2009
DOI: 10.1016/j.chembiol.2009.04.008
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Chemical Inhibition of a Subset of Arabidopsis thaliana GSK3-like Kinases Activates Brassinosteroid Signaling

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 demonstra… Show more

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Cited by 249 publications
(293 citation statements)
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“…This would suggest that PIF4 has fewer phosphorylation sites than BES1, reported to be modified by this kinase in at least 10 independent Ser/Thr residues (Ryu et al 2010). Incubation with the specific inhibitor bikinin (De Rybel et al 2009) blocked PIF4 phosphorylation as well as autophosphorylation of BIN2, confirming that labeling of this protein is mediated by the BIN2 kinase (Fig. 3C).…”
Section: Bin2 Phosphorylates Pif4 In Vitrosupporting
confidence: 56%
“…This would suggest that PIF4 has fewer phosphorylation sites than BES1, reported to be modified by this kinase in at least 10 independent Ser/Thr residues (Ryu et al 2010). Incubation with the specific inhibitor bikinin (De Rybel et al 2009) blocked PIF4 phosphorylation as well as autophosphorylation of BIN2, confirming that labeling of this protein is mediated by the BIN2 kinase (Fig. 3C).…”
Section: Bin2 Phosphorylates Pif4 In Vitrosupporting
confidence: 56%
“…Consistently, bikinin, which inhibits completely the activity of all members of SKI and SKII and partly that of ATSK32 (ref. 33), caused a similar defect to that observed in the gsk3 sextuple mutant (Fig. 7c-e).…”
Section: Bin2 Interacts With Tdr Cytoplasmic Domain In Y2h Assaysupporting
confidence: 50%
“…Auxin and BRs are known to co-regulate light responses such as the shade avoidance response (Keller et al, 2011;Keuskamp et al, 2011). To test whether BRs and auxin interdependently regulate stomatal development, we tested the effect of NAA on stomata formation in combination with bikinin, an inhibitor of GSK3-like kinases in BR signalling (De Rybel et al, 2009). NAA and bikinin reduced the SI in the wild type and additive effects of both chemicals were evident in the tmm-1 mutant.…”
Section: Auxin Acts Independently Of Brassinosteroids To Suppress Stomentioning
confidence: 99%