Pharmacological targeting of the HIF hydroxylases–a new field in medicine development

MC Chan, JP Holt-Martyn, CJ Schofield… - Molecular aspects of …, 2016 - Elsevier
In human cells oxygen levels are 'sensed'by a set of ferrous iron and 2-oxoglutarate
dependent dioxygenases. These enzymes regulate a broad range of cellular and systemic
responses to hypoxia by catalysing the post-translational hydroxylation of specific residues
in the alpha subunits of hypoxia inducible factor (HIF) transcriptional complexes. The HIF
hydroxylases are now the subject of pharmaceutical targeting by small molecule inhibitors
that aim to activate or augment the endogenous HIF transcriptional response for the …