Targeting STAT3 in Cancer Immunotherapy

Zou, Sailan; Tong, Qiyu; Liu, Bowen; Huang, Wei; Tian, Yan; Fu, Xianghui

doi:10.1186/s12943-020-01258-7

Molecular Cancer

Table 1 Studies of STAT3 inhibitors on pre-clinical cancer models

From: Targeting STAT3 in Cancer Immunotherapy

Therapy	Type	Agent	Cell line tested	Mouse model	Functional outcome	Ref
Direct inhibitors	Peptides	DBD-1	Melanoma, Myeloma	n/d	↑Apoptosis; ↓Proliferation	[87]
		ISS-610 prodrugs	BC	n/d	↑Apoptosis	[88]
		PY*LKTK	NIH3T3/v-Src or v-Ras	n/d	↓Transformation	[89]
	Small molecules	6o	BC, PC, PCa, NSCLC	n/d	↑Apoptosis; ↓Proliferation	[90]
		FLLL32	BC, PC	Xenograft: MDA-MB-231, PANC-1	↑Apoptosis; ↓Proliferation, Vascularization	[91]
		HJC0152	Glioblastoma	Xenograft: U87	↑Apoptosis; ↓Metastasis, Proliferation	[92]
		LL1	CRC	Xenograft: HCT116	↑Apoptosis; ↓Metastasis, Proliferation	[93]
		LLL-3	BC, Glioblastoma	Xenograft: U87	↑Apoptosis; ↓Metastasis, Proliferation	[94]
		LLL12	HCC	Xenograft: SNU398	↑Apoptosis; ↓Proliferation	[95]
		LYW-6	CRC	AOM/DSS induced CRC model; Xenograft: HCT116	↑Apoptosis; ↓Metastasis, Proliferation	[96]
		Nitidine chloride	Oral cancer	Xenograft: HSC3	↑Apoptosis; ↓Proliferation	[97]
		SD-36	BC, CRC, Leukemia, Lymphoma	Xenograft: MOLM-16, SUP-M2, SU-DHL-1	↑Apoptosis; ↓Proliferation	[98]
		Stattic	BC	n/d	↑Apoptosis	[99]
		STX-0119	n/d	Humanized NOG-dKO model	↑Anti-tumor immunity; ↓Proliferation	[100]
		S3I-1757	Melanoma	Xenograft: B16-F10	↓Proliferation	[101]
		S3I-201	BC	Xenograft: MDA-MB-231	↑Apoptosis; ↓Proliferation	[102]
		CPA-7	BC, CRC, Melanoma, PCa, NSCLC	Xenograft: CT26	↑Apoptosis; ↓Proliferation	[103]
		C48	BC, CML, Melanoma, PCa	Xenograft: MDA-MB-468, C3L5	↓Proliferation	[104]
		GPA512	PCa	Xenograft: DU145	↓Proliferation	[105]
		MMPP	BC, CRC, PCa, HCC, Lung, Ovary and Skin cancer	Xenograft: Patient-derived NSCLC, NCI-H460	↑Apoptosis; ↓Proliferation	[106]
	Oligonucleotides	InS3-54A18	BC, NSCLC	Xenograft: A549	↓Metastasis, Proliferation	[107]
	Oligonucleotides	STAT3 hpdODN	CRC	n/d	↓Proliferation	[108]
Indirect inhibitors	JAK2	INCB16562	Leukemia	MPLW515L model	↓Proliferation	[109]
	JAK2	TG101209	Leukemia	AML1-ETO9a leukemia model	↑Apoptosis; ↓Proliferation	[110]
	EGFR	JND3229	BaF3	Xenograft: BaF3-EGFR	↓Proliferation	[111]
	FGFR, VEGFR	ODM-203	Bladder cancer, NSCLC, GC	Xenograft: H1581, KMS11, RT4, SNU16	↑Anti-tumor immunity; ↓Metastasis, Proliferation	[112]
Combination	Direct inhibitor	HJC0152	BC, THP1	Xenograft: 4T1	↑Anti-tumor immunity; ↓Proliferation	[113]
	STING agonist	c-diAM (PS)2	BC, THP1	Xenograft: 4T1	↑Anti-tumor immunity; ↓Proliferation	[113]
	JAK1/2 inhibitor	Ruxolitinib	PC	Xenograft: PANC02-H7	↑Anti-tumor immunity; ↓Proliferation	[114]
	Anti-PD-1 antibody	RMP1-14	PC	Xenograft: PANC02-H7	↑Anti-tumor immunity; ↓Proliferation	[114]
	SRC, ABL inhibitor	Dasatinib	n/d	Tgfbr1/Pten 2cKO model	↑Anti-tumor immunity; ↓Proliferation	[115]
	Anti-CTLA-4 antibody	9D9	n/d	Tgfbr1/Pten 2cKO model	↑Anti-tumor immunity; ↓Proliferation	[115]
	VEGFR2 antibody	DC101	n/d	Xenograft: LLC, CT26	↓Proliferation; ↑Anti-tumor immunity, Vascular normalization	[116]
	STING agonist	cGAMP, RR-CDA	n/d	Xenograft: LLC, CT26		[116]

AOM/DSS Azoxymethane/dextran sodium sulfate, BC Breast cancer, CML Chronic myelogenous leukemia, CRC Colorectal cancer, GC Gastric cancer, HCC Hepatocellular carcinoma, LLC Lewis lung carcinoma, MPLW515L Somatic mutations at codon 515 of the thrombopoietin receptor, NSCLC Non-small cell lung cancer, PC Pancreatic cancer, PCa Prostate cancer, n/d Not determined, hpdODN hairpin decoy oligodeoxynucleotide

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ISSN: 1476-4598

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