Dual activity inhibition of threonine aspartase 1 by a single bisphosphate ligand

Author:

Höing Alexander1ORCID,Struth Robin2ORCID,Beuck Christine3ORCID,Rafieiolhosseini Neda4ORCID,Hoffmann Daniel4ORCID,Stauber Roland H.5ORCID,Bayer Peter3ORCID,Niemeyer Jochen2ORCID,Knauer Shirley K.1ORCID

Affiliation:

1. Molecular Biology II, Center of Medical Biotechnology (ZMB)/Center for Nanointegration Duisburg-Essen (CENIDE), University of Duisburg-Essen, Universitätsstrasse 5, 45141 Essen, Germany

2. Organic Chemistry, Center for Nanointegration Duisburg-Essen (CENIDE), University of Duisburg-Essen, Universitätsstrasse 7, 45141 Essen, Germany

3. Structural and Medicinal Biochemistry, Center for Medical Biotechnology (ZMB), University of Duisburg-Essen, Universitätsstrasse 5, 45141 Essen, Germany

4. Bioinformatics and Computational Biophysics, Center for Medical Biotechnology (ZMB), University of Duisburg-Essen, Universitätsstrasse 5, 45141 Essen, Germany

5. Molecular and Cellular Oncology/ENT, University Medical Center Mainz (UMM), Langenbeckstrasse 1, 55101 Mainz, Germany

Abstract

“Targeting two for the price of one” – a selective bisphosphate ligand allows dual inhibition of threonine aspartase 1 by simultaneously addressing independent key functions – its protein–protein interaction-based activation and enzymatic function.

Funder

Deutsche Forschungsgemeinschaft

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemical Engineering,General Chemistry

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