SERPINB3-targeting small molecule

SERPINB3-targeting small molecule refers to a class of therapeutic candidates being developed to inhibit the activity of SERPINB3 (also known as squamous cell carcinoma antigen or SCCA). SERPINB3 is a cysteine protease inhibitor often overexpressed in cervical cancer and associated with poor prognosis, radioresistance, and metastasis. It functions by blocking lysosomal-mediated cell death through the inhibition of cathepsins L and S. Researchers at Washington University School of Medicine in St. Louis identified these small molecules using a DNA-encoded library screen of 4.4 billion compounds. Preclinical studies have shown that these molecules can sensitize SERPINB3-overexpressing tumor cells to radiation therapy, although the exact mechanism of action may differ from direct protease inhibition, as in vitro assays did not show a blockade of SERPINB3's inhibitory function.