Epidermal Growth Factor Receptor as a Target for Anti-Cancer Agent Design
The epidermal growth factor (EGF) receptors, one family of protein tyrosine kinases (PTK), are promising targets for the cancer therapy. Many potential inhibitors including monoclonal antibodies (mAbs), reversible inhibitors and irreversible inhibitors have been developed. Some of them have been approved by the FDA or in the stage of clinical trials. This report reviews the recent progress of the structures, functions and inhibitors of the epidermal growth factor receptor tyrosine kinases.
Keywords: EGFR, epidermal growth factor receptor, protein tyrosine kinase, receptor tyrosine kinase, structure activity relationship, Anti-Cancer Agent, epidermal growth factor (EGF) receptors, protein tyrosine kinases, cancer therapy, monoclonal antibodies, cysteine-rich domains, α-and β-phosphates, DFG aspartate residue, DFG phenylalanine residue, Lapatinib, sorafenib, erlotinib, EGFR kinase, CDK2, transforming growth factor-α, amphiregulin, heparin-binding EGF, neuregulins, breast caner, mitogen-activated protein kinase (MAPK) pathway, phosphatidylinositol 3-kinase (PI3K)/protein kinase B (PKB/AKT) pathway, signal transducer and activator of transcription (STAT) pathway, phospholipase C pathway and SRC/FAK pathway, avian erythroblastosis tumor, Autocrine-paracrine stimulation, umor necrosis factor-α(TGF-α), Cetuximab, Erbitux, Trastuzumab, Herceptin, Pertuzumab, Quinazoline Scaffold, Gefitinib, anilinoquinazoline scaffold, Alkynyl Pyrimidine Scaffold, Pyrrolotrizaine Scaff, Thiazolopyrimidine Scaffold, Quinoline-3-Carbonitrile Scaffold, Benzylidene Hydantoin Scaffold, 4-Amino-6-Arylaminopyrimidine-5-Carbaldehyde Oximes Scaffold, 4-Amino-6-Arylaminopyrimidine-5-Carbaldehyde Hydrazones Scaffold, 5-Oxadiazol-4,6-Diaminopyrimidines Scaffold, 5,7-Diazaindolinone Scaffold, Thiazolidinone Scaffold, Imidazothiazole Scaffold, Histone Deacetylases (HDACs), Pyrrolpyrimidine Scaffold, Acrylamide Scaffold, 1,2-Dithiolane Scaffold, Prrolidinyl-Acetylenicthienopyrimidine Scaffold
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