SR31747A

SR31747A is a synthetic small molecule that acts as a peripheral sigma receptor ligand with both immunomodulatory and antitumor activities. It binds to multiple targets in human cells, including the sigma receptors (notably sigma-1 and sigma-2), sterol regulatory element-binding protein 1 (SRBP1), HSI, and its relative SRBP2. Mechanistically, it functions primarily as an antagonist at the sigma receptors and modulates other proteins involved in sterol metabolism. Preclinically, it has demonstrated the ability to block proliferation of human and mouse lymphocytes, modulate pro-inflammatory and anti-inflammatory cytokine expression, protect animals from acute graft-versus-host disease, sepsis models (staphylococcal enterotoxin B or lipopolysaccharide-induced lethality), rheumatoid arthritis models, and inhibit tumor cell line proliferation both in vitro and in vivo. In animal studies with mammary and prostate cancer xenografts, daily treatment reduced tumor incidence and growth by over 40%. The drug was developed by Sanofi for oncology indications such as prostate cancer but development appears to have been discontinued after phase II trials[1][2][3][5][6].

Other names

Arylacenamide