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 μM) and indirubin (indirubin-3’-monoxime, IC50 = 4.2 ± 0.9 μM) 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.
Highlights
The main characteristic of C4 plants is their ability to thrive in warm and dry environmental conditions by efficient usage of nitrogen, water and CO2 [1,2,3]
To search for inhibitory compounds blocking the nucleotide binding site, a set of 80 commercially available kinase inhibitors was screened for effects on phosphate dikinase (PPDK) from the C4 plant Flaveria trinervia
Seven of the top scoring compounds belong to the chemical class of bisindolylmaleimides which are characterized by an indol-substituted maleimide structure and varying other structural elements
Summary
The main characteristic of C4 plants is their ability to thrive in warm and dry environmental conditions by efficient usage of nitrogen, water and CO2 [1,2,3]. Novel inhibitors of a C4 plant enzyme as potential herbicides binding site from a set of commercially available kinase inhibitors by using PPDK from the C4 plant Flaveria trinervia in an in vitro assay.
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