Reisinger, Bernd, Kuzmanovic, Natascha, Löffler, Patrick, Merkl, Rainer, König, Burkhard and Sterner, Reinhard (2014) Exploiting Protein Symmetry To Design Light-Controllable Enzyme Inhibitors. Angewandte Chemie International Edition 53, pp. 595-598.
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Abstract
The activity of the metabolic branch-point enzyme
PriA from Mycobacterium tuberculosis (mtPriA) can be
controlled reversibly by light. Two-pronged inhibitors based
on the dithienylethene scaffold were designed utilizing
mtPriA�s natural rotational symmetry. Switching from the
flexible, ring-open to the rigid, ring-closed isomer reduces
inhibition activity by one order of magnitude.
Export bibliographical data
| Item type: | Article | ||||
|---|---|---|---|---|---|
| Date: | 2014 | ||||
| Institutions: | Biology, Preclinical Medicine > Institut für Biophysik und physikalische Biochemie > Prof. Dr. Reinhard Sterner Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König | ||||
| Projects: | GRK 1910, Graduiertenkolleg "Medicinal Chemistry of Selective GPCR Ligands" | ||||
| Identification Number: |
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| Keywords: | biosynthesis · enzyme catalysis · enzyme inhibitors · molecular switches · photochromism | ||||
| Dewey Decimal Classification: | 500 Science > 540 Chemistry & allied sciences | ||||
| Status: | Published | ||||
| Refereed: | Yes, this version has been refereed | ||||
| Created at the University of Regensburg: | Yes | ||||
| Item ID: | 29759 |
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