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Chemical inhibition of a subset of Arabidopsis thaliana GSK3-like kinases activates brassinosteroid signaling

Bert De Rybel UGent, Dominique Audenaert UGent, Grégory Vert, Wilfried Rozhon, Juliane Mayerhofer, Frank Peelman UGent, Silvie Coutuer UGent, Tinneke Denayer, Leentje Jansen UGent and Long Nguyen UGent, et al. (2009) CHEMISTRY & BIOLOGY. 16(6). p.594-604
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 1311 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.
Please use this url to cite or link to this publication:
author
organization
year
type
journalArticle (original)
publication status
published
subject
keyword
GLYCOGEN-SYNTHASE KINASE-3, GENE-EXPRESSION, REGULATED GENES, CYTOCHROME-P450, TRANSCRIPTION, MANAGEMENT, SYSTEM, STEROIDS, ENCODES, ELONGATION
journal title
CHEMISTRY & BIOLOGY
Chem. Biol.
volume
16
issue
6
pages
594 - 604
Web of Science type
Article
Web of Science id
000267727900005
JCR category
BIOCHEMISTRY & MOLECULAR BIOLOGY
JCR impact factor
6.523 (2009)
JCR rank
32/281 (2009)
JCR quartile
1 (2009)
ISSN
1074-5521
DOI
10.1016/j.chembiol.2009.04.008
language
English
UGent publication?
yes
classification
A1
copyright statement
I have transferred the copyright for this publication to the publisher
id
721910
handle
http://hdl.handle.net/1854/LU-721910
date created
2009-08-04 20:10:20
date last changed
2012-12-05 09:32:26
@article{721910,
  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 1311 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.},
  author       = {De Rybel, Bert and Audenaert, Dominique and Vert, Gr{\'e}gory and Rozhon, Wilfried and Mayerhofer, Juliane and Peelman, Frank and Coutuer, Silvie and Denayer, Tinneke and Jansen, Leentje and Nguyen, Long and Vanhoutte, Isabelle and Beemster, Gerrit and Vleminckx, Kris and Jonak, Claudia and Chory, Joanne and Inz{\'e}, Dirk and Russinova, Eugenia and Beeckman, Tom},
  issn         = {1074-5521},
  journal      = {CHEMISTRY \& BIOLOGY},
  keyword      = {GLYCOGEN-SYNTHASE KINASE-3,GENE-EXPRESSION,REGULATED GENES,CYTOCHROME-P450,TRANSCRIPTION,MANAGEMENT,SYSTEM,STEROIDS,ENCODES,ELONGATION},
  language     = {eng},
  number       = {6},
  pages        = {594--604},
  title        = {Chemical inhibition of a subset of Arabidopsis thaliana GSK3-like kinases activates brassinosteroid signaling},
  url          = {http://dx.doi.org/10.1016/j.chembiol.2009.04.008},
  volume       = {16},
  year         = {2009},
}

Chicago
De Rybel, Bert, Dominique Audenaert, Grégory Vert, Wilfried Rozhon, Juliane Mayerhofer, Frank Peelman, Silvie Coutuer, et al. 2009. “Chemical Inhibition of a Subset of Arabidopsis Thaliana GSK3-like Kinases Activates Brassinosteroid Signaling.” Chemistry & Biology 16 (6): 594–604.
APA
De Rybel, B., Audenaert, D., Vert, G., Rozhon, W., Mayerhofer, J., Peelman, F., Coutuer, S., et al. (2009). Chemical inhibition of a subset of Arabidopsis thaliana GSK3-like kinases activates brassinosteroid signaling. CHEMISTRY & BIOLOGY, 16(6), 594–604.
Vancouver
1.
De Rybel B, Audenaert D, Vert G, Rozhon W, Mayerhofer J, Peelman F, et al. Chemical inhibition of a subset of Arabidopsis thaliana GSK3-like kinases activates brassinosteroid signaling. CHEMISTRY & BIOLOGY. 2009;16(6):594–604.
MLA
De Rybel, Bert, Dominique Audenaert, Grégory Vert, et al. “Chemical Inhibition of a Subset of Arabidopsis Thaliana GSK3-like Kinases Activates Brassinosteroid Signaling.” CHEMISTRY & BIOLOGY 16.6 (2009): 594–604. Print.