Drug intelligence / Profile preview

A2ti-1

Development stage
Unknown
Modality
Small Molecules
01

Overview

A2ti-1 is a selective, small molecule inhibitor of the protein-protein interaction (PPI) between Annexin A2 (ANXA2) and S100 calcium-binding protein A10 (S100A10), which together form the heterotetrameric annexin A2/S100A10 complex (A2t). By binding to S100A10, A2ti-1 disrupts the assembly of this complex with an IC50 of 24 μM. Disruption of the A2t complex impairs non-canonical endocytic viral entry and intracellular trafficking, which has been shown to prevent human papillomavirus type 16 (HPV16) infection in vitro. Additionally, A2ti-1 has been investigated in preclinical models for its potential to reduce hepatic fibrosis, suppress stellate cell activation, and modulate smooth muscle cell proliferation in atherosclerosis.

Other names
2-[4-(2-ethylphenyl)-5-o-tolyloxymethyl-4H-[1,2,4]triazol-3-ylsulfanyl]acetamide2-[[4-(2-ethylphenyl)-5-[(2-methylphenoxy)methyl]-4H-1,2,4-triazol-3-yl]thio]-acetamideS100A10-ANXA2 heterotetramer inhibitor-1S-100A10-ANXA2 heterotetramer inhibitor-1S 100A10-ANXA2 heterotetramer inhibitor-1S100A10-ANXA2 inhibitorS-100A10-ANXA2 inhibitorS 100A10-ANXA2 inhibitor
02

Targets

S100A10 (Exosome complex component 6)

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