Boehringer Ingelheim RCV, Dr. Boehringer Gasse 5-11, 1121 Vienna, Austria.
Cancer Biomark. 2010;9(1-6):267-86. doi: 10.3233/CBM-2011-0164.
Cutaneous melanoma is a highly aggressive cancer with still limited, but increasingly efficacious, standard treatment options. Recent preclinical and clinical findings support the notion that cutaneous melanoma is not one malignant disorder but rather a family of distinct molecular diseases. Incorporation of genetic signatures into the conventional histopathological classification of melanoma already has great implications for the management of cutaneous melanoma. Herein, we review our rapidly growing understanding of the molecular biology of cutaneous melanoma, including the pathogenic roles of the mitogen-associated protein kinase (MAPK) pathway, the phosphatidylinositol 3 kinase [PI3K]/phosphatase and tensin homologue deleted on chromosome 10 [PTEN]/Akt/mammalian target of rapamycin [mTOR])PTEN (phosphatase and tensin homolog) pathway, MET (hepatocyte growth factor), Notch signaling, and other key molecules regulating cell cycle progression and apoptosis. The mutation Val600Glu in the BRAF oncogene (designated BRAF(V600E)) has been associated with clinical benefit from agents that inhibit BRAF(V600E) or MEK (a kinase in the MAPK pathway). Cutaneous melanomas arising from mucosal, acral, chronically sun-damaged surfaces sometimes have oncogenic mutations in KIT, against which several inhibitors have shown clinical efficacy. These findings suggest that prospective genotyping of patients with melanoma, combined with the growing availability of targeted agents, which can be used to rationally exploit these findings, should be used increasingly as we work to develop new and more effective treatments for this devastating disease.
皮肤黑色素瘤是一种高度侵袭性的癌症,目前的标准治疗选择有限,但越来越有效。最近的临床前和临床研究结果支持这样一种观点,即皮肤黑色素瘤不是一种恶性疾病,而是一组不同的分子疾病。将遗传特征纳入黑色素瘤的常规组织病理学分类已经对皮肤黑色素瘤的管理产生了重大影响。在此,我们回顾了我们对皮肤黑色素瘤分子生物学的快速增长的认识,包括丝裂原活化蛋白激酶(MAPK)途径、磷脂酰肌醇 3 激酶[PI3K]/磷酸酶和张力蛋白同源物缺失的致癌作用[PTEN]/Akt/哺乳动物雷帕霉素靶蛋白[mTOR])PTEN(磷酸酶和张力蛋白同源物)途径、MET(肝细胞生长因子)、Notch 信号通路和其他调节细胞周期进程和细胞凋亡的关键分子。BRAF 致癌基因(命名为 BRAF(V600E))中的 Val600Glu 突变与抑制 BRAF(V600E)或 MEK(MAPK 途径中的一种激酶)的药物的临床获益相关。源自粘膜、肢端、慢性日光损伤表面的皮肤黑色素瘤有时会发生 KIT 的致癌突变,针对这些突变,几种抑制剂已显示出临床疗效。这些发现表明,对黑色素瘤患者进行前瞻性基因分型,结合越来越多的靶向药物的应用,这些药物可以被用来合理地利用这些发现,应该越来越多地被用于开发这种毁灭性疾病的新的、更有效的治疗方法。