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Development of Proteasome Inhibitors as Therapeutic Drugs.蛋白酶体抑制剂作为治疗药物的研发。
J Clin Cell Immunol. 2012 Mar 15;S5:5. doi: 10.4172/2155-9899.s5-005.
2
Proteasome inhibitors: a therapeutic strategy for haematological malignancy.蛋白酶体抑制剂：血液系统恶性肿瘤的一种治疗策略。
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Proteasome inhibitors in the treatment of B-cell malignancies.蛋白酶体抑制剂在B细胞恶性肿瘤治疗中的应用
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Targeting the proteasome in mantle cell lymphoma: a promising therapeutic approach.靶向套细胞淋巴瘤中的蛋白酶体：一种有前景的治疗方法。
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Proteasome inhibitors in cancer therapy.蛋白酶体抑制剂在癌症治疗中的应用。
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Emerging role of immunoproteasomes in pathophysiology.免疫蛋白酶体在病理生理学中的新作用。
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本文引用的文献

1
Novel proteasome inhibitors to overcome bortezomib resistance.新型蛋白酶体抑制剂克服硼替佐米耐药性。
J Natl Cancer Inst. 2011 Jul 6;103(13):1007-17. doi: 10.1093/jnci/djr160. Epub 2011 May 23.
2
The involvement of SMILE/TMTC3 in endoplasmic reticulum stress response.SMILE/TMTC3 在内质网应激反应中的作用。
PLoS One. 2011;6(5):e19321. doi: 10.1371/journal.pone.0019321. Epub 2011 May 16.
3
Second generation proteasome inhibitors: carfilzomib and immunoproteasome-specific inhibitors (IPSIs).第二代蛋白酶体抑制剂：卡非佐米和免疫蛋白酶体特异性抑制剂（IPSIs）。
Curr Cancer Drug Targets. 2011 Mar;11(3):285-95. doi: 10.2174/156800911794519725.
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A novel dithiocarbamate analogue with potentially decreased ALDH inhibition has copper-dependent proteasome-inhibitory and apoptosis-inducing activity in human breast cancer cells.一种新型的二硫代氨基甲酸盐类似物，可能降低了 ALDH 抑制作用，在人乳腺癌细胞中具有铜依赖性蛋白酶体抑制和诱导细胞凋亡的活性。
Cancer Lett. 2011 Jan 1;300(1):87-95. doi: 10.1016/j.canlet.2010.09.010. Epub 2010 Oct 29.
5
Structure, assembly and homeostatic regulation of the 26S proteasome.26S 蛋白酶体的结构、组装和动态平衡调节。
J Mol Cell Biol. 2010 Dec;2(6):308-17. doi: 10.1093/jmcb/mjq030. Epub 2010 Oct 7.
6
Bortezomib sensitizes human esophageal squamous cell carcinoma cells to TRAIL-mediated apoptosis via activation of both extrinsic and intrinsic apoptosis pathways.硼替佐米通过激活外源性和内源性凋亡途径，使人类食管鳞癌细胞对 TRAIL 介导的凋亡敏感。
Mol Cancer Ther. 2010 Jun;9(6):1842-51. doi: 10.1158/1535-7163.MCT-09-0918. Epub 2010 Jun 1.
7
Bortezomib sensitizes human renal cell carcinomas to TRAIL apoptosis through increased activation of caspase-8 in the death-inducing signaling complex.硼替佐米通过增加死亡诱导信号复合物中 caspase-8 的激活，使人类肾细胞癌对 TRAIL 凋亡敏感。
Mol Cancer Res. 2010 May;8(5):729-38. doi: 10.1158/1541-7786.MCR-10-0022. Epub 2010 May 4.
8
Inhibition of the ubiquitin-proteasome system by natural products for cancer therapy.天然产物抑制泛素-蛋白酶体系统治疗癌症。
Planta Med. 2010 Aug;76(11):1064-74. doi: 10.1055/s-0029-1240901. Epub 2010 Feb 25.
9
Bortezomib induces autophagic death in proliferating human endothelial cells.硼替佐米诱导增殖的人内皮细胞发生自噬性死亡。
Exp Cell Res. 2010 Apr 1;316(6):1010-8. doi: 10.1016/j.yexcr.2009.11.005. Epub 2009 Nov 13.
10
Proteasome inhibitors activate autophagy as a cytoprotective response in human prostate cancer cells.蛋白酶体抑制剂通过诱导自噬作为一种细胞保护应答激活人前列腺癌细胞。
Oncogene. 2010 Jan 21;29(3):451-62. doi: 10.1038/onc.2009.343. Epub 2009 Nov 2.

蛋白酶体抑制剂作为治疗药物的研发。

Development of Proteasome Inhibitors as Therapeutic Drugs.

作者信息

Pellom Samuel Troy, Shanker Anil

机构信息

Laboratory of Lymphocyte Function, Department of Biochemistry and Cancer Biology, School of Medicine, Meharry Medical College, Nashville, TN 37208, USA ; School of Graduate Studies and Research, Meharry Medical College, Nashville, TN 37208, USA ; Department of Microbiology and Immunology, School of Medicine, Meharry Medical College, Nashville, TN 37208, USA.

出版信息

J Clin Cell Immunol. 2012 Mar 15;S5:5. doi: 10.4172/2155-9899.s5-005.

DOI:10.4172/2155-9899.s5-005
PMID:23338480
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3546515/
Abstract

The proteasome is a multi-unit enzyme complex found in the cytoplasm and nucleus of all eukaryotic cells and is responsible for degradation of unneeded or damaged intracellular proteins by proteolysis, a chemical reaction that breaks peptide bonds. Proteasome inhibition presents a promising approach to cancer therapy by targeting the proteasome function in tumor cells. Delineating the success of bortezomib in the treatment of multiple myeloma and mantle cell lymphoma, this review explores various proteasome inhibitors, currently in development, as molecular targeting agents in the fight against cancer. Proteasome inhibitors can be used alone or in combination with other conventional cancer therapies to sensitize tumor cells to cell death by various mechanisms and improve therapeutic benefits.

摘要

蛋白酶体是一种多亚基酶复合物，存在于所有真核细胞的细胞质和细胞核中，负责通过蛋白水解作用降解不需要的或受损的细胞内蛋白质，蛋白水解是一种断裂肽键的化学反应。通过靶向肿瘤细胞中的蛋白酶体功能，蛋白酶体抑制为癌症治疗提供了一种有前景的方法。鉴于硼替佐米在治疗多发性骨髓瘤和套细胞淋巴瘤方面的成功，本综述探讨了目前正在研发的各种蛋白酶体抑制剂，作为对抗癌症的分子靶向药物。蛋白酶体抑制剂可单独使用或与其他传统癌症疗法联合使用，通过多种机制使肿瘤细胞对细胞死亡敏感，并提高治疗效果。