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The ATPases: a new family for a family-based drug design approach.

机译:ATPases:基于家族药物设计方法的新家族。

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摘要

The rapid discovery of new drugs is greatly facilitated when a family of related proteins is targeted with a similar approach in chemistry. Few protein families have so far been investigated using this kind of 'family-based' approach. Therefore, to increase the size of our Pharmacopeia and to cure human diseases more efficiently, new druggable protein families must be identified. It is shown in this review that ATPases are very good candidates for a family-based approach. The human proteome contains many ATPases, which are involved in several diseases. All the ATPases contain a nucleotide-binding site, and it is therefore possible to target all of them with a single strategy in chemistry; the design of competitive ATP inhibitors. Moreover, because a similar approach has been conducted with the protein kinases, the compound libraries and the knowledge developed in the kinase field can be directly applied to the ATPases.
机译:当以化学上的类似方法靶向相关蛋白家族时,极大地促进了新药的快速发现。到目前为止,很少有蛋白质家族使用这种“基于家族”的方法进行研究。因此,为了增加我们的药典的规模并更有效地治疗人类疾病,必须确定新的可药物化蛋白家族。该评价表明,ATP酶是基于家庭的方法的非常好的候选者。人类蛋白质组包含许多ATPase,与多种疾病有关。所有的ATPase都含有一个核苷酸结合位点,因此可以通过化学上的单一策略将它们全部靶向。竞争性ATP抑制剂的设计。此外,由于已经对蛋白激酶进行了类似的研究,因此化合物文库和在激酶领域发展起来的知识可以直接应用于ATPase。

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