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使蛋白质相互作用成为可药物作用靶点:靶向PDZ结构域。

Making protein interactions druggable: targeting PDZ domains.

作者信息

Dev Kumlesh K

机构信息

Neuroscience Research, Novartis Institutes for BioMedical Research, Novartis Pharma AG, WSJ-386.7.43, CH-4002 Basel, Switzerland.

出版信息

Nat Rev Drug Discov. 2004 Dec;3(12):1047-56. doi: 10.1038/nrd1578.

Abstract

Modulating protein-protein interactions involved in disease pathways is an attractive strategy for developing drugs, but remains a challenge to achieve. One approach is to target certain domains within proteins that mediate these interactions. One example of such a domain is the PDZ domain, which is involved in interactions between many different proteins in a variety of cellular contexts. Because PDZ domains have well-defined binding sites, they are promising targets for drug discovery. However, there is still much to learn about the function of these domains before drugs targeting PDZ interactions can become a reality.

摘要

调节参与疾病通路的蛋白质-蛋白质相互作用是开发药物的一种有吸引力的策略,但要实现这一目标仍然是一项挑战。一种方法是针对蛋白质中介导这些相互作用的特定结构域。这种结构域的一个例子是PDZ结构域,它在多种细胞环境中参与许多不同蛋白质之间的相互作用。由于PDZ结构域具有明确的结合位点,它们是药物发现的有希望的靶点。然而,在针对PDZ相互作用的药物成为现实之前,关于这些结构域的功能仍有许多需要了解的地方。

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