Molecular and cellular mechanisms of HIF prolyl hydroxylase inhibitors in clinical trials.

@article{Yeh2017MolecularAC,
  title={Molecular and cellular mechanisms of HIF prolyl hydroxylase inhibitors in clinical trials.},
  author={Tzu-Lan Yeh and Thomas M. Leissing and Martine I Abboud and Cyrille C Thinnes and Onur Atasoylu and James P. Holt-Martyn and Dong Zhang and Anthony Tumber and Kerstin Lippl and Christopher T Lohans and Ivanhoe K H Leung and Helen Morcrette and Ian J. Clifton and Timothy D W Claridge and Akane Kawamura and Emily Flashman and Xin Lu and Peter J Ratcliffe and Rasheduzzaman Chowdhury and Christopher W Pugh and Christopher J. Schofield},
  journal={Chemical science},
  year={2017},
  volume={8 11},
  pages={7651-7668}
}
Inhibition of the human 2-oxoglutarate (2OG) dependent hypoxia inducible factor (HIF) prolyl hydroxylases (human PHD1-3) causes upregulation of HIF, thus promoting erythropoiesis and is therefore of therapeutic interest. We describe cellular, biophysical, and biochemical studies comparing four PHD inhibitors currently in clinical trials for anaemia treatment, that describe their mechanisms of action, potency against isolated enzymes and in cells, and selectivities versus representatives of… CONTINUE READING