From: Proteolysis-targeting chimeras (PROTACs) in cancer therapy
Target | PROTAC | PROTAC structure | Cancer | Ref | Target | PROTAC | PROTAC structure | Cancer | Ref |
---|---|---|---|---|---|---|---|---|---|
BRD4 | ARV-825 |
| BL | [39] | BRD4 | SNIPER(BRD4)-1 |
| BC | [89] |
BRD4 | dBET1 |
| AML | [12] | BRD4 | A1874 |
| CRC, M, BL, et al. | [90] |
BRD4 | MZ1 |
| CC | BRD4 | CLIPTAC-BRD4 |
| CC, M, CRC | [26] | |
BRD4 | dBET6 |
| T-ALL | [92] | BRD4 | opto-dBE T1 |
| MM, PC, ALCL, et al. | [22] |
BRD4 | ZXH-3-26 |
| MM | [93] | BRD4 | PROTAC4 |
| BC, PC | [23] |
BRD4 | ARV-771 |
| PC | [76] | BRD4 | pc-PROTAC1 |
| BL, HCC | [25] |
BRD4 | macroPROTAC-1 |
| PC, AML | [94] | BRD4 | PHOTAC-I-3 |
| ALL | [21] |
BRD4 | BETd-246 |
| TNBC | [95] | BRD4 | photoPROTAC-1 |
| BL | [20] |
BRD4 | BETd-260 |
| AML, ALL | [96] | BRD4 | PROTAC3 |
| CC | [24] |
BRD4 | KB02-JQ1 |
| / | [97] | EGFR | compound 1 |
| OC, CC | [79] |
BRD4 | XH2 |
| BC | [98] | EGFR | compound 14o |
| NSCLC | [99] |
BRD4 | DP1 |
| DLBCL | [100] | EGFR | compound P3 |
| LC | [101] |
CDK4/6 | BSJ-03-123 |
| AML | [102] | EGFR | MS154 |
| LC | [103] |
CDK4/6 | pal-pom |
| TNBC | [104] | EGFR | DDC-01-163 |
| LC | [80] |
CDK4/6 | BSJ-02-162 |
| MCL | [77] | AURORA-A | JB170 |
| AML, OS, NB, HCC | [81] |
CDK4/6 | BSJ-04-132 |
| T-ALL | [77] | Raf | P4B |
| M, CRC | [60] |
CDK4/6 | YX-2-107 |
| ALL | [78] | AR | PROTAC 14 |
| CC | [7] |
CDK4/6 | compound 11 |
| M | [105] | AR | ARCC-4 |
| PC | [106] |
CDK4/6 | PROTAC 34 |
| ALL, AML, MM, TNBC | [107] | AR | TD-802 |
| PC | [108] |
AR | MTX-23 |
| PC | [109] | BRD7/9 | ACBI1 |
| AML, M, NSCLC | [83] |
AR | ARD-69 |
| PC | [110] | CDK2/5 | TMX-2172 |
| OC | [84] |
AR | SNIPER(AR)-51 |
| PC | [111] | CDK8 | JH-XI-10-02 |
| T-ALL | [112] |
ALK | MS4077 |
| NSCLC, ALCL | [113] | CDK9 | PROTAC 3 |
| CRC | [114] |
ALK | TL13–12 |
| ALCL, NB, NSCLC | [52] | CDK9 | THAL-SNS-032 |
| T-ALL | [38] |
ALK | opto-dALK |
| NSCLC, ALCL | [22] | CDK9 | B03 |
| AML | [115] |
ALK | SIAIS117 |
| NSCLC, ALCL | [116] | CDK9 | compound F3 |
| PC | [117] |
BLK | PROTAC 7 |
| CML | [118] | Cdc20 | CP5V |
| BC | [119] |
BRD7/9 | dBRD9 |
| AML | [82] | c-Met | PROTAC 7 |
| TNBC, GC | [79] |
BRD7/9 | VZ185 |
| MRT | [120] | CREPT | PRTC |
| PaC | [121] |
CYP1B1 | compound 6C |
| PC | [122] | MEK1/2 | MS432 |
| CRC, M | [86] |
DHODH | probe 10 |
| PaC | [123] | Ras | LC-2 |
| NSCLC, PaC | [87] |
ER | ERD-308 |
| BC | [124] | GSPT1 | CC-885 |
| AML | [125] |
ER | compound I-6 |
| BC | [126] | PLK1 | HBL-4 |
| AML | [127] |
ER | TD-PROTAC |
| BC | [128] | SLC9A1 | d9A-2 |
| CML | [129] |
ER | SNIPER(ER)-87 |
| BC | [89] | TACC3 | SNIPER(TACC3)-1 |
| FS, OS, CRC | [130] |
ERK1/2 | ERK-CLIPTAC |
| CC, M, CRC | [26] | TRIM 24 | dTRIM24 |
| AML | [131] |
FLT-3 | FLT-3 PROTAC |
| AML | [132] | TRKA/C | CG416 |
| CRC, AML | [133] |
HER2 | PROTAC 1 |
| OC, BC | [79] | Wee1 | ZNL-02-096 |
| OC, T-ALL | [88] |
MEK1/2 | compound 3 |
| M | [85] | α1A-AR | α1A-AR |
| PC | [134] |