Table 2.
PROTACs studied in vitro and in vivo in TNBC.
| PROTAC’s Name/s | Target | In Vitro | In Vivo | E3 Ligase | Ref. |
|---|---|---|---|---|---|
| Compound 29 | CDK9 | MDA-MB-231 cells | MDA-MB-231 xenograft | CRBN | [70] |
| ZLC491 | CDK12 and CDK13 | MDA-MB-231 cells | MDA-MB-231 xenograft | CRBN | [71] |
| Compound 19s | PAK1 | MDA-MB-231 cells | MDA-MB-231 xenograft | CRBN and VHL | [72] |
| CEP1347-VHL-02 | MLK3 | MDA-MB-468 and HCC1806 cells | - | VHL | [73] |
| ARV-825 | BRD4 | MDA-MB-231 cells | MDA-MB-231 xenograft | CRBN | [74] |
| ARV-771 and MZ1 | BET | MDA-MB-231 and MDA-MB-468 cells | - | VHL | [75] |
| Ganoderic acid A (GAA) | MDM2 | MDA-MB-231 cells | MDA-MB-231 xenograft in zebrafish | VHL | [76] |
| MS8847 | EZH2 | MDA-MB-468 and BT549 cells, and BT549 3D cultures | - | VHL | [77] |
| US-10113 | S100A4 | MDA-MB-231 and 4T1 cells | 4T1 allograft | CRBN | [78] |
| PU7-1 | USP7-1 | MDA-MB-468 and BT549 cells | MDA-MB-468 xenograft | CRBN and VHL | [79] |
| A4 | CDK4/6 | MDA-MB-231 cells | MDA-MB-231 xenograft | DCAF16 | [80] |
| CT-4 | HDAC8 | MDA-MB-231 cells | - | CRBN | [81] |
| TEP | MYC | MDA-MB-468, Hs578T cells and 4T1 | 4T1 allograft | Pomalidomide | [82] |
| MZ1 and ARV-825 | BRD2 and BRD4 | MDA-MB-231 and BT549 cells | MDA-MB-231 xenograft | CRBN and VHL | [83] |
| MS83 | BRD3 and BRD4 | MDA-MB-231 and MDA-MB-468 cells | - | KEAP1 | [84] |
| C8 | PARP2 | MDA-MB-231 cells | MDA-MB-231 xenograft | DCAF16 | [85] |
| LB23 | PARP1 | MDA-MB-231 cells | - | CRBN | [86] |
| NN3 | PARP1 | MDA-MB-231 cells | MDA-MB-231 xenograft | MDM2 | [87] |
| PP-C8 | CDK12-Cyclin K complex | MDA-MB-231 cells | - | CRBN | [88] |
| IY-IY-pom | TrkC | Hs578T | - | CRBN | [89] |
| Compound 6n | AXL kinase | MDA-MB-231 and MDA-MB-468 cells, and TNBC patient organoids | MDA-MB-231 xenograft | CRBN | [90] |
| UI3i | EZH2 | MDA-MB-231 and MDA-MB-468 | - | CRBN | [91] |
| MS8815 | EZH2 | MDA-MB-453, BT549 and patient-derived TNBC cells | - | VHL | [92] |
| AR-PROTAC | AR | BT549 | BT549 xenograft | VHL | [93] |
| dTRIM24 | TRIM24 | Metaplastic and non-metaplastic TNBC tumorspheres | - | VHL | [94] |
| Compound 45 | CDK9 | MDA-MB-231 cells | MDA-MB-231 xenograft | CRBN | [95] |
Abbreviations: AR, androgen receptor; BET, bromodomain and extra terminal; BRD, bromodomain; CDK, cyclin-dependent kinase; CRBN, Cereblon; DCAF16, DDB1- and CUL4-associated factor 16; EZH2, Enhancer of Zeste Homolog 2; KEAP1, Kelch-like ECH-associated protein 1; HDAC, histone deacetylase; MDM2, mouse double minute 2 homolog; MLK3, mixed-lineage protein kinase 3; PAK1, P21 (RAC)1 activated kinase 1; PARP, Polyadenosine 5′-diphosphoribose polymerase; TrkC, Tropomyosin receptor kinase C; USP7, Ubiquitin-specific-processing protease 7; VHL, Von Hippel–Lindau tumor suppressor.