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

Author:

Yeh Tzu-Lan12345ORCID,Leissing Thomas M.12345,Abboud Martine I.12345ORCID,Thinnes Cyrille C.12345ORCID,Atasoylu Onur12345ORCID,Holt-Martyn James P.12345,Zhang Dong12345,Tumber Anthony12345,Lippl Kerstin12345,Lohans Christopher T.12345ORCID,Leung Ivanhoe K. H.12345ORCID,Morcrette Helen678910,Clifton Ian J.12345ORCID,Claridge Timothy D. W.12345,Kawamura Akane12345ORCID,Flashman Emily12345,Lu Xin11123135ORCID,Ratcliffe Peter J.14153165ORCID,Chowdhury Rasheduzzaman12345ORCID,Pugh Christopher W.14153165ORCID,Schofield Christopher J.12345ORCID

Affiliation:

1. Chemistry Research Laboratory

2. Department of Chemistry

3. University of Oxford

4. Oxford OX1 3TA

5. UK

6. Radcliffe Department of Medicine

7. Division of Cardiovascular Medicine

8. BHF Centre of Research Excellence

9. Wellcome Trust Centre for Human Genetics

10. Oxford OX3 7BN

11. Ludwig Institute for Cancer Research

12. Nuffield Department of Clinical Medicine

13. Oxford OX3 7DQ

14. Target Discovery Institute (TDI)

15. Nuffield Department of Medicine

16. Oxford OX3 7FZ

Abstract

Four compounds in clinical trials for anaemia treatment are potent inhibitors of the hypoxia inducible factor (HIF) prolyl hydroxylases (PHDs), but differ in potency and how they interact with HIF at the PHD active site.

Funder

Cancer Research UK

Wellcome Trust

Ludwig Institute for Cancer Research

Engineering and Physical Sciences Research Council

Biotechnology and Biological Sciences Research Council

British Heart Foundation

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

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