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Table 1 Recent examples of successfully developed covalent PPI inhibitors

From: The design and development of covalent protein-protein interaction inhibitors for cancer treatment

Name Type Target Prototypic cancer   Year Reference
Stattic Peptide HIF-1a/ARNT Hepatocellular carcinoma   2012 [84]
Aldehyde boronic acid Small molecule warheads Mcl-1/Bak Multiple myeloma   2016 [47]
RP-D Peptide Grb2/Sos1 Breast cancer   2017 [85]
Achiral oxoapomorphine Small molecule inhibitors P53/MDM2 Prostate cancer   2017 [86]
1_AM Small molecule inhibitors KRAS/G12C Lung cancer   2017 [87]
COH000 Small molecule inhibitors SUMO E1 Colorectal cancer   2018 [88]
Oridonin Small molecule inhibitors NLRP3/NEK7 Breast cancer   2018 [89]
TED-347 Small molecule inhibitors TEAD/Yap Glioblastoma   2019 [90]
Aryl-sulfonyl fluorides/aryl-fluoro sulfates Small molecule warheads XIAP/BIR3 Ovarian cancer   2019 [61]
cHBIs Small molecule inhibitors Allergen/sIgE Colorectal cancer   2019 [91]