Targeting Mast Cells Tryptase in Tumor Microenvironment: A Potential Antiangiogenetic Strategy

Table 1

All preclinical studies mentioned above that have considered gabexate mesylate.

Author, reference, year	Drug/s	Tumor target	Molecular mechanisms of action	Results
Yoon et al. [46] 2004	gabexate mesylate	several human colon cancer cell lines	(1) down-regulation of MMPs; (2) inhibition of uPA-plasmin system	inhibition of angiogenesis, tumor cell growth, invasion, metastasis
Brandi et al. [47] 2012	(1) gabexate mesylate; (2) gabexate mesylate plus cetuximab	several human colorectal cancer cell lines (wt/mut KRAS, BRAF, PIK3CA)	not analyzed	(1) inhibition of tumor cell growth, angiogenesis, invasion, metastasis; (2) antitumoral efficacy of the combination therapy was not superior than gabexate mesylate alone
Uchima et al. [48] 2003	gabexate mesylate	several human pancreatic cancer cell lines	down-regulation of uPA, TAT, PAT, MMPs, TGF-β1, VEGF	inhibition of angiogenesis, cell growth, invasion, metastasis

MMPs, Metalloproteinases; uPA, urokinase-type plasminogen activator; wt, wild-type; mut, mutated; TAT, Tumor-associated trypsinogen; PAT, Pancreatic acinar trypsinogen; TGF-β1, Tumor growth factor-beta1; VEGF, Vascular endothelial growth factor.