Covalent (irreversible) tyrosine kinase inhibitors (TKIs), p...

created [InstanceEdit:1225977] Orlic-Milacic, Marija, 2011-03-03
dbId 1225971
displayName Covalent (irreversible) tyrosine kinase inhibitors (TKIs), p...
modified [InstanceEdit:2010568] Orlic-Milacic, Marija, 2011-11-22
schemaClass Summation
text 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.
Cite Us!