Table 2.

Inhibition of FAP in CRC treatment and its outcomes, preclinical phases

FAP inhibitor	FAP inhibitor type	Study type	Cell line/tumor model	Assay	Results	Refs
Oxytocin	peptide hormone	In vitro	Ls174t and SW480	Fluorescent IHC and invasion assay	Decrease in tumor cells migration	[115]
BF211-03	Dipeptide (Z-Gly-Pro)-conjugated BF211 prodrug	In vivo	HCT-116 xenograft model	Western blot, Cytotoxicity assay, and measuring body weight and tumor volume	Tumor selectivity and anti-tumor effects of prodrug were observed	[114]
pcDNA3.1/V5-His-TOPO-Fap	DNA vaccine	In vivo	BALB/c mice with CT26 cells, xenograft model	IHC and T cell infiltration	Increase host immune responses, CD8+ T cells activity, and survival while used in combination with chemotherapy	[16]
pFAP-vaccine	DNA vaccine	In vivo	CT26 mouse CRC xenograft model	IHC and cell staining	Primary tumor and pulmonary metastases suppression, promotion of T-cell-mediated host immune responses, increased survival	[89]
PT‑100 combined with oxaliplatin	dipeptidyl peptidase inhibitor and chemotherapeutic drug	In vivo	CT26 mouse CRC xenograft model	Western blot analysis, Flow cytometry, and RT‑qPCR	better the response to chemotherapy was observed, declined the activity of immune tumor‑promoting cells, inhibition of angiogenesis	[116]
M83	FAP/prolyl oligopeptidase inhibitor	In vivo	HCT116 mouse CRC model	IHC and Immunoblot Analysis	Decrease angiogenesis and tumor growth	[117]

DNA Deoxyribonucleic Acid, RT‑qPCR Reverse‑transcription quantitative polymerase chain reaction