4dfn

Crystal structure of spleen tyrosine kinase complexed with an adamantylpyrazine inhibitorCrystal structure of spleen tyrosine kinase complexed with an adamantylpyrazine inhibitor

Structural highlights 4dfn is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: Related: 4dfl Gene: SYK (Homo sapiens) Activity: Non-specific protein-tyrosine kinase, with EC number 2.7.10.2 Resources: FirstGlance, OCA, RCSB, PDBsum Publication Abstract from PubMed A series of aminopyrazines as inhibitors of Syk kinase activity and showing inhibition of LAD2 cells degranulation is described. Optimization of the carboxamide motif with aminomethylpiperidines provided high potency inhibiting Syk but low cellular activity. Amides of cis and trans adamantanol showed good inhibitory activity against Syk as well as remarkable activity in LAD2 cells degranulation assay. Pyrazine-based Syk kinase inhibitors.,Forns P, Esteve C, Taboada L, Alonso JA, Orellana A, Maldonado M, Carreno C, Ramis I, Lopez M, Miralpeix M, Vidal B Bioorg Med Chem Lett. 2012 Apr 15;22(8):2784-8. Epub 2012 Mar 2. PMID:22425453 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Tyrosine kinase

spinqualitylabelsall models 4dfn, resolution 2.48Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image