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Literature summary extracted from

  • Walz, C.; Cross, N.C.; Van Etten, R.A.; Reiter, A.
    Comparison of mutated ABL1 and JAK2 as oncogenes and drug targets in myeloproliferative disorders (2008), Leukemia, 22, 1320-1334.
    View publication on PubMedView publication on EuropePMC

Protein Variants

EC Number Protein Variants Comment Organism
2.7.10.2 C616Y the JAK2 mutation is associated with polycythemia vera Homo sapiens
2.7.10.2 C618R the JAK2 mutation is associated with polycythemia vera Homo sapiens
2.7.10.2 D620E the JAK2 mutation is associated with myeloproliferative syndrome and polycythemia vera Homo sapiens
2.7.10.2 E627E the JAK2 mutation is associated with myeloproliferative disorder Homo sapiens
2.7.10.2 K539L the JAK2 mutation is associated with polycythemia vera Homo sapiens
2.7.10.2 K607N the JAK2 mutation is associated with acute myelogenous leukemia Homo sapiens
2.7.10.2 L611S the JAK2 mutation is associated with acute lymphocytic leukemia Homo sapiens
2.7.10.2 T478S the JAK1 mutation is associated with acute myelogenous leukemia Homo sapiens
2.7.10.2 V617F impairment of JAK2 autoregulation caused by this mutation renders the JAK2 kinase constitutively active Homo sapiens
2.7.10.2 V623A the JAK1 mutation is associated with acute myelogenous leukemia Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.10.2 AZD-1480 Jak2 inhibitor Homo sapiens
2.7.10.2 AZD-1480 Jak2 inhibitor Mus musculus
2.7.10.2 bosutinib previously SKI-606, inhibits ABL1 Homo sapiens
2.7.10.2 bosutinib previously SKI-606, inhibits ABL1 Mus musculus
2.7.10.2 dasatinib potent ABL1 inhibitor Homo sapiens
2.7.10.2 dasatinib potent ABL1 inhibitor Mus musculus
2.7.10.2 imatinib inhibits ABL1autophosphorylation as well as substrate phosphorylation Homo sapiens
2.7.10.2 imatinib inhibits ABL1autophosphorylation as well as substrate phosphorylation Mus musculus
2.7.10.2 INCB018424 Jak2 inhibitor Homo sapiens
2.7.10.2 INCB018424 Jak2 inhibitor Mus musculus
2.7.10.2 INNO-406 previously NS-187, inhibits ABL1 Homo sapiens
2.7.10.2 INNO-406 previously NS-187, inhibits ABL1 Mus musculus
2.7.10.2 ITF2357 Jak2 inhibitor Homo sapiens
2.7.10.2 ITF2357 Jak2 inhibitor Mus musculus
2.7.10.2 lestaurtinib formerly CEP701, JAK2 inhibitor Homo sapiens
2.7.10.2 lestaurtinib formerly CEP701, JAK2 inhibitor Mus musculus
2.7.10.2 LS104 Jak2 inhibitor Homo sapiens
2.7.10.2 LS104 Jak2 inhibitor Mus musculus
2.7.10.2 MK-0457 Jak2 inhibitor Homo sapiens
2.7.10.2 MK-0457 Jak2 inhibitor Mus musculus
2.7.10.2 additional information ABL1 is autoinhibited in an intramolecular fashion that is similar to SRC kinases, where the SH3 domain is engaged with a single proline residue in the spacer region between the SRC homology 2 and tyrosine kinase domains Homo sapiens
2.7.10.2 additional information ABL1 is autoinhibited in an intramolecular fashion that is similar to SRC kinases, where the SH3 domain is engaged with a single proline residue in the spacer region between the SRC homology 2 and tyrosine kinase domains Mus musculus
2.7.10.2 nilotinib potent ABL1 inhibitor Homo sapiens
2.7.10.2 nilotinib potent ABL1 inhibitor Mus musculus
2.7.10.2 peroxiredoxin 1 inhibits ABL1 intracellularly Homo sapiens
2.7.10.2 peroxiredoxin 1 inhibits ABL1 intracellularly Mus musculus
2.7.10.2 PIP2 inhibits ABL1 intracellularly Homo sapiens
2.7.10.2 PIP2 inhibits ABL1 intracellularly Mus musculus
2.7.10.2 SB1518 Jak2 inhibitor Homo sapiens
2.7.10.2 SB1518 Jak2 inhibitor Mus musculus
2.7.10.2 TG101209 Jak2 inhibitor Homo sapiens
2.7.10.2 TG101209 Jak2 inhibitor Mus musculus
2.7.10.2 TG101348 Jak2 inhibitor Homo sapiens
2.7.10.2 TG101348 Jak2 inhibitor Mus musculus
2.7.10.2 XL019 Jak2 inhibitor Homo sapiens
2.7.10.2 XL019 Jak2 inhibitor Mus musculus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.7.10.2 nucleus ABL1 is translocated into the nucleus where its activity contributes to induction of apoptosis and inhibition of cell growth Mus musculus 5634
-
2.7.10.2 nucleus ABL1 is translocated into the nucleus where its activity contributes to induction of apoptosis and inhibition of cell growth Homo sapiens 5634
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.10.2 ATP + a [protein]-L-tyrosine Mus musculus
-
 ADP + a [protein]-L-tyrosine phosphate
-
 ?
2.7.10.2 ATP + a [protein]-L-tyrosine Homo sapiens
-
 ADP + a [protein]-L-tyrosine phosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.10.2 Homo sapiens
-
-
-
2.7.10.2 Mus musculus
-
-
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
2.7.10.2 acetylation normal activation of the ABL1 proteins requires acetylation Mus musculus
2.7.10.2 acetylation normal activation of the ABL1 proteins requires acetylation Homo sapiens
2.7.10.2 acylation normal activation of the ABL1 proteins requires myristoylation Mus musculus
2.7.10.2 acylation normal activation of the ABL1 proteins requires myristoylation Homo sapiens
2.7.10.2 phosphoprotein normal activation of the ABL1 proteins requires phosphorylation Mus musculus
2.7.10.2 phosphoprotein normal activation of the ABL1 proteins requires phosphorylation Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.10.2 ATP + a [protein]-L-tyrosine
-
 Mus musculus ADP + a [protein]-L-tyrosine phosphate
-
 ?
2.7.10.2 ATP + a [protein]-L-tyrosine
-
 Homo sapiens ADP + a [protein]-L-tyrosine phosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.10.2 Abelson murine leukemia viral homolog (1) protein
-
 Mus musculus
2.7.10.2 Abelson murine leukemia viral homolog (1) protein
-
 Homo sapiens
2.7.10.2 ABL1
-
 Mus musculus
2.7.10.2 ABL1
-
 Homo sapiens
2.7.10.2 Jak1
-
 Mus musculus
2.7.10.2 Jak1
-
 Homo sapiens
2.7.10.2 JAK2
-
 Mus musculus
2.7.10.2 JAK2
-
 Homo sapiens
2.7.10.2 Janus kinase 1
-
 Mus musculus
2.7.10.2 Janus kinase 1
-
 Homo sapiens
2.7.10.2 Janus kinase 2
-
 Mus musculus
2.7.10.2 Janus kinase 2
-
 Homo sapiens
2.7.10.2 just another kinase 2
-
 Mus musculus
2.7.10.2 non-receptor tyrosine kinase
-
 Mus musculus
2.7.10.2 non-receptor tyrosine kinase
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.10.2 ATP
-
 Mus musculus
2.7.10.2 ATP
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.10.2 0.000025
-
 ABL1 Homo sapiens nilotinib

General Information

EC Number General Information Comment Organism
2.7.10.2 malfunction only 75% of ABL1 knockout mice survive the first week,33 the remaining animals show severe defects in spermatogenesis, thymic and splenic atrophy, susceptibility to infections and reductions of T- and B-cell lymphocytes and their early precursors in lymphoid organs Mus musculus
2.7.10.2 physiological function ABL1 binds to the actin cytoskeleton and is involved in cytoskeletal organization, non-erythroid myelopoiesis and regulation of small GTPases, in response to genotoxic stress such as DNA damage or the increase of reactive oxygen species, ABL1 is translocated into the nucleus where its activity contributes to induction of apoptosis and inhibition of cell growth Mus musculus
2.7.10.2 physiological function ABL1 binds to the actin cytoskeleton and is involved in cytoskeletal organization, non-erythroid myelopoiesis and regulation of small GTPases, in response to genotoxic stress such as DNA damage or the increase of reactive oxygen species, ABL1 is translocated into the nucleus where its activity contributes to induction of apoptosis and inhibition of cell growth Homo sapiens