PARP - 百度百科
PARP，即poly (ADP- ribose) polymerase，是定位在 细胞核 内，和应激条件下 DNA修复 密切相关的一种酶。 PARP在体外可以被多种Caspase剪切，在体内是Caspase 3的主要剪切对象。 对于人PARP，在Asp124和Gly215之间被Caspase剪切后，使PARP 羧基端 的催化 结构域 (89kD)和氨基端的sb DNA结合结构域 (24kD) 相分离，从而使PARP失去其 酶活力。 PARP对于细胞的稳定和存活非常重要，PARP失去酶活力会加速细胞的不稳定。 PARP (poly ADP-ribose …
Poly (ADP-ribose) polymerase - Wikipedia
Poly (ADP-ribose) polymerase (PARP) is a family of proteins involved in a number of cellular processes such as DNA repair, genomic stability, and programmed cell death. [1] The PARP family comprises 17 members (10 putative). [2] . They vary greatly in …
What are PARP inhibitors? - MD Anderson Cancer Center
2024年4月3日 · PARP inhibitors are a type of targeted therapy commonly used to treat breast cancer and ovarian cancer, among others. They target PARP, or poly (ADP-ribose) polymerase, which is a protein in cells that helps repair damaged DNA.
《Science》癌症特刊：PARP抑制剂深度盘点-上海交大医学院图书馆
PARP抑制剂是一种靶向聚ADP核糖聚合酶 (Poly ADP-ribose Polymerase) 的癌症疗法。 它是第一种成功利用合成致死 (Synthetic Lethality) 概念获得批准在临床使用的抗癌药物。 它的原理不难理解：携带BRCA1或BRCA2种系基因突变 (germline...
PARP Inhibitors: Clinical Relevance, Mechanisms of Action and …
2020年9月9日 · PARP inhibitors (PARPi) were the first approved cancer drugs that specifically targeted the DNA damage response in BRCA1/2 mutated breast and ovarian cancers. Since then, there has been significant advances in our understanding of the mechanisms behind sensitization of tumors to PARP inhibitors and expansion of the use of PARPi to treat several ...
The Potential of PARP Inhibitors as Antitumor Drugs and the …
2 天之前 · PARP (poly-ADP ribose polymerase) has received widespread attention in cancer treatment. Research has shown that PARP plays a crucial role in DNA damage repair and has become a popular target for drug design. Based on the mechanism of “synthetic lethality”, multiple PARPis (PARP inhibitors) have been launched for the treatment of BRCA deficient tumors. For example, the approved PARPis have ...
Poly (ADP-ribose) polymerase (PARP) inhibitors as ... - ScienceDirect
2024年8月5日 · Poly (ADP-ribose) polymerase (PARP) is considered an essential component in case of DNA (Deoxyribonucleic acid) damage, response by sensing DNA damage and engaging DNA repair proteins. Those proteins repair the damaged DNA via an aspect of posttranslational modification, known as poly (ADP-Ribosyl)ation (PARylation).
Poly(ADP-ribose) polymerase inhibition: past, present and future
2020年9月3日 · This Review provides a timeline of PARP biology and medicinal chemistry, summarizes the pathophysiological processes in which PARP plays a role and highlights key opportunities and challenges...
The complex universe of inactive PARP1: Trends in Genetics - Cell …
2024年9月20日 · Poly(ADP-ribose) polymerase 1 (PARP1) is a crucial member of the PARP family, which modifies targets through ADP-ribosylation and plays key roles in a variety of biological processes. PARP inhibitors (PARPis) hinder ADP-ribosylation and lead to the retention of PARP1 at the DNA lesion (also known as trapping), which underlies their toxicity.
Minimizing DNA trapping while maintaining activity inhibition via ...
2024年12月18日 · Poly ADP-ribose polymerase 1 (PARP1) plays a pivotal role in DNA repair [1,2,3].Upon detection of DNA damage, PARP1 binds to the site of DNA breakage and catalyzes the decomposition of ...