Hart Stephen M
Dept. of Cancer Medicine, Division of Medicine, Faculty of Medicine, Imperial College of Science, Technology & Medicine, Du Cane Road, London W12 0NN, UK.
Biol Res. 2002;35(2):295-303. doi: 10.4067/s0716-97602002000200021.
Nuclear receptors comprise a family of transcription factors that regulate gene expression in a ligand dependent manner. They can activate or repress target genes by binding directly to DNA response elements as homo- or hetero-dimers or by binding to other classes of DNA-bound transcription factors. These activities have been linked to the formation of complexes with molecules that appear to serve as coactivators or corepressors, causing local modification of chromatin structure in order to regulate expression of their target genes. Several members of nuclear receptor family are directly associated with human malignancies including breast cancer, prostate cancer and leukaemia. The pathogenesis of each of these diseases is underpinned by the activities of a member of the superfamily; estrogen receptor-alpha (ER alpha) in breast cancer, androgen receptor (AR) in prostate cancer, and retinoic acid receptor alpha (RAR alpha) in acute promyelocytic leukaemia.
核受体是一类转录因子家族，它们以配体依赖的方式调节基因表达。它们可以通过作为同二聚体或异二聚体直接结合DNA反应元件，或通过与其他类别的DNA结合转录因子结合来激活或抑制靶基因。这些活性与与似乎作为共激活剂或共抑制因子的分子形成复合物有关，导致染色质结构的局部修饰，从而调节其靶基因的表达。核受体家族的几个成员与人类恶性肿瘤直接相关，包括乳腺癌、前列腺癌和白血病。这些疾病中每一种的发病机制都由该超家族的一个成员的活性所支撑；乳腺癌中的雌激素受体α（ERα）、前列腺癌中的雄激素受体（AR）和急性早幼粒细胞白血病中的维甲酸受体α（RARα）。
