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

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

  • Medchemcomm. 2016 Oct 19;8(1):21-52. doi: 10.1039/c6md00432f.
Anthony R Martin 1 Cyril Ronco 1 Luc Demange 1 2 3 Rachid Benhida 1
Affiliations

Affiliations

  • 1 Université Côte d'Azur , CNRS , Institut de Chimie de Nice UMR 7272 - 06108 Nice , France . Email: luc.demange@unice.fr ; Email: rachid.benhida@unice.fr ; ; Tel: +33 4 92076143.
  • 2 UFR des Sciences Pharmaceutiques , Université Paris Descartes , Sorbonne Paris Cité , 4 avenue de l'Observatoire , Paris Fr-75006 , France.
  • 3 UFR Biomédicale des Saints Pères , 45 rue des Saints Pères , Paris Fr-75006 , France.
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.

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