Identification and characterization of a novel class of c-Jun N-terminal kinase inhibitors.
Mol Pharmacol. 2012.
PMID: 22434859
Free PMC article.
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Identification and characterization of a novel class of c-Jun N-terminal kinase inhibitors.
Schepetkin IA, Kirpotina LN, Khlebnikov AI, Hanks TS, Kochetkova I, Pascual DW, Jutila MA, Quinn MT.
Schepetkin IA, et al.
Mol Pharmacol. 2012 Jun;81(6):832-45. doi: 10.1124/mol.111.077446. Epub 2012 Mar 20.
Mol Pharmacol. 2012.
PMID: 22434859
Free PMC article.
The sodium salt of IQ-1 inhibited LPS-induced TNF-alpha and IL-6 production in MonoMac-6 cells with IC(50) values of 0.25 and 0.61 muM, respectively. Screening of 131 protein kinases revealed that derivative IQ-3 [11H-indeno[1,2-b]quinoxalin-11-one-O-(2-furoyl)oxime …
The sodium salt of IQ-1 inhibited LPS-induced TNF-alpha and IL-6 production in MonoMac-6 cells with IC(50) values of 0.25 and 0.61 muM, resp …
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Identification of Chemical Inhibitors of β-Catenin-Driven Liver Tumorigenesis in Zebrafish.
Evason KJ, Francisco MT, Juric V, Balakrishnan S, Lopez Pazmino Mdel P, Gordan JD, Kakar S, Spitsbergen J, Goga A, Stainier DY.
Evason KJ, et al.
PLoS Genet. 2015 Jul 2;11(7):e1005305. doi: 10.1371/journal.pgen.1005305. eCollection 2015 Jul.
PLoS Genet. 2015.
PMID: 26134322
Free PMC article.
As expected for a malignant process, transgenic zebrafish showed significantly decreased mean adult survival compared to non-transgenic control siblings. Using this novel transgenic model, we screened for druggable pathways that mediate beta-catenin-induced liver growth an …
As expected for a malignant process, transgenic zebrafish showed significantly decreased mean adult survival compared to non-transgenic cont …
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Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors.
De SK, Chen V, Stebbins JL, Chen LH, Cellitti JF, Machleidt T, Barile E, Riel-Mehan M, Dahl R, Yang L, Emdadi A, Murphy R, Pellecchia M.
De SK, et al.
Bioorg Med Chem. 2010 Jan 15;18(2):590-6. doi: 10.1016/j.bmc.2009.12.013. Epub 2009 Dec 11.
Bioorg Med Chem. 2010.
PMID: 20045647
Free PMC article.
A series of thiadiazole derivatives has been designed as potential allosteric, substrate competitive inhibitors of the protein kinase JNK. We report on the synthesis, characterization and evaluation of a series of compounds that resulted in the …
A series of thiadiazole derivatives has been designed as potential allosteric, substrate competitive inhibitors of the protein …
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