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

(2009) CHEMISTRY & BIOLOGY. 16(6). p.594-604
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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.
Keywords
GLYCOGEN-SYNTHASE KINASE-3, GENE-EXPRESSION, REGULATED GENES, CYTOCHROME-P450, TRANSCRIPTION, MANAGEMENT, SYSTEM, STEROIDS, ENCODES, ELONGATION

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MLA
De Rybel, Bert, et al. “Chemical Inhibition of a Subset of Arabidopsis Thaliana GSK3-like Kinases Activates Brassinosteroid Signaling.” CHEMISTRY & BIOLOGY, vol. 16, no. 6, 2009, pp. 594–604, doi:10.1016/j.chembiol.2009.04.008.
APA
De Rybel, B., Audenaert, D., Vert, G., Rozhon, W., Mayerhofer, J., Peelman, F., … Beeckman, T. (2009). Chemical inhibition of a subset of Arabidopsis thaliana GSK3-like kinases activates brassinosteroid signaling. CHEMISTRY & BIOLOGY, 16(6), 594–604. https://doi.org/10.1016/j.chembiol.2009.04.008
Chicago author-date
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. https://doi.org/10.1016/j.chembiol.2009.04.008.
Chicago author-date (all authors)
De Rybel, Bert, Dominique Audenaert, Grégory Vert, Wilfried Rozhon, Juliane Mayerhofer, Frank Peelman, Silvie Coutuer, Tinneke Denayer, Leentje Jansen, Long Nguyen, Isabelle Vanhoutte, Gerrit Beemster, Kris Vleminckx, Claudia Jonak, Joanne Chory, Dirk Inzé, Eugenia Russinova, and Tom Beeckman. 2009. “Chemical Inhibition of a Subset of Arabidopsis Thaliana GSK3-like Kinases Activates Brassinosteroid Signaling.” CHEMISTRY & BIOLOGY 16 (6): 594–604. doi:10.1016/j.chembiol.2009.04.008.
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.
IEEE
[1]
B. De Rybel et al., “Chemical inhibition of a subset of Arabidopsis thaliana GSK3-like kinases activates brassinosteroid signaling,” CHEMISTRY & BIOLOGY, vol. 16, no. 6, pp. 594–604, 2009.
@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, Grégory 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 Inzé, Dirk and Russinova, Eugenia and Beeckman, Tom},
  issn         = {1074-5521},
  journal      = {CHEMISTRY & BIOLOGY},
  keywords     = {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},
}

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