Table 2.

PLK1 inhibitors combined with targeted therapy.

PLK1 inhibitor	Cancer Type	Interacting Protein	Interacting protein inhibition	Affected process	Affected pathways	Ref
BI2536	KRAS-mutant cancers	ROCK	fasudil	Apoptosis, cell cycle arrest	p21	[46]
BI2536	Esophageal squamous cell carcinoma	mTOR	Rapamycin	Colony formation	S6, 4E-BP1, AKT	[47]
BI2536	Glioblastoma	STAT3	Stattic	Apoptosis	MYC	[48]
BI2536	Glioblastomas	EGFR	Gefitinib and temozolomide	Colony formation, tumor growth	NA	[49]
BI2536	EGFRvIII positive glioma	Src	Saracatinib	Neurosphere formation, cell apoptosis	NOTCH1, SOX2	[49]
BI2536	Castration-resistant prostate cancer	HDAC	Metformin	Colony formation, cell metabolism, tumor growth	TP53	[50]
BI2536	Castration-Resistant Prostate Cancer	PARP	Olaparib	G2/M arrest, colony formation	Ki67, Caspase-3	[51],[52]
BI2536, BI6727	Prostate cancer	HDAC	Valproic acid, Vorinostat	Cell viability, colony formation	NA	[53]
BI2536	Chronic myeloid leukemia	Bcr-Abl fusion protein	Imatinib	Cell cycle, apoptosis	NA	[54]
BI2536	Bcr-Abl-positive leukemia	Proteasome	Bortezomib	Cell viability	STAT5	[55]
BI2536	Squamous cell carcinoma of the head and neck	Proteasome	Bortezomib	Cell proliferation	NA	[56]
BI6727	Melanoma	MEK	JTP-74017	Apoptosis, cell cycle arrest	TP53	[58]
BI6727	Melanoma	NOTCH	MK0752	Apoptosis, colony formation	MAPK, PI3K, RAS, Apobec3G, BTK, FCER1G	[59]
BI6727	Non-small cell lung cancer	Survivin	Sepantronium	Apoptosis, colony formation	NA	[60]
BI6727	Non-small cell lung cancer	EGFR	Erlotinib	G2/M arrest and apoptosis	PARP	[61],[62]
BI6727	Paclitaxel-resistant lung cancer	USP7	P22077	Apoptosis	MDR1/ABCB1	[63]
BI6727	NRAS-mutant non-small cell lung cancer	RAF	LXH254	G2/M phase arrest, colony formation	NA	[65]
BI6727	Non-small cell lung cancer	CRBN	CC-885	Cell death, cell cycle	PLK1, TCTP, MYTL	[66]
BI6727	Double-hit lymphoma	BCL-2	ABT-199	Tumorigenicity	NA	[68]
BI6727	Double-hit lymphoma	HDAC	Vorinostat	Cell apoptosis	NA	[69]
BI6727	Non-Hodgkin's lymphoma	HDAC	Belinostat	Cell apoptosis, cell viability, cell cycle, tumor growth	H2AX, Caspase-3, PARP	[70]
BI6727	Anaplastic thyroid cancer	PI3K	BKM120	Mitotic slippage, endoreduplication	AKT, HH3, H2AX, PARP	[71]
BI6727	Medulloblastoma	BRD4	MK-8628	Cell viability	BRD4, CCND1	[72]
BI6727	TP53-mutated hepatocellular carcinoma	BIRC5	YM155	Cell viability, apoptosis, tumor growth	NA	[73]
SBE13	Multiple cancer cells	PKCβ	Enzastaurin	Cell proliferation, cell cycle	PLK1, GSK3B	[74]
GSK461364	Castration-resistant prostate cancer	BRD4	JQ1	Colony formation, tumor growth	AR/Ki67, Caspase-3	[75]
GW843682X	Triple-negative breast cancer	TNKS1	XAV939	Cell invasion and migration, apoptosis	PARP cleavage	[76]
RO3280	Non-small cell lung cancer	TRAIL receptors	rhTRAIL	Cell apoptosis, cell cycle, tumor growth	MCL-1, PARP	[77]