ARV-825

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ARV-825 是一种 PROTAC 类的 BRD4 降解剂。ARV-825 对 BRD4 的 BD1 和 BD2 结构域具有高亲和力,Kd 值分别为 90 和 28 nM。

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描述

ARV-825 is a hetero-bifunctional proteolysis-targeting chimera (PROTAC) that recruits BRD4 to the E3 ubiquitin ligase cereblon. ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of the former via the proteasome. Given that BRD4 and cereblon binding moieties in ARV-825 have Kds of 28-90 nM and ~3 µM to their respective targets, this suggests that ARV-825 acts in a substoichiometric way in mediating BRD4 degradation. ARV-825 treatment results in prolonged BRD4 down-regulation and downstream signaling suppression compared to BRD4 inhibitors[1].

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