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COH34 是一种有效且特异性的聚 (ADP-核糖) 糖水解酶 (PARG) 抑制剂,IC50为 0.37 nM。COH34 与 PARG 的催化结构域 (Kd= 0.547 μM) 结合,从而延长了 DNA 损伤处的 PARylation 并捕获了 DNA 修复因子。
COH34 is a potent and specific poly(ADP-ribose) glycohydrolase (PARG) inhibitor with an IC50 of 0.37 nM. COH34 binds to the catalytic domain of PARG (Kd=0.547 μM), thereby prolonging PARylation at DNA lesions and trapping DNA repair factors[1].
[1]. Chen SH, et al. Targeting dePARylation selectively suppresses DNA repair-defective and PARP inhibitor-resistant malignancies. Sci Adv. 2019 Apr 10;5(4):eaav4340.
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