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Antitumor activity of a novel PARP1/2 inhibitor YHP-743
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Ming JI, Hai-ping YAO, Jie ZHOU, Jing JIN, Li-yuan WANG, Fang-fang LAI, Ni-na XUE, Bai-ling XU, Xiao-guang CHEN*
Acta Pharmaceutica Sinica | 2018, 53(6) : 938 - 943
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Acta Pharmaceutica Sinica | 2018, 53(6): 938-943
• Medicinal Chemistry Pharmacology •
Antitumor activity of a novel PARP1/2 inhibitor YHP-743
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Ming JI, Hai-ping YAO, Jie ZHOU, Jing JIN, Li-yuan WANG, Fang-fang LAI, Ni-na XUE, Bai-ling XU, Xiao-guang CHEN*
Affiliations
  • State Key Laboratory of Bioactive Substances and Functions of Natural Medicines/Beijing Key Laboratory of Non-Clinical Drug Metabolism and PK/PD Study, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, China
Published: 2018-06-12 doi: 10.16438/j.0513-4870.2018-0247
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Poly(ADP-ribose) polymerase (PARP)-1 and PARP2 function as ADP-ribosylases involved in DNA repair. PARP1/2 is highly expressed in cancers and emerged as an attractive target for antitumor drug. In this study, we investigated the antitumor activity of a novel PARP1/2 inhibitor YHP-743 in vitro and in vivo. The results showed that YHP-743 had potent enzymatic inhibitory activity against PARP1 and PARP2 to down-regulate the PAR level. YHP-743 not only inhibited breast cancer cells with genes deficiency of homologous recombination repair, but also potentiated chemotherapy agent's cytotoxicity, such as temozolomide, topotecan, cisplatin and doxorubicin. YHP-743 elicited good antitumor activity in combination with temo-zolomide in vivo.

poly (ADP-ribose) polymerase-1  /  poly (ADP-ribose) polymerase-2  /  DNA repair  /  antitumor activity  /  inhibitor
Ming JI, Hai-ping YAO, Jie ZHOU, Jing JIN, Li-yuan WANG, Fang-fang LAI, Ni-na XUE, Bai-ling XU, Xiao-guang CHEN. Antitumor activity of a novel PARP1/2 inhibitor YHP-743[J]. Acta Pharmaceutica Sinica, 2018 , 53 (6) : 938 -943 . DOI: 10.16438/j.0513-4870.2018-0247
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Article Info
doi: 10.16438/j.0513-4870.2018-0247
  • Receive Date：2018-03-21
  • Online Date：2026-01-15
  • Published：2018-06-12
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History
  • Received：2018-03-21
  • Revised：2018-04-08
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    State Key Laboratory of Bioactive Substances and Functions of Natural Medicines/Beijing Key Laboratory of Non-Clinical Drug Metabolism and PK/PD Study, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, China
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小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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