The School of Pharmacy, University of London, 29-39 Brunswick Square, London, UK.
Future Med Chem. 2009 Apr;1(1):65-93. doi: 10.4155/fmc.09.12.
Over the last two decades, an increasing research effort in academia and industry has focused on the modulation (both inhibition and stabilization) of protein-protein interactions (PPIs) in order to develop novel therapeutic approaches and target-selective agents in drug discovery.
The diversity and complexity of highly dynamic systems such as PPIs present many challenges for the identification of drug-like molecules with the ability to modulate the PPI with the necessary selectivity and potency. In this review, a number of these strategies will be presented along with a critical overview of the challenges and potential solutions relating to the exploitation of PPIs as molecular targets.
Both traditional drug discovery approaches and some more recently developed innovative strategies have already provided valuable tools for the discovery of PPI modulators, and a number of successful examples have highlighted the potential of targeting PPIs for therapeutic intervention, especially in the oncology area.
在过去的二十年中，学术界和工业界越来越重视蛋白质-蛋白质相互作用（PPIs）的调节（包括抑制和稳定），以开发新的治疗方法和药物发现中的靶标选择性试剂。
像 PPIs 这样高度动态系统的多样性和复杂性给具有调节 PPI 的能力的药物样分子的鉴定带来了许多挑战，这种调节需要必要的选择性和效力。在这篇综述中，将介绍其中一些策略，并对利用 PPIs 作为分子靶标所涉及的挑战和潜在解决方案进行批判性概述。
传统的药物发现方法和一些最近开发的创新策略已经为 PPI 调节剂的发现提供了有价值的工具，许多成功的例子突出了针对 PPIs 进行治疗干预的潜力，特别是在肿瘤学领域。
