Pyrazolyl-pyrimidones inhibit the function of human solute carrier protein SLC11A2 (hDMT1) by metal chelation

Author:

Poirier Marion1234,Pujol-Giménez Jonai52346ORCID,Manatschal Cristina7894ORCID,Bühlmann Sven1234,Embaby Ahmed1234,Javor Sacha1234ORCID,Hediger Matthias A.52346ORCID,Reymond Jean-Louis1234ORCID

Affiliation:

1. Department of Chemistry and Biochemistry

2. University of Bern

3. 3012 Bern

4. Switzerland

5. Institute of Biochemistry and Molecular Medicine

6. Membrane Transport Discovery Lab

7. Department of Biochemistry

8. University of Zürich

9. Zürich

Abstract

Activity optimization of a pyrazolyl-pyrimidone against the iron transporter SLC11A2 (hDMT1) and mechanistic studies revealed that this class of inhibitors act by metal chelation.

Funder

Schweizerischer Nationalfonds zur Förderung der Wissenschaftlichen Forschung

Publisher

Royal Society of Chemistry (RSC)

Subject

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

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