TY - JOUR
T1 - Epidermal growth factor receptor tyrosine kinase inhibitors in cancer therapy
AU - Adjei, Alex A.
PY - 2001
Y1 - 2001
N2 - Receptor tyrosine kinases are transmembrane proteins involved in signal transduction. They propagate growth factor signals from the cell surface to intracellular processes that control critical functions such as growth, differentiation, angiogenesis and inhibition of apoptosis. In malignancies, these signaling pathways are often exploited to optimize tumor growth and metastasis. One such family of receptor tyrosine kinases is the epidermal growth factor receptor (EGFR) tyrosine kinase. These receptors are overexpressed in a wide variety of epithelial cancers and have been implicated in tumor aggressiveness. Thus, targeting the EGFR tyrosine kinase has attracted considerable attention. This review will summarize current preclinical and clinical knowledge of the small-molecule oral inhibitors of the EGFR tyrosine kinase, which include ZD-1839, OSI-774, CI-1033, EKB-569, PKI-166, GW-2016 and BIBX-1382.
AB - Receptor tyrosine kinases are transmembrane proteins involved in signal transduction. They propagate growth factor signals from the cell surface to intracellular processes that control critical functions such as growth, differentiation, angiogenesis and inhibition of apoptosis. In malignancies, these signaling pathways are often exploited to optimize tumor growth and metastasis. One such family of receptor tyrosine kinases is the epidermal growth factor receptor (EGFR) tyrosine kinase. These receptors are overexpressed in a wide variety of epithelial cancers and have been implicated in tumor aggressiveness. Thus, targeting the EGFR tyrosine kinase has attracted considerable attention. This review will summarize current preclinical and clinical knowledge of the small-molecule oral inhibitors of the EGFR tyrosine kinase, which include ZD-1839, OSI-774, CI-1033, EKB-569, PKI-166, GW-2016 and BIBX-1382.
UR - http://www.scopus.com/inward/record.url?scp=0035685245&partnerID=8YFLogxK
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U2 - 10.1358/dof.2001.026.11.858717
DO - 10.1358/dof.2001.026.11.858717
M3 - Review article
AN - SCOPUS:0035685245
SN - 0377-8282
VL - 26
SP - 1087
EP - 1092
JO - Drugs of the Future
JF - Drugs of the Future
IS - 11
ER -