The HIF pathway as a therapeutic target
Related Experiment Video
Updated: Aug 14, 2026

Method for Identifying Small Molecule Inhibitors of the Protein-protein Interaction Between HCN1 and TRIP8b
Published on: November 11, 2016
Kirsty S Hewitson1, Christopher J Schofield
1Oxford Centre for Molecular Sciences and the Department of Chemistry, Chemistry Research Laboratory, Mansfield Road, Oxford, OX1 3TA, UK. kirsty.hewitson@chem.ox.ac.uk
Abstract:
Hypoxia-inducible factor (HIF) is an alpha,beta-heterodimeric transcription factor that mediates cellular responses to low oxygen concentration via the transcriptional activation of specific genes involved in both tumorogenesis and angiogenesis. Manipulation of the HIF pathway has potential use for the treatment of ischemic disease and cancer. Unlike HIF-beta, which is constitutively expressed, the levels and activity of the HIF-alpha subunit are regulated by processes involving posttranslational hydroxylation, catalyzed by Fe(II)- and 2-oxoglutarate-dependent oxygenases. This review focuses on the HIF pathway as a therapeutic target.
Related Concept Videos
Targeted Cancer Therapies
There are several types of targeted therapies against specific...
Regulation of Angiogenesis and Blood Supply
Targets for Drug Action: Overview
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers
TKIs, such as imatinib (Gleevec), are particularly effective in tackling the growth and mitogenic factors that become upregulated in PAH patients. These factors contribute to the...
Pharmacogenomics: Identification of New Drug Targets

