Small molecules targeting HIF-1α pathway for cancer therapy in recent years

Bioorg Med Chem. 2020 Jan 15;28(2):115235. doi: 10.1016/j.bmc.2019.115235. Epub 2019 Nov 29.

Abstract

Hypoxia is a very important feature of tumors, especially for solid tumors, and it was demonstrated highly relevant with aggressive biology, including anti-apoptosis, vasculogenesis and radiation or chemotherapy resistance. Correlatively, hypoxia-inducible factors 1-α (HIF-1α), which the wildest contribution of hypoxia-inducible factors (HIFs), plays a crucial role in the adaptation of tumor cells to hypoxia via upregulating the transcription of the oncogene and downregulating the transcription of suppressor gene. This review focus on the HIF-1α regulation including hydroxylation and acetylation, growth factors pathway, heat shock proteins(HSPs), and small molecule inhibitors for HIF-1α directly or indirectly.

Keywords: HIF-1α; Hypoxia; Inhibitor.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Humans
  • Hypoxia-Inducible Factor 1, alpha Subunit / antagonists & inhibitors*
  • Hypoxia-Inducible Factor 1, alpha Subunit / metabolism
  • Molecular Structure
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Small Molecule Libraries / chemistry
  • Small Molecule Libraries / pharmacology*

Substances

  • Antineoplastic Agents
  • Hypoxia-Inducible Factor 1, alpha Subunit
  • Small Molecule Libraries