Title
Chemical inhibition of a subset of **Arabidopsis thaliana** GSK3-like kinases activates brassinosteroid signaling
Author
Faculty/Department
Faculty of Sciences. Biology
Publication type
article
Publication
London ,
Subject
Biology
Source (journal)
Chemistry and biology. - London
Volume/pages
16(2009) :6 , p. 594-604
ISSN
1074-5521
ISI
000267727900005
Carrier
E
Target language
English (eng)
Full text (Publishers DOI)
Affiliation
University of Antwerp
Abstract
Glycogen synthase kinase 3 (GSK3) is a key regulator in signaling pathways in both animals and plants. Three Arabidopsis thaliana GSK3s are shown to be related to brassinosteroid (BR) signaling. In a phenotype-based compound screen we identified bikinin, a small molecule that activates BR signaling downstream of the BR receptor. Bikinin directly binds the GSK3 BIN2 and acts as an ATP competitor. Furthermore, bikinin inhibits the activity of six other Arabidopsis GSK3s. Genome-wide transcript analyses demonstrate that simultaneous inhibition of seven GSK3s is sufficient to activate BR responses. Our data suggest that GSK3 inhibition is the sole activation mode of BR signaling and argues against GSK3-independent BR responses in Arabidopsis. The opportunity to generate multiple and conditional knockouts in key regulators in the BR signaling pathway by bikinin represents a useful tool to further unravel regulatory mechanisms.
Full text (open access)
https://repository.uantwerpen.be/docman/irua/2f47fd/8301.pdf
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