c2

c2 is an investigational cyclic peptide derived from the structure of human group IIA secreted phospholipase A2 (hGIIA). Developed by Prof. Paul de Souza and collaborators at Western Sydney University, c2 acts as a phospholipase A2 (PLA2) inhibitor that specifically targets protein-protein interactions (PPIs) rather than enzymatic activity. Its mechanism involves suppressing the interaction between hGIIA and the epidermal growth factor receptor (EGFR), which reduces cytosolic PLA2-α activation and prostaglandin E2 production. Additionally, it blocks the interaction between hGIIA and vimentin, triggering aggresome formation and apoptosis in cancer cells. Preclinical studies have demonstrated that c2 is orally bioavailable, cell-permeable, and non-toxic, showing potent anti-tumor activity in xenograft models of prostate cancer. It is currently being evaluated in Phase 0 and early dose-escalation clinical trials for the treatment of prostate cancer, including metastatic castrate-resistant forms.

Other names

PLA2 inhibitor c2PLA-2 inhibitor c2PLA 2 inhibitor c2