in OCM-1 and OCM-3 human UM cell lines suggests that they could serve as a potential molecular target for therapy of UM using modern powerful cytotoxic SST analogs targeting SSTR-2 and SSTR-5 receptors.
葡萄膜黑色素瘤 (UM) 是成年人中最常见的原发性眼内恶性肿瘤，发病率为每百万 4⁻5 例。UM 的预后非常差。在本研究中，我们旨在通过 qRT-PCR、western blot 和配体竞争分析，研究 somatostatin 受体类型-1、-2、-3、-4、-5（SSTR-1⁻5）在人 UM 组织样本和 OCM-1 和 OCM-3 人 UM 细胞系中的 mRNA 和蛋白表达。与 SSTR-5 相比，SSTR-2 在 UM 组织中的 mRNA 表达明显更高。通过配体竞争分析，在 70%的 UM 标本中证实了 SSTRs 的存在，两种人 UM 模型均显示出特异性高亲和力 SSTRs。在这五个 SSTR 中，研究的 SSTR-2 和 SSTR-5 受体 mRNA 在两种人 UM 细胞系中均强烈表达，SSTR-5 表达最高。western blot 证实了两种细胞系中 SSTR-2 和 SSTR-5 受体蛋白的存在。总之，人 UM 标本和 OCM-1 和 OCM-3 人 UM 细胞系中 somatostatin 受体的表达表明，它们可能成为使用针对 SSTR-2 和 SSTR-5 受体的现代强大细胞毒性 SST 类似物治疗 UM 的潜在分子靶标。
