WNT/β-catenin signaling orchestrates various physiological processes, including embryonic development, growth, tissue homeostasis, and regeneration. Abnormal WNT/β-catenin signaling is associated with various cancers and its inhibition has shown effective antitumor responses. In this review, we discuss the pathway, potential targets for the development of WNT/β-catenin inhibitors, available inhibitors, and their specific molecular interactions with the target proteins. We also discuss inhibitors that are in clinical trials and describe potential new avenues for therapeutically targeting the WNT/β-catenin pathway. Furthermore, we introduce emerging strategies, including artificial intelligence (AI)-assisted tools and technology-based actionable approaches, to translate WNT/β-catenin inhibitors to the clinic for cancer therapy.

WNT/β-连环蛋白信号协调各种生理过程，包括胚胎发育、生长、组织稳态和再生。异常的 WNT/β-catenin 信号传导与多种癌症相关，其抑制已显示出有效的抗肿瘤反应。在这篇综述中，我们讨论了开发 WNT/β-连环蛋白抑制剂的途径、潜在靶点、可用的抑制剂以及它们与靶蛋白的特定分子相互作用。我们还讨论了临床试验中的抑制剂，并描述了治疗靶向 WNT/β-连环蛋白途径的潜在新途径。此外，我们引入了新兴策略，包括人工智能 (AI) 辅助工具和基于技术的可行方法，将 WNT/β-连环蛋白抑制剂转化为临床用于癌症治疗。