GENE
PROTEIN · ACTIVATION
TUMOR(S)
TARGETED DRUG
ERBB2 (HER2)
receptor tyrosine kinase
Amplification
Breast, gastric carcinoma
Trastuzumab, pertuzumab
EGFR (ERBB1)
receptor tyrosine kinase
Activating mutation
Lung adenocarcinoma (non-smokers, women, Asian)
Erlotinib, osimertinib; cetuximab in colon (if KRAS wild-type)
ALK
receptor tyrosine kinase
Rearrangement (EML4-ALK)
Lung adenocarcinoma (young non-smokers); anaplastic large cell lymphoma
Crizotinib, alectinib
RET
receptor tyrosine kinase
Point mutation (germline) · RET/PTC rearrangement
MEN2A, MEN2B, medullary thyroid · papillary thyroid
Prophylactic thyroidectomy in carriers
KIT (CD117)
receptor tyrosine kinase
Activating mutation
GIST, systemic mastocytosis, seminoma
Imatinib
Point mutation → can't hydrolyze GTP → always on
Pancreatic (KRAS ~90%), colorectal, lung adenocarcinoma; most common mutated oncogene
KRAS mutation → anti-EGFR antibodies fail
BRAF
serine/threonine kinase
V600E point mutation
Melanoma, papillary thyroid, hairy cell leukemia, colorectal
Vemurafenib, dabrafenib
ABL (BCR-ABL)
non-receptor tyrosine kinase
t(9;22) Philadelphia chromosome
CML; subset of ALL (worse prognosis)
Imatinib, dasatinib
JAK2
non-receptor tyrosine kinase
V617F point mutation
Polycythemia vera, essential thrombocythemia, myelofibrosis
Ruxolitinib
MYC family
transcription factor
c-MYC: t(8;14) · N-MYC: amplification · L-MYC: amplification
Burkitt lymphoma · neuroblastoma (poor prognosis) · small cell lung cancer
—
CCND1 (cyclin D1)
cell-cycle regulator
t(11;14)
Mantle cell lymphoma
CDK4/6 inhibitors exist (breast)
t(14;18) → overexpression
Follicular lymphoma
Venetoclax (BCL-2 inhibitor, CLL)
MDM2 · CDK4
p53/Rb opponents
Amplification
Well-differentiated and dedifferentiated liposarcoma
MDM2 degrades p53