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抑制热休克蛋白90可增强多西他赛对去势抵抗性前列腺癌的治疗效果。

Inhibition of Hsp90 augments docetaxel therapy in castrate resistant prostate cancer.

作者信息

Ku ShengYu, Lasorsa Elena, Adelaiye Remi, Ramakrishnan Swathi, Ellis Leigh, Pili Roberto

机构信息

Genitourinary Program, Roswell Park Cancer Institute, Buffalo, New York, United States of America; Department of Cancer Prevention and Pathology, Roswell Park Cancer Institute, Buffalo, New York, United States of America.

Genitourinary Program, Roswell Park Cancer Institute, Buffalo, New York, United States of America; Department of Pharmacology and Therapeutics, Roswell Park Cancer Institute, Buffalo, New York, United States of America.

出版信息

PLoS One. 2014 Jul 29;9(7):e103680. doi: 10.1371/journal.pone.0103680. eCollection 2014.

Abstract

First line treatment of patients with castrate resistant prostate cancer (CRPC) primarily involves administration of docetaxel chemotherapy. Unfortunately, resistance to docetaxel therapy is an ultimate occurrence. Alterations in androgen receptor (AR) expression and signaling are associated mechanisms underlying resistance to docetaxel treatment in CRPC. Heat shock protein 90 (Hsp90) is a molecular chaperone, which regulates the activation, maturation and stability of critical signaling proteins involved in prostate cancer, including the AR. This knowledge and recent advances in compound design and development have highlighted Hsp90 as an attractive therapeutic target for the treatment of CRPC. We recently reported the development of a MYC-CaP castrate resistant (MYC-CaP/CR) transplant tumor model, which expresses amplified wild type AR. Within, we report that a second generation Hsp90 inhibitor, NVP-AUY922, inhibits cell growth and significantly induces cell death in MYC-CaP/CR and Pten-CaP/cE2 cell lines. NVP-AUY922 induced proteasome degradation of AR, though interestingly does not require loss of AR protein to inhibit AR transcriptional activity. Further, NVP-AUY922 increased docetaxel toxicity in MYC-CaP/CR and Pten-CaP/cE2 cell lines in vitro. Finally, NVP-AUY922/docetaxel combination therapy in mice bearing MYC-CaP/CR tumors resulted in greater anti-tumor activity compared to single treatment. This study demonstrates that NVP-AUY922 elicits potent activity towards AR signaling and augments chemotherapy response in a mouse model of CRPC, providing rationale for the continued clinical development of Hsp90 inhibitors in clinical trials for treatment of CRPC patients.

摘要

去势抵抗性前列腺癌(CRPC)患者的一线治疗主要包括多西他赛化疗。不幸的是,对多西他赛治疗产生耐药是最终会发生的情况。雄激素受体(AR)表达和信号传导的改变是CRPC中多西他赛治疗耐药的相关机制。热休克蛋白90(Hsp90)是一种分子伴侣,可调节参与前列腺癌的关键信号蛋白(包括AR)的激活、成熟和稳定性。这一认识以及化合物设计与开发方面的最新进展凸显了Hsp90作为治疗CRPC的有吸引力的治疗靶点。我们最近报道了一种表达扩增野生型AR的MYC-CaP去势抵抗性(MYC-CaP/CR)移植瘤模型的建立。在此,我们报告第二代Hsp90抑制剂NVP-AUY922可抑制MYC-CaP/CR和Pten-CaP/cE2细胞系的细胞生长并显著诱导细胞死亡。NVP-AUY922诱导AR的蛋白酶体降解,不过有趣的是,抑制AR转录活性并不需要AR蛋白缺失。此外,NVP-AUY922在体外增加了MYC-CaP/CR和Pten-CaP/cE2细胞系对多西他赛的敏感性。最后,在携带MYC-CaP/CR肿瘤的小鼠中,NVP-AUY922/多西他赛联合治疗与单一治疗相比具有更强的抗肿瘤活性。本研究表明,NVP-AUY922在CRPC小鼠模型中对AR信号传导具有强大作用并增强化疗反应,为Hsp90抑制剂在CRPC患者临床试验中的持续临床开发提供了理论依据。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/843d/4114978/19b12aa8dc05/pone.0103680.g001.jpg

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