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为去势抵抗性前列腺癌选择激酶抑制剂

英文原题:Choosing Kinase Inhibitors for Androgen Deprivation Therapy-Resistant Prostate Cancer.

查看英文原题

Choosing Kinase Inhibitors for Androgen Deprivation Therapy-Resistant Prostate Cancer.

PubMed 2022/02/24(内容时间) Pharmaceutics Q1 · IF 6.9(JCR 2025)

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中文摘要

雄激素剥夺疗法(ADT)是晚期前列腺癌(PCa)的全身性治疗方法。尽管大多数患者最初对ADT有反应,但几乎所有癌症最终都会发展为去势抵抗。去势抵抗性PCa(CRPC)预后极差,其治疗是一项严峻的临床挑战。越来越多的证据表明,多种激酶的异常表达和激活与CRPC的发生和维持相关。为靶向CRPC中的关键激酶,已开展了大量小分子抑制剂的开发工作。这些抑制剂旨在抑制激酶活性或阻断与PCa雄激素非依赖性(AI)生长及CRPC发展相关的激酶介导的信号通路。在本综述中,我们简要总结了在CRPC中异常表达和/或激活的激酶的作用,以及靶向激酶的小分子抑制剂用于治疗CRPC的最新进展。

展开英文摘要原文

Androgen deprivation therapy (ADT) is a systemic therapy for advanced prostate cancer (PCa). Although most patients initially respond to ADT, almost all cancers eventually develop castration resistance. Castration-resistant PCa (CRPC) is associated with a very poor prognosis, and the treatment of which is a serious clinical challenge. Accumulating evidence suggests that abnormal expression and activation of various kinases are associated with the emergence and maintenance of CRPC.

Many efforts have been made to develop small molecule inhibitors to target the key kinases in CRPC. These inhibitors are designed to suppress the kinase activity or interrupt kinase-mediated signal pathways that are associated with PCa androgen-independent (AI) growth and CRPC development. In this review, we briefly summarize the roles of the kinases that are abnormally expressed and/or activated in CRPC and the recent advances in the development of small molecule inhibitors that target kinases for the treatment of CRPC.

论文信息

作者
Zhong S、Peng S、Chen Z、Chen Z、Luo JL
第一作者单位
Department of General Surgery, Xiangya Hospital, Central South University, Hunan 410008, China.China
通讯作者单位
Department of Molecular Medicine, The Scripps Research Institute, Jupiter, FL 33459, USA.United States
文献类型
综述
期刊
Pharmaceutics2022 Feb 24
原文标识
PubMed 35335873 · DOI 10.3390/pharmaceutics14030498