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Catalytically active MAP KAP kinase 2 structures in complex with staurosporine and ADP reveal differences with the autoinhibited enzyme.
Underwood KW, Parris KD, Federico E, Mosyak L, Czerwinski RM, Shane T, Taylor M, Svenson K, Liu Y, Hsiao CL, Wolfrom S, Maguire M, Malakian K, Telliez JB, Lin LL, Kriz RW, Seehra J, Somers WS, Stahl ML. Underwood KW, et al. Among authors: czerwinski rm. Structure. 2003 Jun;11(6):627-36. doi: 10.1016/s0969-2126(03)00092-3. Structure. 2003. PMID: 12791252 Free article.
Catalytic domain crystal structure of protein kinase C-theta (PKCtheta).
Xu ZB, Chaudhary D, Olland S, Wolfrom S, Czerwinski R, Malakian K, Lin L, Stahl ML, Joseph-McCarthy D, Benander C, Fitz L, Greco R, Somers WS, Mosyak L. Xu ZB, et al. J Biol Chem. 2004 Nov 26;279(48):50401-9. doi: 10.1074/jbc.M409216200. Epub 2004 Sep 13. J Biol Chem. 2004. PMID: 15364937 Free article.
Interleukin 1/Toll-like receptor-induced autophosphorylation activates interleukin 1 receptor-associated kinase 4 and controls cytokine induction in a cell type-specific manner.
Cushing L, Stochaj W, Siegel M, Czerwinski R, Dower K, Wright Q, Hirschfield M, Casanova JL, Picard C, Puel A, Lin LL, Rao VR. Cushing L, et al. J Biol Chem. 2014 Apr 11;289(15):10865-10875. doi: 10.1074/jbc.M113.544809. Epub 2014 Feb 24. J Biol Chem. 2014. PMID: 24567333 Free PMC article.
The advantages of describing covalent inhibitor in vitro potencies by IC50 at a fixed time point. IC50 determination of covalent inhibitors provides meaningful data to medicinal chemistry for SAR optimization.
Thorarensen A, Balbo P, Banker ME, Czerwinski RM, Kuhn M, Maurer TS, Telliez JB, Vincent F, Wittwer AJ. Thorarensen A, et al. Among authors: czerwinski rm. Bioorg Med Chem. 2021 Jan 1;29:115865. doi: 10.1016/j.bmc.2020.115865. Epub 2020 Nov 18. Bioorg Med Chem. 2021. PMID: 33285410
41 results