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Updated: Mar 6, 2026

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发现了临床候选者IAG933,一个强大的YAP-TEAD PPI破坏者

Markus Vögtle¹, Holger Sellner¹, Emilie Chapeau¹

¹Novartis BioMedical Research, 4002 Basel, Switzerland.

Journal of medicinal chemistry

|March 4, 2026

概括

研究人员开发了IAG933,它是一种强大的抑制剂,向TEAD-YAP蛋白相互作用,对癌症生长至关重要. 这种候选药物显示出作为一种新的癌症治疗方法临床评估的前景.

科学领域:

在瘤学瘤学.
药用化学医学化学
分子生物学分子生物学

背景情况:

河马信号通路调节器官大小和细胞增殖.
河马通路的失调导致转录增强关联域 (TEAD) 和是关联蛋白 (YAP) 综合体的异常激活.
这种TEAD-YAP相互作用在各种癌症中驱动瘤功能.

研究的目的:

为了识别和开发TEAD-YAP蛋白质-蛋白质相互作用的强有力的抑制剂.
为了发现一种具有有利临床开发特性的小分子.
为由河马通路驱动的癌症提供潜在的新疗法策略.

主要方法:

药用化学优化程序. 药用化学优化程序.
基于结构的药物设计原则.
在体外和体内临床前评估 (暗示ADME概况和临床评估).

主要成果:

发现IAG933,一种新的小分子抑制剂.
IAG933有效地抑制了TEAD-YAP的相互作用.
IAG933具有平衡的吸收,分布,新陈代谢和分泌 (ADME) 概况.

结论:

IAG933是针对TEAD-YAP驱动癌症的一种有前途的候选药物.
均衡的ADME概况支持其临床评估的潜力.
这一发现为癌症治疗提供了一条新的途径,通过抑制一个关键的致癌途径.

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