Xanthine-based photoaffinity probes allow assessment of ligand engagement by TRPC5 channels

Author:

Bauer Claudia C.12345,Minard Aisling12345,Pickles Isabelle B.12345,Simmons Katie J.12345,Chuntharpursat-Bon Eulashini12345,Burnham Matthew P.67895,Kapur Nikil10345,Beech David J.12345,Muench Stephen P.1134512ORCID,Wright Megan H.1331445ORCID,Warriner Stuart L.1331445,Bon Robin S.12345ORCID

Affiliation:

1. Leeds Institute of Cardiovascular and Metabolic Medicine

2. LIGHT Laboratories

3. University of Leeds

4. Leeds LS2 9JT

5. UK

6. Discovery Sciences

7. R&B Biopharmaceuticals

8. AstraZeneca

9. Alderley Park

10. School of Mechanical Engineering

11. School of Biomedical Sciences

12. Astbury Centre for Structural Molecular Biology

13. School of Chemistry

14. Woodhouse Lane

Abstract

Diazirine-containing photoaffinity probes, based on the potent and selective TRPC1/4/5 channel inhibitor Pico145, allowed the development of an assay to probe cellular interactions between TRPC5 protein and xanthine-based TRPC5 channel modulators.

Funder

British Heart Foundation

Wellcome Trust

Biotechnology and Biological Sciences Research Council

AstraZeneca

Publisher

Royal Society of Chemistry (RSC)

Subject

Biochemistry, Genetics and Molecular Biology (miscellaneous),Molecular Biology,Biochemistry,Chemistry (miscellaneous)

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