Eden P A, Taylor J E
Biomeasure Inc, Milford, MA 01757-3650.
Life Sci. 1993;53(1):85-90. doi: 10.1016/0024-3205(93)90614-9.
Somatostatin (SRIF) analogues display anti-tumor properties believed to be mediated by specific cell surface somatostatin receptors (SSTR). SSTR subtypes have unique pharmacological properties, including specific GTP-binding protein coupling, ion channel regulation, and cAMP inhibition; therefore, identification of isotypes expressed in tumor cells facilitates current efforts to design potent anti-tumor SRIF analogues. Human and rodent solid, transplantable tumors and tumor cell lines were examined for gene expression of SSTR1, SSTR2 and SSTR3 by reverse transcription of tumor mRNA and subsequent amplification of cDNA by the polymerase chain reaction, using SSTR subtype-specific oligonucleotide primers. SSTR2 mRNA transcripts were observed in all of the tumor cell lines examined. SSTR1 gene expression was seen in several human and rat tumor types, and SSTR3 gene expression observed in two rodent tumor types. SSTR mRNA-positive tumors are expected to possess membrane-bound receptors which could potentially interact with anti-tumor SRIF analogues.
生长抑素(SRIF)类似物具有抗肿瘤特性,据信这是由特定的细胞表面生长抑素受体(SSTR)介导的。SSTR亚型具有独特的药理学特性,包括特定的GTP结合蛋白偶联、离子通道调节和cAMP抑制;因此,鉴定肿瘤细胞中表达的同型物有助于当前设计强效抗肿瘤SRIF类似物的努力。通过肿瘤mRNA的逆转录以及随后使用SSTR亚型特异性寡核苷酸引物通过聚合酶链反应扩增cDNA,对人和啮齿动物的实体可移植肿瘤及肿瘤细胞系进行SSTR1、SSTR2和SSTR3基因表达检测。在所检测的所有肿瘤细胞系中均观察到SSTR2 mRNA转录本。在几种人类和大鼠肿瘤类型中可见SSTR1基因表达,在两种啮齿动物肿瘤类型中观察到SSTR3基因表达。预计SSTR mRNA阳性肿瘤会拥有可与抗肿瘤SRIF类似物潜在相互作用的膜结合受体。