Inhibiting protein-protein interactions with small drug-like molecules is extremely challenging. We report here a breakthrough regarding the YAP-TEAD interaction. The potency of a weakly active virtual screening hit was increased by five orders of magnitude by structure-based design, providing the first class of small molecules able to efficiently disrupt the YAP-TEAD interaction, an important target in oncology.

中文翻译：

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第一类通过直接竞争有效破坏 YAP-TEAD 相互作用的小分子

抑制蛋白质与药物样小分子的相互作用极具挑战性。我们在此报告有关 YAP-TEAD 交互的突破。通过基于结构的设计，弱活性虚拟筛选命中的效力提高了五个数量级，提供了第一类能够有效破坏 YAP-TEAD 相互作用的小分子，这是肿瘤学的一个重要目标。