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