3f3t | pdb_00003f3t

Kinase domain of cSrc in complex with inhibitor RL38 (Type III)

spinqualitylabelsall models 3f3t, resolution 2.50Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 3f3t is a 2 chain structure with sequence from Gallus gallus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: 1AU Related: 2qlq, 2qi8, 2qq7, 3f3u, 3f3v, 3f3w Activity: Non-specific protein-tyrosine kinase, with EC number 2.7.10.2 Resources: FirstGlance, OCA, RCSB, PDBsum Evolutionary Conservation Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf. Publication Abstract from PubMed Targeting kinases outside the highly conserved ATP pocket is thought to be a promising strategy for overcoming bottlenecks in kinase inhibitor research, such as limited selectivity and drug resistance. Here we report the development and application of a direct binding assay to detect small molecules that stabilize the inactive conformation of the tyrosine kinase cSrc. Protein X-ray crystallography validated the assay results and confirmed an exclusively allosteric binding mode. A new screening assay for allosteric inhibitors of cSrc.,Simard JR, Kluter S, Grutter C, Getlik M, Rabiller M, Rode HB, Rauh D Nat Chem Biol. 2009 Jun;5(6):394-6. Epub 2009 Apr 26. PMID:19396179 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Tyrosine kinase

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