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Novel thidiazuron-derived inhibitors of cytokinin oxidase/dehydrogenase

Overview of attention for article published in Plant Molecular Biology, July 2016
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Title
Novel thidiazuron-derived inhibitors of cytokinin oxidase/dehydrogenase
Published in
Plant Molecular Biology, July 2016
DOI 10.1007/s11103-016-0509-0
Pubmed ID
Authors

Jaroslav Nisler, David Kopečný, Radka Končitíková, Marek Zatloukal, Václav Bazgier, Karel Berka, David Zalabák, Pierre Briozzo, Miroslav Strnad, Lukáš Spíchal

Abstract

Two new TDZ derivatives (HETDZ and 3FMTDZ) are very potent inhibitors of CKX and are promising candidates for in vivo studies. Cytokinin hormones regulate a wide range of essential processes in plants. Thidiazuron (N-phenyl-N'-1,2,3-thiadiazol-5-yl urea, TDZ), formerly registered as a cotton defoliant, is a well known inhibitor of cytokinin oxidase/dehydrogenase (CKX), an enzyme catalyzing the degradation of cytokinins. TDZ thus increases the lifetime of cytokinins and their effects in plants. We used in silico modeling to design, synthesize and characterize twenty new TDZ derivatives with improved inhibitory properties. Two compounds, namely 1-[1,2,3]thiadiazol-5-yl-3-(3-trifluoromethoxy-phenyl)urea (3FMTDZ) and 1-[2-(2-hydroxyethyl)phenyl]-3-(1,2,3-thiadiazol-5-yl)urea (HETDZ), displayed up to 15-fold lower IC 50 values compared with TDZ for AtCKX2 from Arabidopsis thaliana and ZmCKX1 and ZmCKX4a from Zea mays. Binding modes of 3FMTDZ and HETDZ were analyzed by X-ray crystallography. Crystal structure complexes, solved at 2.0 Å resolution, revealed that HETDZ and 3FMTDZ bound differently in the active site of ZmCKX4a: the thiadiazolyl ring of 3FMTDZ was positioned over the isoalloxazine ring of FAD, whereas that of HETDZ had the opposite orientation, pointing toward the entrance of the active site. The compounds were further tested for cytokinin activity in several cytokinin bioassays. We suggest that the combination of simple synthesis, lowered cytokinin activity, and enhanced inhibitory effects on CKX isoforms, makes 3FMTDZ and HETDZ suitable candidates for in vivo studies.

Twitter Demographics

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Mendeley readers

The data shown below were compiled from readership statistics for 22 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 22 100%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 10 45%
Researcher 3 14%
Unspecified 2 9%
Student > Postgraduate 2 9%
Professor > Associate Professor 2 9%
Other 3 14%
Readers by discipline Count As %
Agricultural and Biological Sciences 10 45%
Chemistry 5 23%
Unspecified 3 14%
Computer Science 1 5%
Biochemistry, Genetics and Molecular Biology 1 5%
Other 2 9%

Attention Score in Context

This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 17 July 2016.
All research outputs
#9,836,688
of 12,316,795 outputs
Outputs from Plant Molecular Biology
#2,123
of 2,374 outputs
Outputs of similar age
#165,009
of 233,927 outputs
Outputs of similar age from Plant Molecular Biology
#14
of 30 outputs
Altmetric has tracked 12,316,795 research outputs across all sources so far. This one is in the 11th percentile – i.e., 11% of other outputs scored the same or lower than it.
So far Altmetric has tracked 2,374 research outputs from this source. They receive a mean Attention Score of 4.0. This one is in the 6th percentile – i.e., 6% of its peers scored the same or lower than it.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 233,927 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 16th percentile – i.e., 16% of its contemporaries scored the same or lower than it.
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