Targeting Wnt-driven cancers: Discovery of novel tankyrase inhibitors

Martina Ferri, Paride Liscio, Andrea Carotti, Stefania Asciutti, Roccaldo Sardella, Antonio Macchiarulo, Emidio Camaioni

Research output: Contribution to journalReview articlepeer-review

48 Scopus citations


Recent years have seen substantially heightened interest in the discovery of tankyrase inhibitors (TNKSi) as new promising anticancer agents. In this framework, the aim of this review article is focused on the description of potent TNKSi also endowed with disruptor activity toward the Wnt/β-catenin signaling pathway. Beginning with an overview of the most characterized TNKSi deriving from several drug design approaches and classifying them on the basis of the molecular interactions with the target, we discuss only those ones acting against Wnt cancer cell lines. In addition, comprehensive structure property relationships (SPR) emerging from the hit evolution processes and preclinical results are provided. We then review the most promising TNKSi hitherto reported in literature, acting in vivo models of Wnt-driven cancers. Some outlooks on current issues and future directions in this field are also discussed.

Original languageEnglish
Pages (from-to)506-522
Number of pages17
JournalEuropean Journal of Medicinal Chemistry
StatePublished - 15 Dec 2017


  • PARP family
  • Tankyrase inhibitors
  • Wnt pathway disruption
  • Wnt-driven cancers
  • Wnt/β-catenin signaling pathway


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