摘要
油漆酶属于称为聚ADP核糖基聚合酶(PARP)的一组酶。随着新一代PARP的小分子抑制剂临床使用,如OLAPARIB;被USFDA加速批准用于治疗卵巢癌和乳腺癌,PARP作为各种疾病条件下的新靶标的视野已经上升。阻聚酶(PARP 5)是另一类PARP,其在不同的底物蛋白上进行多聚ADP核糖基化,有助于癌症,纤维化,糖尿病和神经障碍等许多疾病的进展。由于表面过表达,端粒重复结合因子蛋白(TRF1),轴抑制蛋白(AXIN 1&2),胰岛素反应性氨基肽酶(IRAP),核有丝分裂装置蛋白(NuMa)在超增殖疾病状况下的酶,如癌症,纤维化和代谢性疾病如糖尿病。槽状酶通过影响Wnt信号通路介入许多生理过程,如细胞生长和存活。另一方面,这些功能在癌症和纤维化过程中尤为突出。癌症新型疗法的发展是与目前的抗癌药物如耐药性和毒性发展相关的若干问题的一个永无止境的过程。纤维化疾病如肺纤维化是一种衰弱病症,治疗选择和存活率有限。因此,特异性小分子抑制剂的阻滞酶抑制剂可以成为治疗高增殖性疾病和糖尿病的良好组合或单一治疗策略。鉴于所有这些问题,本文旨在简要介绍卡诺酶的作用及其抑制作用,以克服目前治疗方案所面临的障碍。
关键词: PARP,卡诺酶,癌症,纤维化,糖尿病,神经系统疾病,新型分子靶点。
Current Drug Targets
Title:Tankyrase as a Novel Molecular Target in Cancer and Fibrotic Diseases
Volume: 18 Issue: 10
关键词: PARP,卡诺酶,癌症,纤维化,糖尿病,神经系统疾病,新型分子靶点。
摘要: Tankyrases belong to a group of enzymes called poly ADP ribosyl polymerases (PARPs). With the advent of a new class of small molecule inhibitors of PARP for clinical use like OLAPARIB; that gained accelerated approval by the USFDA in treating ovarian and breast cancers, the horizons of the PARPs as a novel target in various disease conditions has risen. Tankyrases (PARP 5) are yet another class of PARPs that perform poly ADP ribosylation on different substrate proteins aiding in progression of many diseases like cancer, fibrosis, diabetes and neurological disorders even. Few of the substrates of Tankyrases are Telomeric Repeat binding Factor protein (TRF1), Axis Inhibitory protein (AXIN 1&2), Insulin Responsive Amino Peptidase (IRAP), Nuclear Mitotic Apparatus protein (NuMa), that become aberrantly active due to the apparent overexpression of the enzyme during hyper proliferative disease conditions like cancer, fibrosis and metabolic disorders like diabetes. Tankyrases intervene in many physiological processes like cell growth and survival by affecting the Wnt signaling pathways. On the other hand, these functions are overdone during cancer and fibrosis especially. The development of novel therapies for cancer is a never ending process pertaining to several issues associated with current anticancer drugs like development of drug resistance and toxicity. A fibrotic disease like lung fibrosis is a debilitating condition with limited treatment options and survival rate. Tankyrase inhibition by specific small molecule inhibitors can therefore become a good combinatorial or single treatment strategy in treating hyper proliferative diseases and diabetes. In light of all these concerns, this article aims to brief the role of Tankyrase and the relevance of its inhibition to overcome the hurdles faced by current treatment regimens.
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Tankyrase as a Novel Molecular Target in Cancer and Fibrotic Diseases, Current Drug Targets 2017; 18 (10) . https://dx.doi.org/10.2174/1389450117666160715152503
DOI https://dx.doi.org/10.2174/1389450117666160715152503 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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