Table 3.
The structures of PROTAC molecules targeting apoptosis or angiogenesis in cancers. (red: POI ligand; yellow: E3 ligand)
| Target | PROTAC | PROTAC structure | Cancer | Ref | Target | PROTAC | PROTAC structure | Cancer | Ref |
|---|---|---|---|---|---|---|---|---|---|
| Bcl-xL | DT2216 |
|
T-ALL | [167] | BCR-ABL | DAS-6-2-2-6-CRBN |
|
CML | [171] |
| Bcl-xL | XZ739 |
|
T-ALL | [184] | BCR-ABL | Azo-PROTAC-4C |
|
CML | [19] |
| Bcl-xL | compound 8a |
|
TL | [185] | BCR-ABL | SNIPER(ABL)-38 |
|
CML | [89] |
| Bcl-xL | XZ424 |
|
T-ALL | [168] | BCR-ABL | compound 19 |
|
CML | [186] |
| Bcl-xL | PROTAC 6 |
|
AML | [187] | BCR-ABL | GMB-475 |
|
CML | [172] |
| PARP1 | compound 2 |
|
CRC | [188] | BCR-ABL | GMB-805 |
|
CML | [189] |
| PARP1 | iRucaparib-AP5 |
|
CC, RCC, BC, PC | [170] | BCR-ABL | SIAIS178 |
|
CML | [190] |
| PARP1 | compound 3 |
|
TNBC | [191] | BCR-ABL | BT1 |
|
CML | [192] |
| PARP1 | SK-575 |
|
BC, CRC, PC, PaC | [169] | AKT | INY-03-041 |
|
BC | [173] |
| Bcl-2 | C5 |
|
CC, CML, NSCLC | [174] | eIF4E | PROTAC 23a |
|
TNBC, CML | [176] |
| Bcl-6 | PROTAC 15 |
|
DLBCL | [193] | HDAC1/2/3 | PROTAC 4 |
|
CRC | [194] |
| c-IAP | compound 6 |
|
FS | [175] | HDAC1/2/3 | XZ9002 |
|
TNBC | [195] |
| CK2 | PROTAC 2 |
|
TNBC, NSCLC | [196] | HDAC6 | PROTAC 4 |
|
OSCC, GB | [197] |
| CRABP I/II | compound 4b |
|
NB | [8] | HDAC6 | degrader 12d |
|
MM | [198] |
| CRABP I/II | compound 6 |
|
FS | [175] | HDAC6 | NP8 |
|
MM, CC | [199] |
| CRABP I/II | β-NF-ATRA |
|
BC, NB | [140] | HDAC6 | NH2 |
|
MM, CC | [200] |
| eEF2K | compound 11l |
|
BC | [201] | HDAC6 | P1 |
|
MM | [202] |
| HDAC6 | compound 3j |
|
MM | [203] |
CBP/ p300 |
dCBP-1 |
|
MM | [181] |
| Mcl-1 | dMCL1-2 |
|
MM | [177] | RIPK2 | PROTAC_RIPK2 |
|
BC, AML | [17] |
| Mcl-1 | C3 |
|
CC, CML, NSCLC | [174] | SGK3 | SGK3-PROTAC1 |
|
BC | [204] |
| MDM2 | MD-224 |
|
ALL, AML | [179] | SirT2 | PROTAC 12 |
|
CC | [182] |
| MDM2 | degrader 32 |
|
ALL | [178] | VEGFR2 | PROTAC-5 |
|
/ | [183] |
| PI3K | compound D |
|
HCC | [180] |