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] |