3gta | pdb_00003gta

Structure of an ML-IAP/XIAP chimera bound to a peptidomimetic

spinqualitylabelsall models 3gta, resolution 1.70Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 3gta is a 2 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: 851, BTB, EDO, LI, ZN Related: 3f7h, 3f7i, 3f7g, 2i3h, 2i3i, 1tw6 Gene: BIRC7 (HUMAN) Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT 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 A series of IAP antagonists based on thiazole or benzothiazole amide isosteres was designed and synthesized. These compounds were tested for binding to the XIAP-BIR3 and ML-IAP BIR using a fluorescence polarization assay. The most potent of these compounds, 19a and 33b, were found to have K(i)'s of 20-30 nM against ML-IAP and 50-60 nM against XIAP-BIR3. Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres.,Cohen F, Koehler MF, Bergeron P, Elliott LO, Flygare JA, Franklin MC, Gazzard L, Keteltas SF, Lau K, Ly CQ, Tsui V, Fairbrother WJ Bioorg Med Chem Lett. 2010 Apr 1;20(7):2229-33. Epub 2010 Feb 8. PMID:20189383 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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