|
|||||
|
|
Exploiting Protein Symmetry To Design Light‐Controllable Enzyme Inhibitors |
|
| Authors: | Bernd Reisinger Natascha Kuzmanovic Patrick Löffler Prof. Dr. Rainer Merkl Prof. Dr. Burkhard König Prof. Dr. Reinhard Sterner |
| Affiliation: | 1. Institut für Biophysik und physikalische Biochemie, Universit?t Regensburg, 93040 Regensburg (Germany);2. Institut für Organische Chemie, Universit?t Regensburg, 93040 Regensburg (Germany) |
| 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. |
| Keywords: | biosynthesis enzyme catalysis enzyme inhibitors molecular switches photochromism |