Jump to main content
Jump to site search

Issue 1, 2017
Previous Article Next Article

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

Author affiliations

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

Back to tab navigation
Please wait while Download options loads

Publication details

The article was received on 29 Jul 2016, accepted on 10 Oct 2016 and first published on 19 Oct 2016


Article type: Review Article
DOI: 10.1039/C6MD00432F
Citation: Med. Chem. Commun., 2017,8, 21-52
  •   Request permissions

    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

Search articles by author