Prospects for prevention and treatment of cancer with selective PPARgamma modulators (SPARMs).
Prospects for prevention and treatment of cancer with selective PPARgamma modulators (SPARMs).
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使用选择性 PPARgamma 调节剂 (SPARM) 预防和治疗癌症的前景。
DOI：
10.1016/s1471-4914(01)02100-1
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发表时间：
2001
期刊：
影响因子：
--
通讯作者：
Mangelsdorf,DJ
中科院分区：
文献类型：
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作者：
Sporn,MB;Suh,N;Mangelsdorf,DJ
过氧化物酶体增殖物激活受体γ（Peroxisome proliferator-activated receptor γ，PPARγ）是一种核受体和转录因子，可调控多种与肿瘤发生相关的基因的表达，是肿瘤防治新药开发的重要靶点。过氧化物酶体增殖物激活受体γ的表达不足可能是致癌的一个重要危险因素，尽管在某些情况下过表达会增强致癌作用。PPARγ配体在实验模型中抑制乳腺癌发生并诱导人脂肪肉瘤细胞分化。通过类比选择性雌激素受体调节剂（SERM）的概念，建议选择性PPARγ调节剂（SPARMs），设计为对特定基因和靶组织具有期望的作用而不对其他基因和靶组织产生不良影响，将在未来的癌症化学预防和化学治疗中具有重要的临床意义。
Peroxisome proliferator-activated receptor γ (PPARγ), a nuclear receptor and transcription factor that regulates the expression of many genes relevant to carcinogenesis, is now an important target for development of new drugs for the prevention and treatment of cancer. Deficient expression of PPARγ can be a significant risk factor for carcinogenesis, although in some cases overexpression enhances carcinogenesis. Ligands for PPARγ suppress breast carcinogenesis in experimental models and induce differentiation of human liposarcoma cells. By analogy to the selective estrogen receptor modulator (SERM) concept, it is suggested that selective PPARγ modulators (SPARMs), designed to have desired effects on specific genes and target tissues without undesirable effects on others, will be clinically important in the future for chemoprevention and chemotherapy of cancer.