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Nuclear receptor coactivators as potentialtherapeutical targets: the HATs on the mouse trap

机译:核受体共激活剂作为潜在的治疗靶点:捕鼠器上的HAT

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The recent past has seen an immense burst in our understanding of nuclear receptor (NR) signaling. Key achievements have been the structure determination of the ligand binding domain and the identification of coregulators which mediate the transcriptional effects of NRs. Both types of studies have now converged on the description of the NR coactivator interface at the atomic level, which, together with the elucidation of the structure of two coactivator related histone acetyl transferases (HATs) points towards previously unknown targets for drug design potentially leading to novel types of non-ligand antagonists of NR function.
机译:最近的过去在我们对核受体(NR)信号的理解中看到了巨大的爆发。关键成就是配体结合域的结构确定和介导NRs转录作用的共调节剂的鉴定。这两种类型的研究现在都集中在原子水平上的NR共激活因子界面的描述上,再加上对两种共激活因子相关的组蛋白乙酰转移酶(HATs)结构的阐明,它们指向了以前未知的药物设计目标,可能导致新型的NR功能非配体拮抗剂。

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