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. Author manuscript; available in PMC: 2023 Aug 1.
Published in final edited form as: Mol Aspects Med. 2022 Apr 7;86:101097. doi: 10.1016/j.mam.2022.101097

Table 1.

Selected drugs or compounds trageting PTMs.

Gene/protein Target Targeted Modification Drugs Cancer Phase
20S proteasome Ubiquitination Bortezomib, Carfilzomib, Myeloma, Lymphoma, Lung, Pancreas FDA approved
ALK Phosphorylation Alectinib, Brigatinib, Ceritinib, Crizotinib, Lorlatinib Lung FDA approved
BRAF Phosphorylation Dabrafenib, Encorafenib, Vemurafenib Melanoma, Lung, Colon, Rectum FDA approved
CDK4/6 Phosphorylation Abemaciclib, Ribociclib, and Palbociclib Breast FDA approved
CRBN Ubiquitination Thalidomide, Lenalidomide, Pomalidomide Myeloma FDA approved
EGFR Phosphorylation Afatinib, Almonertinib, Dacomitinib, Erlotinib, Gefitinib, Osimertinib, Amivantamab, Mobocertinib, Cetuximab, Panitumumab Lung, Head and neck, Colon, Rectum FDA approved
HDAC Acetylation Vorinostat, Belinostat, Panobinostat, and Chidamide, Romidepsin Lymphoma, Myeloma FDA approved
HER2/HER3 Phosphorylation Lapatinib, Neratinib, Tucatinib, Trastuzumab and Pertuzumab Lung, Breast FDA approved
Mdm2 Ubiquitination PRIMA Liver, Pancreas FDA approved
MEK1/2 Phosphorylation Binimetinib, Trametinib, and Cobimetinib Melanoma, Lung FDA approved
PD-L1 Glycosylation gPD-L1 Breast Preclinical
PI3K Phosphorylation Copanlisib Lymphomas FDA approved
PI3K Phosphorylation Copanlisib Breast Phase II
Ras/SHP2 Phosphorylation TNO155, JAB-3068, RMC-4630 Solid tumors Phase 1, 2a
Wnt/LRP6 Phosphorylation Salinomycin, Rottlerin, and Monensin Preclinical
Wnt/SRSF Phosphorylation SM08502 Solid tumors Phase 1
Wnt/β-catenin Ubiquitination MSAB Colon Preclinical