Parry D, Peters G
Imperial Cancer Research Fund Laboratories, London, United Kingdom.
Mol Cell Biol. 1996 Jul;16(7):3844-52. doi: 10.1128/MCB.16.7.3844.
Altered expression or function of the p16CDKN2 tumor suppressor gene on chromosome 9p21 occurs in a wide range of human tumors, and mutations in the gene have been shown to segregate with familial predisposition to malignant melanoma. We have used a variety of assays to examine the functional properties of tumor-associated alleles, including eight premature termination mutants, eight missense mutants, and three isoforms of p16 initiated at different amino-terminal methionine codons. The amino- and carboxy-terminal domains of the protein, outside the ankyrin-like repeats, appeared to be dispensable, but the majority of the premature termination mutations led to loss of function. Of the missense mutations tested, four displayed clear loss of function whereas two behaved like the wild type under all conditions tested. The remaining two mutations, a G-to-W mutation at position 101 (Gl01W) and V126D, both of which are associated with familial melanoma, were found to be temperature sensitive for binding to Cdk4 and Cdk6 in vitro, for inhibiting cyclin D1-Cdk4 in a reconstituted pRb-kinase assay, and for increasing the proportion of G1-phase cells following transfection. These findings clarify previous disparities and argue strongly that p16CDKN2 is a bona fide tumor suppressor associated with familial melanoma.
位于9号染色体p21区域的p16CDKN2肿瘤抑制基因的表达或功能改变在多种人类肿瘤中均有发生,并且该基因的突变已被证明与家族性恶性黑色素瘤易感性相关。我们使用了多种检测方法来研究肿瘤相关等位基因的功能特性,包括8个过早终止突变体、8个错义突变体以及3种由不同氨基末端甲硫氨酸密码子起始的p16异构体。该蛋白的氨基末端和羧基末端结构域(锚蛋白样重复序列之外)似乎是可有可无的,但大多数过早终止突变导致功能丧失。在所检测的错义突变中,4个表现出明显的功能丧失,而另外2个在所有检测条件下表现得与野生型相似。其余2个突变,即第101位的G-to-W突变(G101W)和V126D突变,这两个突变均与家族性黑色素瘤相关,发现在体外与Cdk4和Cdk6结合、在重组的pRb激酶检测中抑制细胞周期蛋白D1-Cdk4以及转染后增加G1期细胞比例方面对温度敏感。这些发现澄清了先前的差异,并有力地表明p16CDKN2是一种与家族性黑色素瘤相关的真正的肿瘤抑制基因。