Targeting PTP1B with Trodusquemine: A Novel ...

Targeting PTP1B with Trodusquemine: A Novel Approach for Atherosclerosis Management

Author Name : M. Kalyan Bhushan, M. Kaushik Bhushan

ABSTRACT Atherosclerosis, a chronic inflammatory condition marked by the accumulation of cholesterol-rich plaques in arterial walls, poses a significant risk for cardiovascular disease. Emerging evidence implicates the proteintyrosine phosphatase 1B (PTP1B) gene in the pathogenesis of atherosclerosis, where increased PTP1B activity correlates with dyslipidaemia, insulin resistance, and heightened inflammation, exacerbating plaque formation and progression. Targeting PTP1B has thus emerged as a potential therapeutic approach. Trodusquemine, an allosteric inhibitor of PTP1B, has shown promise in preclinical studies for its ability to mitigate atherosclerosis progression. By inhibiting PTP1B activity, Trodusquemine effectively suppresses foam cell formation, reduces inflammatory cytokine secretion, and improves lipid profiles, thereby attenuating plaque development. Additionally, Trodusquemine exerts pleiotropic effects on various cellular processes implicated in atherosclerosis, including endothelial dysfunction and immune cell activation.