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Arabidopsis Glycogen synthase kinase 3 (GSK3)-like kinases, also known as Shaggy-like kinases (AtSKs), are a family of 10 highly conserved serine/threonine protein kinases in Arabidopsis thaliana that play pivotal roles in plant growth and development (Youn and Kim, 2015, PMID: 25613340). They are best characterized as negative regulators of the brassinosteroid (BR) signaling pathway, where the member BIN2 (Brassinosteroid-insensitive 2) phosphorylates transcription factors BES1 and BZR1 to inhibit their activity and promote their degradation (UniProt, Q9S735). Beyond BR signaling, these kinases are involved in various processes including stomatal patterning, root development, and responses to abiotic stresses such as salt and drought (Youn and Kim, 2015, PMID: 25613340). Because of their central role in plant architecture and stress resilience, they are significant targets for agricultural biotechnology and chemical biology research. Small molecules like bikinin have been developed to specifically inhibit these kinases, providing tools to manipulate plant growth and study the complex signaling networks they govern (De Rybel et al., 2009, PMID: 19234452).
Inhibition of kinase activity through competitive binding at the ATP-binding pocket, preventing the phosphorylation of downstream substrates such as BES1 and BZR1 (De Rybel et al., 2009, PMID: 19234452).
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