Universität zu Köln

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

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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:	Creators Email ORCID ORCID Put Code Minges, Alexander UNSPECIFIED orcid.org/0000-0001-7760-2753 UNSPECIFIED Groth, Georg UNSPECIFIED UNSPECIFIED UNSPECIFIED
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:	Keywords Language PROTEIN-KINASE-C; SWIVELING-DOMAIN MECHANISM; BUNDLE SHEATH-CELLS; ORTHOPHOSPHATE DIKINASE; C-4 PHOTOSYNTHESIS; REVERSIBLE PHOSPHORYLATION; INACTIVATION; ACTIVATION; DESIGN; CANCER Multiple languages Multidisciplinary Sciences Multiple languages
Refereed:	Yes
URI:	http://kups.ub.uni-koeln.de/id/eprint/22504