Table 1.
Cancer Types | Target Protein | TPD Approach | References |
---|---|---|---|
Solid tumors | |||
Prostate cancer | AR | ARCC-4 PROTAC | [30] |
AR Splice Variant-7 | MTX-23 PROTAC | [61] | |
Breast cancer | Estrogen receptor | ARV-471 PROTAC | [62] |
AC682 PROTAC | |||
DT2216 PROTAC | |||
SGK3 | SGK3-PROTAC1, HaloTag tool | [38,50] | |
IGF-1R/Src | CPR3/CPR4 PROTACs | [63] | |
BRD4 | Ab-PROTAC 3 | [64] | |
BRD4 | Bioorthogonal PROTAC | [65] | |
Lung cancer | IGF-1R/Src | CPR3/CPR4 PROTACs | [63] |
BRD4 | H2O2-inducible PROTAC | [66] | |
EML4-ALK fusion | dALK opto-PROTAC | [67] | |
Osteosarcoma | BET proteins | MZ1 PROTAC | [29] |
BETd-260 PROTAC | [68] | ||
Ewing sarcoma | EWS::FLI1 | dTAG tool | [43] |
TRIM8 | dTAG tool | [69] | |
ETV6 | dTAG tool | [70] | |
BRD4 | BETd PROTAC | [71] | |
CK1 | CK1α PROTAC | [72] | |
Glioblastoma | HDAC6 | J22352 PROTAC | [57] |
Rhabdomyosarcoma | SMARCA4/A2 | ACBI-1 PROTAC | [73] |
PAX3::FOXO1 | dTAG tool | [74] | |
Melanoma | Mutant BRAF | SJF-0661 PROTAC | [53] |
Synovial sarcoma | BRD9 | dBRD9-A PROTAC | [75] |
CFT8634 | [76] | ||
FHD-609 | [76] | ||
Cervical carcinoma | BET proteins | MZ1 PROTAC | [29] |
Hematological tumors | |||
Diffuse large B-cell lymphoma | BTK | UBX-382 PROTAC | [77] |
Chronic myeloid leukemia | BCR-ABL1 | DMP11 PROTAC | [78] |
GMB-475 PROTAC | [79] | ||
LIN28 | RNA-PROTAC | [80] | |
STAT5 | AK-2292 PROTAC | [81] | |
MLL-rearranged leukemia | IKZF | MS40 PROTAC | [82] |
Acute myeloid leukemia | CDK2/CDK5 | dTAG tool | [43] |
Anaplastic large cell lymphoma | NPM-ALK fusion | dALK opto-PROTAC | [67] |