Minges, Alexander ORCID: 0000-0001-7760-2753 and Groth, Georg (2017). Small-molecule inhibition of pyruvate phosphate dikinase targeting the nucleotide binding site. PLoS One, 12 (7). SAN FRANCISCO: PUBLIC LIBRARY SCIENCE. ISSN 1932-6203
Full text not available from this repository.Abstract
Pyruvate phosphate dikinase (PPDK) is an essential enzyme of C4 photosynthesis in plants, catalyzing the ATP-driven conversion of pyruvate to phosphoenolpyruvate ( PEP). It is further used by some bacteria and unicellular protists in the reverse, ATP-forming direction. Many weed species use C4 photosynthesis in contrast to world's major crops, which are C3 plants. Hence inhibitors of PPDK may be used as C4-specific herbicides. By screening a library of 80 commercially available kinase inhibitors, we identified compounds derived from bisindolylmaleimide (bisindolylmaleimide IV, IC50 = 0.76 +/- 0.13 mu M) and indirubin (indirubin3'- monoxime, IC50 = 4.2 +/- 0.9 mu M) that showed high inhibitory potency towards PPDK and are among the most effective PPDK inhibitors described today. Physiological studies on leaf tissues of a C4 model plant confirmed in vivo inhibition of C4-driven photosynthesis by these substances. Moreover, comparative docking studies of non-inhibitory bisindolylmaleimide derivatives suggest that the selectivity towards PPDK may be increased by addition of functional groups to the core structure.
Item Type: | Journal Article | ||||||||||||
Creators: |
|
||||||||||||
URN: | urn:nbn:de:hbz:38-225045 | ||||||||||||
DOI: | 10.1371/journal.pone.0181139 | ||||||||||||
Journal or Publication Title: | PLoS One | ||||||||||||
Volume: | 12 | ||||||||||||
Number: | 7 | ||||||||||||
Date: | 2017 | ||||||||||||
Publisher: | PUBLIC LIBRARY SCIENCE | ||||||||||||
Place of Publication: | SAN FRANCISCO | ||||||||||||
ISSN: | 1932-6203 | ||||||||||||
Language: | English | ||||||||||||
Faculty: | Unspecified | ||||||||||||
Divisions: | Unspecified | ||||||||||||
Subjects: | no entry | ||||||||||||
Uncontrolled Keywords: |
|
||||||||||||
Refereed: | Yes | ||||||||||||
URI: | http://kups.ub.uni-koeln.de/id/eprint/22504 |
Downloads
Downloads per month over past year
Altmetric
Export
Actions (login required)
View Item |