PARP1: A Promising Target for the Development of PARP1-based Candidates for Anticancer Intervention

Author(s): Xiaolei Zhu, Xiaodong Ma, Yongzhou Hu

Journal Name: Current Medicinal Chemistry

Volume 23 , Issue 17 , 2016

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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.

Keywords: Anticancer, clinical trial, PARP1 inhibitors, PARPs, structure-activity relationship (SAR).

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Article Details

Year: 2016
Published on: 02 June, 2016
Page: [1756 - 1774]
Pages: 19
DOI: 10.2174/0929867321666140915143516
Price: $65

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