A Novel PARP Inhibitor YHP-836 For the Treatment of BRCA-Deficiency Cancers.
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SUBMITTER: Du T
PROVIDER: S-EPMC9326368 | biostudies-literature | 2022
REPOSITORIES: biostudies-literature
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A Novel PARP Inhibitor YHP-836 For the Treatment of BRCA-Deficiency Cancers.
Du Tingting T Zhang Zhihui Z Zhou Jie J Sheng Li L Yao Haiping H Ji Ming M Xu Bailing B Chen Xiaoguang X
Frontiers in pharmacology 20220713
PARP inhibitors have clinically demonstrated good antitumor activity in patients with BRCA mutations. Here, we described YHP-836, a novel PARP inhibitor, YHP-836 demonstrated excellent inhibitory activity for both PARP1 and PARP2 enzymes. It also allosterically regulated PARP1 and PARP2 via DNA trapping. YHP-836 showed cytotoxicity in tumor cell lines with BRCA mutations and induced cell cycle arrest in the G2/M phase. YHP-836 also sensitized tumor cells to chemotherapy agents <i>in vitro</i>. O ...[more]
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