2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinase

Author:

Matheson Christopher J.12345,Coxon Christopher R.12345ORCID,Bayliss Richard67859ORCID,Boxall Kathy1011125,Carbain Benoit12345,Fry Andrew M.6785ORCID,Hardcastle Ian R.12345,Harnor Suzannah J.12345ORCID,Mas-Droux Corine911125,Newell David R.11314153,Richards Mark W.6785,Sivaprakasam Mangaleswaran12345,Turner David12345,Griffin Roger J.12345,Golding Bernard T.12345ORCID,Cano Céline12345ORCID

Affiliation:

1. Cancer Research UK Newcastle Drug Discovery Unit

2. Chemistry, School of Natural and Environmental Sciences

3. Newcastle University

4. Newcastle upon Tyne

5. UK

6. School of Molecular and Cellular Biology

7. The Astbury Centre for Structural Molecular Biology

8. University of Leeds

9. Section of Structural Biology

10. Cancer Research UK Cancer Therapeutics Unit

11. The Institute of Cancer Research

12. Sutton

13. Translational and Clinical Research Institute

14. Newcastle University Centre for Cancer

15. Faculty of Medical Sciences

Abstract

Renewed interest in covalent inhibitors of enzymes implicated in disease states has afforded several agents targeted at protein kinases of relevance to cancers.

Funder

Cancer Research UK

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

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