Table II

Drugs targeting PTMs in cancer treatment

Examples of drugs that selectively inhibit PTMs currently under clinical trials or that have passed United States Food and Drug Administration (FDA) approval are shown. Antibodies to receptor tyrosine kinases have not been included in this table.

DrugProtein targetCurrent status: clinical indication
Protein kinase inhibitors
    Erlotinib (Tarceva)EGFRFDA-approved (Tarceva): non-small cell lung cancer
    Gefitinib (Iressa)EGFRPhase II: glioblastoma, breast cancer
    Imatinib (Gleevec)PDGFR/Abl/KitFDA-approved: chronic myeloid leukemia
    UCN-01 (7-hydroxystaurosporine)Cyclin-dependent kinasesPhase I: multiple tumor types
    BAY 43–9006Raf kinasePhase I: multiple solid tumors
    E7070CDK2, Cyclin EPhase II: squamous cell carcinoma
    SU5416Vascular endothelial growth factor receptor, c-Kit, FLT3Phase II: acute myeloid leukemia
Histone deacetylase inhibitors
    MS-275, CI-994, Pivanex, valproic acid, depsipeptide, suberoylanilide hydroxamic acidHistones, transcription factors (likely)Phases I and II: multiple tumors
Prenylation inhibitors
    Tipifarnib (Zarnestra), lonafarnib (Sarasar)Farnesyltransferase (Ras prenylation)Phases II and III: multiple myeloma, multiple tumor types
Ubiquitination-proteasome inhibitors
    Bortezomib (Velcade)26 S proteasomeFDA-approved: multiple myeloma