摘要
多聚(ADP-核糖)聚合酶1(PARP1)的抑制剂增加了化疗的敏感性,同时授予同源重组细胞单独的的抑制细胞增殖的能力,提供了一个抗癌治疗干预的独特机会。因此,PARP1,PARP家族中最主要的酶,由于其DNA修复的紧密作用,对于肿瘤的治疗是目前一个行之有效的目标。当前,不断的药物化学努力已发现了12 PARP1抑制剂,并提前进入了临床试验。在这篇文章中,我们基于化学结构包括内酰胺型,伪环型和非典型PARP1抑制剂三大类,对于这些候选品写一个序列性的概述。特别是,一些候选品将发展成为PARP1抑制剂未来勘探的目的。
关键词: 抗癌;临床试验;PARP1抑制剂;PARPs;构效关系(SAR)。
Current Medicinal Chemistry
Title:PARP1: A Promising Target for the Development of PARP1-based Candidates for Anticancer Intervention
Volume: 23 Issue: 17
Author(s): Xiaolei Zhu, Xiaodong Ma, Yongzhou Hu
Affiliation:
关键词: 抗癌;临床试验;PARP1抑制剂;PARPs;构效关系(SAR)。
摘要: Poly(ADP-ribose) polymerase 1 (PARP1) inhibition, increasing chemosensitization and conferring independent antiproliferation against defective homologous recombination cells, has provided a unique opportunity for anticancer therapeutic intervention. Therefore, PARP1, the best characterized enzyme among PARP family, is presently serving as a well-established target for the treatment of oncology attributed to its intimate role in DNA repair. Nowadays, intensified medicinal chemistry efforts have led to the discovery of 12 PARP1 inhibitors that have been advanced into clinical trial. In this article, we classify these candidates as three categories based on the chemical structure, including lactam type, pseudo ring type and untypical PARP1 inhibitors, for a sequential overview of them. In particular, the development of some candidates will serve the purpose for the future exploration of PARP1 inhibitors.
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Cite this article as:
Xiaolei Zhu, Xiaodong Ma, Yongzhou Hu , PARP1: A Promising Target for the Development of PARP1-based Candidates for Anticancer Intervention, Current Medicinal Chemistry 2016; 23 (17) . https://dx.doi.org/10.2174/0929867321666140915143516
DOI https://dx.doi.org/10.2174/0929867321666140915143516 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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