Proteolysis-targeting chimeras (PROTACs) in cancer therapy

Table 3 The structures of PROTAC molecules targeting apoptosis or angiogenesis in cancers. (red: POI ligand; yellow: E3 ligand)

Target	PROTAC	Cancer	Ref	Target	PROTAC	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]

ISSN: 1476-4598