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

@article{citeulike:4996909, 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.}, 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 T. and Vleminckx, Kris and Jonak, Claudia and Chory, Joanne and Inz\'{e}, Dirk and Russinova, Eugenia and Beeckman, Tom}, citeulike-article-id = {4996909}, citeulike-linkout-0 = {http://dx.doi.org/10.1016/j.chembiol.2009.04.008}, citeulike-linkout-1 = {http://linkinghub.elsevier.com/retrieve/pii/S1074552109001410}, citeulike-linkout-2 = {http://view.ncbi.nlm.nih.gov/pubmed/19549598}, citeulike-linkout-3 = {http://www.hubmed.org/display.cgi?uids=19549598}, day = {26}, doi = {10.1016/j.chembiol.2009.04.008}, issn = {1879-1301}, journal = {Chemistry \& biology}, keywords = {arabidopsis, chemical-biology, small-molecule}, month = {June}, number = {6}, pages = {594--604}, posted-at = {2009-08-11 11:03:34}, priority = {2}, 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} }

TY - JOUR ID - citeulike:4996909 L3 - citeulike-article-id:4996909 N2 - 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. IS - 6 JF - Chemistry & biology SN - 1879-1301 EP - 604 TI - Chemical inhibition of a subset of Arabidopsis thaliana GSK3-like kinases activates brassinosteroid signaling. VL - 16 SP - 594 KW - arabidopsis KW - chemical-biology KW - small-molecule AU - De Rybel, Bert AU - Audenaert, Dominique AU - Vert, Grégory AU - Rozhon, Wilfried AU - Mayerhofer, Juliane AU - Peelman, Frank AU - Coutuer, Silvie AU - Denayer, Tinneke AU - Jansen, Leentje AU - Nguyen, Long AU - Vanhoutte, Isabelle AU - Beemster, Gerrit AU - Vleminckx, Kris AU - Jonak, Claudia AU - Chory, Joanne AU - Inzé, Dirk AU - Russinova, Eugenia AU - Beeckman, Tom PY - 2009/06/26/ UR - http://dx.doi.org/10.1016/j.chembiol.2009.04.008 ER -