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Literature summary for 2.7.10.2 extracted from
- The second generation of BCR-ABL tyrosine kinase inhibitors (2006), Int. J. Hematol., 83, 294-300.
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| E255K | naturally occuring Abl mutant, the mutant is inhibitor imatinib-resistant | Homo sapiens |
| H396P | a naturally occuring Abl activation loop mutant | Homo sapiens |
| M351I | naturally occuring Abl mutant, the mutant is inhibitor imatinib-resistant | Homo sapiens |
| Q252H | naturally occuring Abl mutant, the mutant is inhibitor imatinib-resistant | Homo sapiens |
| Y253F | naturally occuring Abl mutant, the mutant is inhibitor imatinib-resistant | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| AMN107 | a specific BCR-ABL tyrosine kinase inhibitor, Abl binding structure, in vivo inhibition study in chronic myeloid leukemia, CML, overview | Homo sapiens |  |
| AP23464 | ineffective against Abl mutant T315I, but inhibitory against imatinib-resistant mutants M351I, E255K, Q252H, and Y253F, and activation loop mutant H396P | Homo sapiens | |
| CGP76030 | growth-inhibitory in vivo | Homo sapiens | |
| dasatinib | i.e. BMS-354825, Abl binding structure, in vivo inhibition study in chronic myeloid leukemia, CML, overview | Homo sapiens | |
| imatinib | i.e. STI-571, Abl binding structure, in vivo inhibition study in chronic myeloid leukemia, CML, overview | Homo sapiens | |
| additional information | inhibition evaluation study using Src family tyrosine kinase inhibitors and Abl tyrosine kinase, overview | Homo sapiens | |
| NS-187 | a specific dual ABL-LYN inhibitor | Homo sapiens | |
| ON012380 | inhibits wild-type and mutant Abls, substrate-competitive, ATP-incompetitive | Homo sapiens | |
| PD166326 | - |
Homo sapiens | |
| PD173955 | - |
Homo sapiens | |
| PD180970 | - |
Homo sapiens | |
| PP1 | growth-inhibitory in vivo | Homo sapiens | |
| SKI-606 | cytotoxic inhibitor of BCR-ABL | Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | Homo sapiens | the BCR-ABL tyrosine kinase is inhibited in Philadelphia chromosome-positive chronic myeloid leukemia, CML, overview | ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | the BCR-ABL tyrosine kinase is inhibited in Philadelphia chromosome-positive chronic myeloid leukemia, CML, overview | Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| BCR-Abl | - |
Homo sapiens |
| BCR-ABL tyrosine kinase | - |
Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | Abl binding structure | Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000001 | - |
inhibition of BCR-ABL | Homo sapiens | SKI-606 | |
| 0.00001 | - |
below, inhibition of BCR-ABL | Homo sapiens | ON012380 | |
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