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Literature summary for 2.7.10.2 extracted from

  • Marit, M.R.; Chohan, M.; Matthew, N.; Huang, K.; Kuntz, D.A.; Rose, D.R.; Barber, D.L.
    Random mutagenesis reveals residues of JAK2 critical in evading inhibition by a tyrosine kinase inhibitor (2012), PLoS ONE, 7, e43437.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.10.2

Cloned(Commentary)

Cloned (Comment) Organism
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 Homo sapiens

Protein Variants

Protein Variants Comment Organism
E864K mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I Homo sapiens
G831R mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I Homo sapiens
G935R mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I. Mutant retains kinase activity exceeding 130 microM JAK inhibitor-I Homo sapiens
M929I mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I Homo sapiens
N909K mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I Homo sapiens
P1057S mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I Homo sapiens
R1127K mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I Homo sapiens
R975G mutation is sufficient to support growth and downstream signaling at high oncentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I Homo sapiens
V881A mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I Homo sapiens
Y918H mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one i.e. JAK inhibitor-I Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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-
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Synonyms

Synonyms Comment Organism
JAK2
-
 Homo sapiens