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Literature summary for 2.7.10.2 extracted from
- Comparison of mutated ABL1 and JAK2 as oncogenes and drug targets in myeloproliferative disorders (2008), Leukemia, 22, 1320-1334.
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| C616Y | the JAK2 mutation is associated with polycythemia vera | Homo sapiens |
| C618R | the JAK2 mutation is associated with polycythemia vera | Homo sapiens |
| D620E | the JAK2 mutation is associated with myeloproliferative syndrome and polycythemia vera | Homo sapiens |
| E627E | the JAK2 mutation is associated with myeloproliferative disorder | Homo sapiens |
| K539L | the JAK2 mutation is associated with polycythemia vera | Homo sapiens |
| K607N | the JAK2 mutation is associated with acute myelogenous leukemia | Homo sapiens |
| L611S | the JAK2 mutation is associated with acute lymphocytic leukemia | Homo sapiens |
| T478S | the JAK1 mutation is associated with acute myelogenous leukemia | Homo sapiens |
| V617F | impairment of JAK2 autoregulation caused by this mutation renders the JAK2 kinase constitutively active | Homo sapiens |
| V623A | the JAK1 mutation is associated with acute myelogenous leukemia | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| AZD-1480 | Jak2 inhibitor | Homo sapiens |  |
| AZD-1480 | Jak2 inhibitor | Mus musculus | |
| bosutinib | previously SKI-606, inhibits ABL1 | Homo sapiens | |
| bosutinib | previously SKI-606, inhibits ABL1 | Mus musculus | |
| dasatinib | potent ABL1 inhibitor | Homo sapiens | |
| dasatinib | potent ABL1 inhibitor | Mus musculus | |
| imatinib | inhibits ABL1autophosphorylation as well as substrate phosphorylation | Homo sapiens | |
| imatinib | inhibits ABL1autophosphorylation as well as substrate phosphorylation | Mus musculus | |
| INCB018424 | Jak2 inhibitor | Homo sapiens | |
| INCB018424 | Jak2 inhibitor | Mus musculus | |
| INNO-406 | previously NS-187, inhibits ABL1 | Homo sapiens | |
| INNO-406 | previously NS-187, inhibits ABL1 | Mus musculus | |
| ITF2357 | Jak2 inhibitor | Homo sapiens | |
| ITF2357 | Jak2 inhibitor | Mus musculus | |
| lestaurtinib | formerly CEP701, JAK2 inhibitor | Homo sapiens | |
| lestaurtinib | formerly CEP701, JAK2 inhibitor | Mus musculus | |
| LS104 | Jak2 inhibitor | Homo sapiens | |
| LS104 | Jak2 inhibitor | Mus musculus | |
| MK-0457 | Jak2 inhibitor | Homo sapiens | |
| MK-0457 | Jak2 inhibitor | Mus musculus | |
| 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 | |
| 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 | |
| nilotinib | potent ABL1 inhibitor | Homo sapiens | |
| nilotinib | potent ABL1 inhibitor | Mus musculus | |
| peroxiredoxin 1 | inhibits ABL1 intracellularly | Homo sapiens | |
| peroxiredoxin 1 | inhibits ABL1 intracellularly | Mus musculus | |
| PIP2 | inhibits ABL1 intracellularly | Homo sapiens | |
| PIP2 | inhibits ABL1 intracellularly | Mus musculus | |
| SB1518 | Jak2 inhibitor | Homo sapiens | |
| SB1518 | Jak2 inhibitor | Mus musculus | |
| TG101209 | Jak2 inhibitor | Homo sapiens | |
| TG101209 | Jak2 inhibitor | Mus musculus | |
| TG101348 | Jak2 inhibitor | Homo sapiens | |
| TG101348 | Jak2 inhibitor | Mus musculus | |
| XL019 | Jak2 inhibitor | Homo sapiens | |
| XL019 | Jak2 inhibitor | Mus musculus | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| nucleus | ABL1 is translocated into the nucleus where its activity contributes to induction of apoptosis and inhibition of cell growth | Mus musculus | 5634 | - |
| 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)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + a [protein]-L-tyrosine | Mus musculus | - |
ADP + a [protein]-L-tyrosine phosphate | - |
? | |
| ATP + a [protein]-L-tyrosine | Homo sapiens | - |
ADP + a [protein]-L-tyrosine phosphate | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Mus musculus | - |
- |
- |
Posttranslational Modification
| Posttranslational Modification | Comment | Organism |
|---|---|---|
| acetylation | normal activation of the ABL1 proteins requires acetylation | Mus musculus |
| acetylation | normal activation of the ABL1 proteins requires acetylation | Homo sapiens |
| acylation | normal activation of the ABL1 proteins requires myristoylation | Mus musculus |
| acylation | normal activation of the ABL1 proteins requires myristoylation | Homo sapiens |
| phosphoprotein | normal activation of the ABL1 proteins requires phosphorylation | Mus musculus |
| phosphoprotein | normal activation of the ABL1 proteins requires phosphorylation | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + a [protein]-L-tyrosine | - |
Mus musculus | ADP + a [protein]-L-tyrosine phosphate | - |
? | |
| ATP + a [protein]-L-tyrosine | - |
Homo sapiens | ADP + a [protein]-L-tyrosine phosphate | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| Abelson murine leukemia viral homolog (1) protein | - |
Mus musculus |
| Abelson murine leukemia viral homolog (1) protein | - |
Homo sapiens |
| ABL1 | - |
Mus musculus |
| ABL1 | - |
Homo sapiens |
| Jak1 | - |
Mus musculus |
| Jak1 | - |
Homo sapiens |
| JAK2 | - |
Mus musculus |
| JAK2 | - |
Homo sapiens |
| Janus kinase 1 | - |
Mus musculus |
| Janus kinase 1 | - |
Homo sapiens |
| Janus kinase 2 | - |
Mus musculus |
| Janus kinase 2 | - |
Homo sapiens |
| just another kinase 2 | - |
Mus musculus |
| non-receptor tyrosine kinase | - |
Mus musculus |
| non-receptor tyrosine kinase | - |
Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Mus musculus | |
| ATP | - |
Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000025 | - |
ABL1 | Homo sapiens | nilotinib | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| 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 |
| 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 |
| 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 |
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