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Peptide and Peptide-Like Modulators of 20S Proteasome Enzymatic Activity in Cancer Cells.
International Journal of Peptide Research and Therapeutics ( IF 2.5 ) Pub Date : 2006-03-04 , DOI: 10.1007/s10989-005-9001-4
Carlos García-Echeverría

The involvement of the ubiquitin-proteasome pathway in the degradation of critical intracellular regulatory proteins suggested a few years ago the potential use of proteasome inhibitors as novel therapeutic agents being applicable in many different disease indications, and in particular for cancer therapy. This article reviews recent salient medicinal chemistry achievements in the design, synthesis, and biological characterization of both synthetic and natural peptide-like proteasome inhibitors, updating recent reviews on this class of agents. As shown herein, different compound classes are capable of modulating the subunit-specific proteolytic activities of the 20S proteasome in ways not previously possible, and one of them, bortezomib, has provided proof-of-concept for this therapeutic approach in cancer clinical settings.

中文翻译:

癌细胞中 20S 蛋白酶体酶活性的肽和肽样调节剂。

几年前泛素-蛋白酶体途径参与关键细胞内调节蛋白的降解表明,蛋白酶体抑制剂作为新型治疗剂的潜在用途可应用于许多不同的疾病适应症,尤其是癌症治疗。本文回顾了最近在合成和天然肽样蛋白酶体抑制剂的设计、合成和生物学特性方面取得的突出药物化学成就,更新了对此类药物的最新评论。如本文所示,不同的化合物类别能够以以前不可能的方式调节 20S 蛋白酶体的亚基特异性蛋白水解活性,其中之一,硼替佐米,为癌症临床环境中的这种治疗方法提供了概念验证。
更新日期:2019-11-01
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