EGFR Inhibitor Resistance Markers

EGFR Inhibitor Resistance Markers
Marker Name Biological Role Evidence References
KRAS v-Ki-ras2 Kirsten rat sarcoma viral oncogene homolog GTPase that relays signals from membrane receptors to downstream effectors (e.g., RAF kinase) to regulate cell proliferation and survival Activating mutations are correlated with resistance to cetuximab and erlotinib in colorectal and lung cancer EGFR inhibitor resistance: KRAS mutation references
BRAF v-raf murine sarcoma viral oncogene homolog B1 Serine/threonine protein kinase that regulates MAPK-ERK signaling pathway Activating mutations are correlated with resistance to cetuximab in colorectal cancer EGFR inhibitor resistance: BRAF references
PTEN Phosphatase and tensin homolog deleted on chromosome 10 PIP3 phosphatase that is a tumor suppressor that reverses the action of PI3 kinase, thereby reducing the activation of AKT and downstream signaling Loss of expression is correlated with resistance to cetuximab in colorectal cancers with WT KRAS EGFR inhibitor resistance: PTEN references
PIK3CA Phosphatidyl-inositol triphosphate kinase catalytic domain, alpha subunit Phosphorylates the lipid PIP2 to form PIP3 which attracts signaling proteins to the membrane, where they activate downstream effectors, e.g., PDK and AKT Activating mutations are associated with resistance to cetuximab in colorectal cancers with WT KRAS EGFR inhibitor resistance: PIK3CA mutation references