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[去势抵抗性前列腺癌中的新一代雄激素受体拮抗剂]

[New generation of androgen receptor antagonist in castration resistant prostate cancer].

作者信息

Uemura Hiroji

出版信息

Nihon Rinsho. 2014 Dec;72(12):2164-9.

Abstract

Androgen ablation therapy is performed for prostate cancer patients especially with advanced stage. Nevertheless, outgrowth of hormone independent cancer cells occurs within several years and leads to a lethal condition, so-called castration resistant prostate cancer (CRPC). Even in CRPC cells under low levels of serum androgens, androgen receptor (AR) signaling still functions and is engaged in the establishment of CRPC. Recently, novel AR antagonists have been developed such as enzalutamide or ARN-509. This review focuses on these AR antagonists that have some features including high affinity to AR compared with bicalutamide, preventing nuclear translocation and DNA binding. These new hormonal agents have changed the landscape of CRPC treatment with a promising outcome.

摘要

雄激素剥夺疗法主要用于晚期前列腺癌患者。然而,数年内会出现激素非依赖性癌细胞的生长,并导致致命状况,即所谓的去势抵抗性前列腺癌(CRPC)。即使在血清雄激素水平较低的CRPC细胞中,雄激素受体(AR)信号传导仍起作用,并参与CRPC的形成。最近,已开发出新型AR拮抗剂,如恩杂鲁胺或ARN-509。本综述重点关注这些AR拮抗剂,它们具有一些特点,包括与比卡鲁胺相比对AR具有高亲和力,可阻止核转位和DNA结合。这些新型激素药物改变了CRPC的治疗格局,前景乐观。

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