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Eur J Med Chem. 2017 Dec 15;142:506-522. doi: 10.1016/j.ejmech.2017.09.030. Epub 2017 Oct 7.

Targeting Wnt-driven cancers: Discovery of novel tankyrase inhibitors.

Author information

1
Department of Pharmaceutical Sciences, University of Perugia, Via del Liceo 1, 06123 Perugia, Italy.
2
TES Pharma, Via P. Togliatti 22bis, 06073 Terrioli, Corciano, Italy.
3
Icahn School of Medicine at Mount Sinai, Department of Oncological Sciences, 1425 Madison Ave, New York, NY 10029 USA.
4
Department of Pharmaceutical Sciences, University of Perugia, Via del Liceo 1, 06123 Perugia, Italy. Electronic address: emidio.camaioni@unipg.it.

Abstract

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.

KEYWORDS:

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

PMID:
29107427
DOI:
10.1016/j.ejmech.2017.09.030
[Indexed for MEDLINE]

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