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Structure-Activity Relationship and Crystallographic Studies on 4-Hydroxypyrimidine HIF Prolyl Hydroxylase Domain Inhibitors |
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| Authors: | Dr James P Holt-Martyn Dr Rasheduzzaman Chowdhury Dr Anthony Tumber Dr Tzu-Lan Yeh Dr Martine I Abboud Dr Kerstin Lippl Dr Christopher T Lohans Dr Gareth W Langley William Figg Jr Dr Michael A McDonough Prof?Dr Christopher W Pugh Prof?Dr Peter J Ratcliffe Prof?Dr Christopher J Schofield |
| Affiliation: | 1. Department of Chemistry, University of Oxford Chemistry Research Laboratory, 12 Mansfield Road, Oxford, OX1 3TA UK;2. NDM Research Building, University of Oxford, Oxford, OX3 7FZ UK;3. NDM Research Building, University of Oxford, Oxford, OX3 7FZ UK
The Francis Crick Institute, London, NW1 1AT UK |
| Abstract: | The 2-oxoglutarate-dependent hypoxia inducible factor prolyl hydroxylases (PHDs) are targets for treatment of a variety of diseases including anaemia. One PHD inhibitor is approved for use for the treatment of renal anaemia and others are in late stage clinical trials. The number of reported templates for PHD inhibition is limited. We report structure–activity relationship and crystallographic studies on a promising class of 4-hydroxypyrimidine-containing PHD inhibitors. |
| Keywords: | anaemia hypoxia prolyl hydroxylases structure-activity relationships |
