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Literature summary for 2.7.10.2 extracted from

  • Chan, W.; Wise, S.; Kaufman, M.; Ahn, Y.; Ensinger, C.; Haack, T.; Hood, M.; Jones, J.; Lord, J.; Lu, W.; Miller, D.; Patt, W.; Smith, B.; Petillo, P.; Rutkoski, T.; Telikepalli, H.; Vogeti, L.; Yao, T.; Chun, L.; Clark, R.; Evangelista, P.; Gavrilescu, L
    Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036 (2011), Cancer Cell, 19, 556-568.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expression in Sf9 cell Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitor 4-[4-([[3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]carbamoyl]amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-[4-([[3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]carbamoyl]amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide inhibitor binds to residues Arg386/Glu282 that isoform ABL1 uses to switch between inactive and active conformations. It potently inhibits both unphosphorylated and phosphorylated ABL1 by inducing a type II inactive conformation, and retains efficacy against the majority of clinically relevant chronic myeloid leukemia resistance mutants, including T315I. The compound inhibits isoform BCR-ABL1T315I-expressing cell lines, prolongs survival in mouse models of T315I-mutant chronic myeloid leukemia and B-lymphoblastic leukemia, and inhibits primary patient leukemia cells expressing mutation T315I in vitro and in vivo Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P00519 ABL1
-

Source Tissue

Source Tissue Comment Organism Textmining

Synonyms

Synonyms Comment Organism
ABL1 tyrosine kinase
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000008
-
wild-type, pH not specified in the publication, temperature not specified in the publication Homo sapiens 4-[4-([[3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]carbamoyl]amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide
0.000004
-
mutant T315I, pH not specified in the publication, temperature not specified in the publication Homo sapiens 4-[4-([[3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]carbamoyl]amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide