芳香化酶抑制剂:作用机制和治疗乳腺癌的作用。

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芳香化酶抑制剂:作用机制和治疗乳腺癌的作用。

Semin 8月杂志。2003;30 (4 5 14):3-11。

PubMed ID

14513432 (在PubMed

]

文摘

乳腺癌的自然历史与雌激素密切相关。这些激素影响疾病风险和许多建立了肿瘤的生长。因此,措施,抑制合成或阻止雌激素的作用机制是有吸引力的治疗策略。这尤其适用于绝经后妇女激素反应是常见的和雌激素的合成主要是坐落在书中脂肪组织,肌肉和乳腺组织,而不是在绝经前妇女的卵巢。抑制生产而言,最具体的效果是最好的实现通过阻断生物合成的最后一步,转换heme-containing雄激素向雌激素的酶,芳香化酶。两个主要的类芳香化酶抑制剂的开发,目前在临床使用。I型甾体药物包括formestane和依西美坦;他们是雄激素结合的底物类似物有竞争力但不可逆酶和被宣传成“抑制剂”。Type II nonsteroidal inhibitors such as anastrozole and letrozole are triazoles; they bind reversibly to the enzyme and fit into the substrate binding site, such that azole nitrogens interact with the heme prosthetic group. This type of association provides exquisite potency for and specificity against the aromatase enzyme. These agents represent several generations of development, with each step in the evolution producing an increase in both potency and specificity. The latest aromatase inhibitors are drugs of immense potential that will undoubtedly play a major role in the management of postmenopausal women with hormone-dependent breast cancer. They also represent tools by which to elucidate the roles of both aromatase and estrogen in the development and growth of breast cancer.

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药物靶点

药物	目标	类	生物	药理作用	行动
阿那曲唑	细胞色素P450 19 a1	蛋白质	人类	是的	抑制剂	细节