loading...| Preferred Name | Covalent tyrosine kinase inhibitors bind and inactivate EGFR kinase domain mutant dimers resistant to non-covalent tyrosine kinase inhibitors | |
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has a Stoichiometric coefficient of 2 Edited: Wu, G, 2011-11-07 Edited: Jassal, B, 2011-11-07 Authored: Orlic-Milacic, M, 2011-11-04 Edited: D'Eustachio, P, 2011-11-07 Covalent (irreversible) tyrosine kinase inhibitors (TKIs), pelitinib, WZ4002, HKI-272, canertinib and afatinib, form a covalent bond with the EGFR cysteine residue C397 and inhibit trans-autophosphorylation of mutants resistant to non-covalent TKIs. However, effective concentrations of covalent TKIs also inhibit wild type EGFR, resulting in severe side effects. Hence, covalent TKIs have not shown much promise as therapeutics. Edited: Matthews, L, 2011-11-07 Reviewed: Greulich, H, 2011-11-15 Reviewed: Savas, S, 2011-11-15 |
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http://purl.obolibrary.org/obo/HINO_0009695 |
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has a Stoichiometric coefficient of 2 Edited: Wu, G, 2011-11-07 Edited: Jassal, B, 2011-11-07 Authored: Orlic-Milacic, M, 2011-11-04 Edited: D'Eustachio, P, 2011-11-07 Covalent (irreversible) tyrosine kinase inhibitors (TKIs), pelitinib, WZ4002, HKI-272, canertinib and afatinib, form a covalent bond with the EGFR cysteine residue C397 and inhibit trans-autophosphorylation of mutants resistant to non-covalent TKIs. However, effective concentrations of covalent TKIs also inhibit wild type EGFR, resulting in severe side effects. Hence, covalent TKIs have not shown much promise as therapeutics. Edited: Matthews, L, 2011-11-07 Reviewed: Greulich, H, 2011-11-15 Reviewed: Savas, S, 2011-11-15 |
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Pubmed20033049 Pubmed20966921 Reactome, http://www.reactome.org |
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Covalent tyrosine kinase inhibitors bind and inactivate EGFR kinase domain mutant dimers resistant to non-covalent tyrosine kinase inhibitors |
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HINO:0009695 |
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Covalent tyrosine kinase inhibitors bind and inactivate EGFR kinase domain mutant dimers resistant to non-covalent tyrosine kinase inhibitors |
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Reactome Database ID Release 431220611 ReactomeREACT_115744 |
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