Table 1.

Key cancer targets that have been successfully targeted with small molecular PROTACs

E3 ligase	Target	Cancer/cell type	Study type	Refs
MDM2	AR	Hela cells	In vitro	[11]
	BRD4	Colon cancer	In vitro	[38]
	PARP1	Breast cancer	In vitro	[39]
IAP	CRABP-2	Fibrosarcoma	In vitro	[41]
	ERα	Breast cancer	In vitro/In vivo	[13, 14]
	BCR-ABL	CML	In vitro	[15, 16]
	AR	Prostate cancer	In vitro	[17]
	TACC3	Fibrosarcoma	In vitro	[19]
VHL	AR	CRPC	In vitro/In vivo	[50, 54]
	ERRα	Breast cancer	In vitro/In vivo	[24]
	RIPK2	Acute monocytic leukemia	In vitro	[24]
	BRD4	Cervical cancer	In vitro	[23, 43]
	BCR-ABL	CML	In vitro	[44]
	TBK1	KRAS-mutant NSCLC	In vitro	[45]
	TRIM24	AML	In vitro	[46]
	FLT-3	AML	In vitro	[47]
	ALK	NSCLC; ALCL	In vitro/In vivo	[48]
	FAK	Breast cancer; Prostate cancer	In vitro	[49]
	P38	Breast cancer	In vitro	[51]
	BCL-XL	T-ALL; SCLC; Breast cancer	In vitro/In vivo	[35, 36]
CRBN	BETs	AML	In vitro	[25]
	BRD4	Burkitt’s lymphoma	In vitro	[22]
	PCAF/GCN5	Acute monocytic leukemia	In vitro	[65]
	ALK	NSCLC; ALCL; Neuroblastoma	In vitro	[105]
	BTK	Burkitt’s lymphoma	In vitro	[60, 61]
	CDK9	Colon cancer; Breast cancer	In vitro	[57]
	CDK6	Multiple myeloma; AML	In vitro	[58, 59]
	BCL-XL	T-ALL; SCLC	In vitro	[34]
	STAT3	AML, ALCL	In vitro/In vivo	[1, 2]
	MDM2	B-ALL	In vitro/In vivo	[40]
DCAF16	FKBP12	HEK293 Cells	In vitro	[70]
RNF4	BRD4	Hela cells	In vitro	[71]
RNF114	BRD4	Breast cancer	In vitro	[72]

Note: CML, Chronic myelogenous leukemia; CRPC, Castration resistant prostate cancer; NSCLC, Non-small cell lung cancer; ALCL, Anaplastic large cell lymphoma; AML, Acute myeloid leukemia; T-ALL, T-cell acute lymphoblastic leukemia; SCLC, Small-cell lung cancer; B-ALL, B-cell acute lymphoblastic leukemia