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50 values for test compounds (concentration of compound that inhibited LPS-stimulated TNF-α production by 50%) were calculated by linear regression analysis.
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0041318841
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Based on Ref. 17b the p38α binding mode from X-ray studies for a p38 inhibitor showing a preference for a (S)-α-methylbenzyl group is depicted below:{A figure is presented}
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Fitzgerald C.E., Patel S.B., Becker J.W., Cameron P.M., Zaller D., Pikounis V.B., O'Keefe S.J., and Scapin G. Nat. Struct. Biol. 10 (2003) 764 Based on Ref. 17b the p38α binding mode from X-ray studies for a p38 inhibitor showing a preference for a (S)-α-methylbenzyl group is depicted below:{A figure is presented}
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31
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0031059866
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note
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5-p38α 30 inhibitor complexes grew spontaneously in hanging drop vapor-diffusion trials conducted at 4 °C with drops containing 1 μL of concentrated protein-inhibitor complex mixed with an equal volume of reservoir solution (10% PEG 8000, 200 mM KCl, 100 mM MgOAc, 50 mM sodium cacodylate, pH 6.5). Prior to data collection, the crystals were slowly transferred to a stabilization solution (8% glycerol, 30% PEG 8000, 200 mM KCl, 100 mM MgOAc, 50 mM sodium cacodylate, pH 6.5) and then flash-frozen in liquid nitrogen. Data to 2.4 Å resolution were collected at the IMCA-CAT beamline BM-17 at the Advanced Photon Source, Argonne, IL. On a MarCCD detector, reduced with the programs DENZO and SCALEPACK, (Otwinowski, Z.; Minor, W. Processing X-ray data collected in oscillation mode. Methods Enzymol. 1997, 276, 307-326.) and refined by program autoBuster (Global Phasing, Ltd, Cambridge, U.K.). The final crystallographic refinement R-factor was 21.2%. The coordinates have been deposited in the Protein Data Bank as entry 3BV2.
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32
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18344395134
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Pargellis C., Tong L., Churchill L., Cirillo P.F., Gilmore T., Graham A.G., Grob P.M., Hickey E.R., Moss N.l., Pav S., and Regan J. Nat. Struct. Biol. 9 (2002) 268
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33
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41849100952
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note
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Based on Ref. 13, the p38α binding mode for a quinazoline p38 inhibitor based on X-ray crystallography studies is depicted below: {A figure is presented}.
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