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Int. J. Mol. Sci. 2017, 18(10), 2111;

PARP1 in Carcinomas and PARP1 Inhibitors as Antineoplastic Drugs

1,2,3,4,* and 1,2,3,4,*
Law Sau Fai Institute for Advancing Translational Medicine in Bone and Joint Diseases, School of Chinese Medicine, Hong Kong Baptist University, Hong Kong, China
Institute of Integrated Bioinfomedicine and Translational Science, School of Chinese Medicine, Hong Kong Baptist University, Hong Kong, China
Institute of Precision Medicine and Innovative Drug Discovery, School of Chinese Medicine, Hong Kong Baptist University, Hong Kong, China
Shenzhen Lab of Combinatorial Compounds and Targeted Drug Delivery, HKBU Institute of Research and Continuing Education, Shenzhen 518000, China
These authors contributed equally to this work.
Authors to whom correspondence should be addressed.
Received: 14 September 2017 / Revised: 30 September 2017 / Accepted: 2 October 2017 / Published: 8 October 2017
(This article belongs to the Section Biochemistry)
Full-Text   |   PDF [3211 KB, uploaded 12 October 2017]   |  


Poly (ADP-ribose) polymerase 1 (PARP1), the best-studied isoform of the nuclear enzyme PARP family, plays a pivotal role in cellular biological processes, such as DNA repair, gene transcription, and so on. PARP1 has been found to be overexpressed in various carcinomas. These all indicate the clinical potential of PARP1 as a therapeutic target of human malignancies. Additionally, multiple preclinical research studies and clinical trials demonstrate that inhibition of PARP1 can repress tumor growth and metastasis. Up until now, PARP1 inhibitors are clinically used not only for monotherapy to suppress various tumors, but also for adjuvant therapy, to maintain or enhance therapeutic effects of mature antineoplastic drugs, as well as protect patients from chemotherapy and surgery-induced injury. To supply a framework for understanding recent research progress of PARP1 in carcinomas, we review the structure, expression, functions, and mechanisms of PARP1, and summarize the clinically mature PARP1-related anticancer agents, to provide some ideas for the development of other promising PARP1 inhibitors in antineoplastic therapy. View Full-Text
Keywords: PARP1; carcinomas; PARP1 inhibitors PARP1; carcinomas; PARP1 inhibitors

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Wang, L.; Liang, C.; Li, F.; Guan, D.; Wu, X.; Fu, X.; Lu, A.; Zhang, G. PARP1 in Carcinomas and PARP1 Inhibitors as Antineoplastic Drugs. Int. J. Mol. Sci. 2017, 18, 2111.

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