TY - JOUR
T1 - Inhibiting tyrosine kinases
T2 - successes and limitations.
AU - Arteaga, Carlos L.
N1 - Funding Information:
Supported by R01 CA80195, Breast Cancer Specialized Program of Research Excellence (SPORE) Grant P50 CA98131, and Vanderbilt-Ingram Cancer Center Support Grant P30 CA68485.
PY - 2003
Y1 - 2003
N2 - Seminal studies with STI-571 and Herceptin in chronic myeloid leukemia, gastrointestinal stromal tumors, and breast cancer have clearly demonstrated that blockade of pathogenic tyrosine kinases can alter the natural history of appropriately selected human tumors. On the other hand, trials with EGF receptor inhibitors in unselected populations have shown anywhere from modest to no clinical activity. I will contrast below aspects in the development of inhibitors of Abl, c-Kit, HER2/neu (erbB2), and EGFR, highlight successes and pitfalls in this field, and propose some approaches for the future development of tyrosine kinase inhibitors in human cancer.
AB - Seminal studies with STI-571 and Herceptin in chronic myeloid leukemia, gastrointestinal stromal tumors, and breast cancer have clearly demonstrated that blockade of pathogenic tyrosine kinases can alter the natural history of appropriately selected human tumors. On the other hand, trials with EGF receptor inhibitors in unselected populations have shown anywhere from modest to no clinical activity. I will contrast below aspects in the development of inhibitors of Abl, c-Kit, HER2/neu (erbB2), and EGFR, highlight successes and pitfalls in this field, and propose some approaches for the future development of tyrosine kinase inhibitors in human cancer.
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U2 - 10.4161/cbt.206
DO - 10.4161/cbt.206
M3 - Review article
C2 - 14508084
AN - SCOPUS:1542751704
SN - 1538-4047
VL - 2
SP - S79-83
JO - Cancer biology & therapy
JF - Cancer biology & therapy
IS - 4 Suppl 1
ER -