Literature summary for 2.7.11.24 extracted from

Shaw, D.; Wang, S.M.; Villasenor, A.G.; Tsing, S.; Walter, D.; Browner, M.F.; Barnett, J.; Kuglstatter, A.
The crystal structure of JNK2 reveals conformational flexibility in the MAP kinase insert and indicates its involvement in the regulation of catalytic activity (2008), J. Mol. Biol., 383, 885-893.

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Activating Compound

Activating Compound	Comment	Organism	Structure
additional information	phosphorylation at the activation loop residue Y185 by MKK4 activates JNK	Homo sapiens

Cloned(Commentary)

Cloned (Comment)	Organism
expression of wild-type and mutant enzymes with or without His6-tag in Escherichia coli strain BL21(DE3)	Homo sapiens

Crystallization (Commentary)

Crystallization (Comment)	Organism
purified recombinant His-tagged mutant enzyme in complex with inhibitor furan-2-carboxylic acid (3-[5-(4H-[1,2,4]triazol-3-yl)-1H-indazol-3-yl]-phenyl)-amide in 0.1 M MES, pH5.6, and 0.88 M sodium citrate, mixing of 0.001 ml of protein in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM MgCl2, 5% glycerol, 5 mM DTT, and 0.02% octyl-beta-D-glucopyranoside with 0.001 ml of 0.1 M MES, pH 5.6, 0.56-0.62 M sodium citrate, and 500 nl of 1000fold diluted seed stock, X-ray diffraction structure determination and analysis at 2.15 A resolution, molecular replacment and modelling	Homo sapiens

Crystallization (Comment)

Organism

purified recombinant His-tagged mutant enzyme in complex with inhibitor furan-2-carboxylic acid (3-[5-(4H-[1,2,4]triazol-3-yl)-1H-indazol-3-yl]-phenyl)-amide in 0.1 M MES, pH5.6, and 0.88 M sodium citrate, mixing of 0.001 ml of protein in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM MgCl2, 5% glycerol, 5 mM DTT, and 0.02% octyl-beta-D-glucopyranoside with 0.001 ml of 0.1 M MES, pH 5.6, 0.56-0.62 M sodium citrate, and 500 nl of 1000fold diluted seed stock, X-ray diffraction structure determination and analysis at 2.15 A resolution, molecular replacment and modelling

Homo sapiens

Protein Variants

Protein Variants	Comment	Organism
C177S/C222S/K250A/K251A/K265A/K270A	site-directed mutagenesis, the hexa-surfaced mutant forms crystallization complexes with inhibitor furan-2-carboxylic acid (3-[5-(4H-[1,2,4]triazol-3-yl)-1H-indazol-3-yl]-phenyl)-amide in contrast to other mutant variants or the wild-type enzyme	Homo sapiens
D3K/C6V/S8N/14E	site-directed mutagenesis using JNK2 1-362 or 1-364, the mutant does not crystallize	Homo sapiens
K203A/E204A	site-directed mutagenesis, the mutant does not crystallize	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
furan-2-carboxylic acid (3-[5-(4H-[1,2,4]triazol-3-yl)-1H-indazol-3-yl]-phenyl)-amide	inhibits JNK2alpha2 enzyme in vitro	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
additional information	Homo sapiens	JNK2 shows conformational flexibility in the MAP kinase insert and its involvement in the regulation of catalytic activity, the MAP kinase insert of JNK2 plays a role in the regulation of JNK2 activation, possibly by interacting with intracellular binding partners, overview	?	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P45984	JNK2	-

Posttranslational Modification

Posttranslational Modification	Comment	Organism
phosphoprotein	phosphorylation ate the activation loop residue Y185 by MKK4 activates JNK	Homo sapiens

Purification (Commentary)

Purification (Comment)	Organism
recombinant wild-type and mutant enzymes from Escherichia coli strain BL21(DE3) by anion exchange chromatography and gel filtration for non-tagged proteins, His6-tagged proteins are purified by nickel affinity chromatography	Homo sapiens

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
additional information	JNK2 shows conformational flexibility in the MAP kinase insert and its involvement in the regulation of catalytic activity, the MAP kinase insert of JNK2 plays a role in the regulation of JNK2 activation, possibly by interacting with intracellular binding partners, overview	Homo sapiens	?	-	?

Subunits

Subunits	Comment	Organism
More	structure analysis of JNK2, conformational flexibility of activation loop and loop 14 region, overview	Homo sapiens

Synonyms

Synonyms	Comment	Organism
c-Jun N-terminal kinase 2	-	Homo sapiens
JNK 2	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.00012	-	-	Homo sapiens	furan-2-carboxylic acid (3-[5-(4H-[1,2,4]triazol-3-yl)-1H-indazol-3-yl]-phenyl)-amide