Issue 1, 2017

Hypoxia inducible factor down-regulation, cancer and cancer stem cells (CSCs): ongoing success stories

Abstract

In cancers, hypoxia inducible factor 1 (HIF-1) is an over-expressed transcription factor, which regulates a large set of genes involved in tumour vascularization, metastases, and cancer stem cells (CSCs) formation and self-renewal. This protein has been identified as a relevant target in oncology and several HIF-1 modulators are now marketed or in advanced clinical trials. The purpose of this review is to summarize the advances in the understanding of its regulation and its inhibition, from the medicinal chemist point of view. To this end, we selected in the recent literature relevant examples of “hit” compounds, including small-sized organic molecules, pseudopeptides and nano-drugs, exhibiting in vitro and/or in vivo both anti-HIF-1 and anti-tumour activities. Whenever possible, a particular emphasis has been dedicated to compounds that selectively target CSCs.

Graphical abstract: Hypoxia inducible factor down-regulation, cancer and cancer stem cells (CSCs): ongoing success stories

Article information

Article type
Review Article
Submitted
29 Jul 2016
Accepted
10 Oct 2016
First published
19 Oct 2016

Med. Chem. Commun., 2017,8, 21-52

Hypoxia inducible factor down-regulation, cancer and cancer stem cells (CSCs): ongoing success stories

A. R. Martin, C. Ronco, L. Demange and R. Benhida, Med. Chem. Commun., 2017, 8, 21 DOI: 10.1039/C6MD00432F

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