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三苯氧胺的主要作用是由于它和代谢物与雌激素受体结合,阻止了3H雌二醇与乳腺肿瘤雌激素受体的结合,使乳腺癌细胞积聚在细胞周期的Go/G1期而抑制生长。其抗肿瘤活性不是杀细胞而是细胞抑制剂。此外,三苯氧胺刺激孕酮受体的产生和肝脏合成佳激素结合球蛋白,后者是血液中主要运输雌激素的蛋白。因此它的含量增加时可使血浆中游离的类固醇浓度降低,减少类固醇对乳腺癌细胞的作用。三苯氧胺还具有非雌激素受体媒介的作用:它与钙调素结合,与细胞中微粒体的抗雌激素部位结合,与蛋白激酶c结合,增加NK细胞活性等。这些作用在临床应用上可能更重要,但确切机
The main effect of tamoxifen is that it binds to estrogen receptors with its metabolites, preventing the binding of 3H estradiol to the estrogen receptor of breast tumors, causing breast cancer cells to accumulate in the Go/G1 phase of the cell cycle and inhibiting growth. Its anti-tumor activity is not cytotoxic but a cytostatic agent. In addition, tamoxifen stimulates the production of progesterone receptors and liver synthesis of good hormone-binding globulin, which is the protein that mainly transports estrogens in the blood. Therefore, when its content increases, the concentration of free steroids in the plasma can be reduced, and the effect of steroids on breast cancer cells can be reduced. Tamoxifen also functions as a non-estrogen receptor mediator: it binds to calmodulin, binds to the anti-estrogenic site of microsomes in cells, binds to protein kinase c, and increases NK cell activity. These effects may be more important in clinical applications, but the exact machine