. 2022 Mar 2;12(3):392. doi: 10.3390/biom12030392

Table 1.

Targeting proteins for inhibiting TAM recruitment and polarization.

Target	Inhibitor	Tumor	Study Design	Anti-Tumor Mechanism	Ref.
Inhibit recruitment of TAMs
CCL2	Celecoxib	GBM	C57BL/6 J mice + Eagle medium F-12	Decrease pNF-κB expression	[9]
	6-Shogaol	BC	MDA-MB-231/A549/4T1 cell line + Leibovitz’s L-15, F-12K, etc. medium	Decrease CCL2 by inhibiting STAT3 activation	[18]
CCR2	Losartan	BC	4T1-Luc, etc. cell line + ICR, etc. mice	Inhibit CCL2-induced p-ERK1/2	[19]
CXCL1	Aiduqing	BC	4T1/293 T cell line + BALB/c mice + DMEM/RPMI-1640	Decrease Tregs differentiation and infiltration	[20]
CCR5	Maraviroc	BC	MDA-MB-436/4T1.2 cell line + DMEM	Inhibit TAM recruitment	[21]
CCL5	HuR	BC	MCF-7/MDA-MB-231 cell line + DMEM	Inhibit CCL5 expression	[22]
CCR1	J113863	FA	NCTC 2472 cell line + NCTC 135 medium + C57BL/6, C3H/He mice	Inhibit thermal hyperalgesia	[23]
CXCR7	CCX771	BC	4T1 cell line + DMEM + BALB/c mice	Reduce p-STAT3 activation	[24]
CXCL8	IFN-γ	PC	BxPC-3, etc. cell line + C57BL/6 mice	Inhibit macrophages traffic	[25]
	ACPP Antibody	NPC	C666-1 cell line + RPMI 1640 medium	Inhibit PI3K/AKT pathway	[26]
IL-1β	Anakinra	BC	4T1 cell line + α-MEM + BALB/c mice	Inhibit CCL5, CXCX12 expression	[27]
IL-6	Siltuximab	OC	Tissue from ovarian cancer patients + endotoxin-free RPMI/DMEM medium	Reduce cytokine and chemokine, inhibit IL-6 signaling	[28]
S100B	Duloxetine	GLA	GL261-Luc/KR158B cell line + DMEM + CX₃CR₁^GFP mice	Decrease CCL2 expression	[29]
CSF-1R	PLX3397	HCC	Hep3B/HepG2/THP-1, etc. cell line + OPN knockout C57BL/6 mice	Inhibit PPARγ activity to reduce TAM numbers	[30]
A2A	SCH58261	HCC	Tissue from HCC patients	Reduce Akt and ERK phosphorylation to reduce TAM numbers	[31]
MEK	GDC-0623	PC	PDA30364 cell line + pan monocyte isolation kit	Exterminate M2 macrophages	[32]
Inhibit the polarization of TAMs
STAT6	Gefitinib	LLC	Cells from Chinese Academy of Sciences + DMEM + C57BL/6 mice	Inhibit IL-13/STAT6 pathway	[33]
CSF-1R	BLZ945	GLA	U-87 MG, etc. cell line + RCAS-hPDGF-B/Nestin-Tv-a; Ink4a/Arf^−/− mice	Inhibit heterotypic signaling	[34]
YAP	Ovatodiolide	CRC	HT-29, etc. cell line + Serum-Free Medium + NOD, SCID, BALB/c mice	Suppress IL-6 induced pathway	[35]
IL-6R	CPEB3	CRC	SW480/HCT116/LoVo, etc. cell line + BALB/c mice	Inhibit epithelial-mesenchymal transition	[36]
Ang-2	AS16	SA	Plasmid pPIC3.5K + BMMY + SD rat	Inhibit M2 polarization	[37]
Integrin β3	Sc-7312	BC	4T1/HEK293T cell line + RPMI-1640 and DMEM + BALB/c mice	Inhibit integrin β3 induced PPARγ activity	[38]
EP4	TP-16	CRC	CT26/4T1/HCT116 cell line + DMEM and F12 medium + C57BL/6, etc. mice	Reprogram IMCs, enhance tumor elimination	[39]
CD206	RP-182	PC	CD206^high M2-like macrophages + KPC, KP16 mice	Reduce M2-like TAMs, improve antitumor immune responses	[40]
PlGF	HRG	BT	T241/Panc02 cell line + C57BL/6, BALB/c mice	Promote vessel normalization, improve tumor perfusion	[41]

GLA: glioma; GBM: glioblastoma multiforme; HCC: hepatocellular carcinoma; PC: prostate cancer; CRC: colorectal cancer; PDAC: pancreatic ductal adenocarcinoma; BC: breast cancer; BT: breast tumor; BPT: breast phyllodes tumors; SC: squamous cancer; LC: lung cancer; LCC: Lewis lung cancer; SCLC: small cell lung cancer; NSCLC: non-small cell lung cancer; NPC: nasopharyngeal carcinoma tumor; FA: fibrosarcoma; SA: sarcoma; OC: ovarian cancer; CCL2: C–C motif chemokine 2; CXCL1: C–X–C motif chemokine 1; CXCR1: C–X–C motif chemokine 1; CCR2: C–C motif chemokine 2; IL-1β: interleukin 1 β: CSF-1R: colony-stimulating factor 1 receptor; YAP: Yes-associated protein; AMPK: AMP-activated protein kinase; Ang2: angiopoietin-2; MEK: MAPK/extracellular signal-regulated kinase; EP4: prostaglandin E2 (PGE2) receptor 4; HuR: human antigen R; CPEB3: Cytoplasmic polyadenylation element binding protein 3; AS16: 16-kilodalton protein: HRG: histidine-rich glycoprotein; STAT: signal transducer and activator of transcription.