HSP90 inhibitors as therapy for multiple myeloma.
HSP90 inhibitors as therapy for multiple myeloma.
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DOI：
10.1016/j.clml.2011.03.027
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发表时间：
2011-06-01
期刊：
影响因子：
--
通讯作者：
Chiosis, Gabriela
中科院分区：
文献类型：
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作者：
Usmani, Saad Z;Chiosis, Gabriela
热休克蛋白90 （HSP90）蛋白家族是普遍存在的分子伴侣蛋白，它复杂地参与了许多蛋白质的折叠、激活、成熟和组装，这些蛋白质包括信号转导和细胞周期进程的必需介质。它们在真核细胞中含量丰富，正常情况下定位于细胞质、线粒体和内质网，占细胞蛋白质总量的1% ~ 2%。HSP90蛋白在包括多发性骨髓瘤在内的许多恶性肿瘤中表达增加。抑制HSP90可以影响骨髓瘤中涉及的多种致癌途径和蛋白质，因此使其成为该疾病药物开发的一个有吸引力的靶点。本文概述了HSP90抑制剂治疗多发性骨髓瘤的临床前数据和临床试验数据。
The heat shock protein 90 (HSP90) family of proteins are ubiquitous molecular chaperones that are intricately involved in folding, activation, maturation, and assembly of many proteins that include essential mediators of signal transduction and cell cycle progression. They are abundant in eukaryotic cells and localized to the cytoplasm and mitochondria as well as the endoplasmic reticulum under normal conditions, making up 1% to 2% of all cellular proteins. HSP90 proteins have increased expression in a number of malignancies, including multiple myeloma. HSP90 inhibition can influence multiple oncogenic pathways and proteins involved in myeloma, therefore making it an attractive target for drug development in this disease. This article serves as an overview of the pre-clinical data and clinical trial data on HSP90 inhibitors in multiple myeloma.