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首页> 外文期刊>Proceedings of the National Academy of Sciences of the United States of America >An endothelin receptor B antagonist inhibits growth and cell death in human melanoma cells in vitro and in vivo
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An endothelin receptor B antagonist inhibits growth and cell death in human melanoma cells in vitro and in vivo

机译：内皮素B受体拮抗剂在体外和体内抑制人黑素瘤细胞的生长和细胞死亡

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摘要

Activation of the endothelin receptor B (ETRB) in cultured melanocyte precursors promotes cell proliferation while inhibiting differentiation, two hallmarks of malignant transformation. We therefore tested whether ETRB has a similar role in malignant transformation of melanoma. When tested in culture, we find that the selective ETRB antagonist BQ788 can inhibit the growth of seven human melanoma cell lines, but not a human kidney cell line. This inhibition often is associated with increases in pigmentation and in the dendritic shape that is characteristic of mature melanocytes. In three cell lines we also observe a major increase in cell death. In contrast, the endothelin receptor A (ETRA) antagonist BQ123 does not have these effects, al- though all the cell lines express both ETRA and ETRB mRNA. Extending these studies in vivo, we find that administration of BQ788 significantly slows human melanoma tumor growth in nude mice, including a complete growth arrest in half of the mice treated systemically. Histological examination of tumor sections suggests that BQ788 also enhances melanoma cell death in vivo. Thus, ETRB inhibitors may be beneficial for the treatment of melanoma.
机译：培养的黑素细胞前体中内皮素受体B（ETRB）的活化促进细胞增殖，同时抑制分化，这是恶性转化的两个标志。因此，我们测试了ETRB在黑色素瘤的恶性转化中是否具有相似的作用。在文化中测试时，我们发现选择性ETRB拮抗剂BQ788可以抑制7种人类黑素瘤细胞系的生长，但不能抑制人类肾细胞系的生长。这种抑制作用通常与色素沉着的增加和成熟黑素细胞所特有的树突状形状有关。在三种细胞系中，我们还观察到细胞死亡的大幅增加。相反，内皮素受体A（ETRA）拮抗剂BQ123没有这些作用，尽管所有细胞系都表达ETRA和ETRB mRNA。在体内扩展这些研究后，我们发现BQ788的使用显着减慢了裸鼠中人黑色素瘤的生长速度，其中包括一半接受全身治疗的小鼠的完全生长停滞。肿瘤切片的组织学检查表明，BQ788还可以增强体内黑色素瘤细胞的死亡。因此，ETRB抑制剂可能对黑色素瘤的治疗有益。

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