Drug intelligence / Profile preview

UK-101

Development stage
Preclinical
Lead developer
University of Kentucky
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

UK-101 is a small molecule inhibitor that selectively targets the immunoproteasome catalytic subunit LMP2 (Low Molecular Mass Polypeptide 2), also known as PSMB9. Developed by researchers at the University of Kentucky, UK-101 acts by covalently modifying the LMP2 subunit, which is often upregulated in various cancers and inflammatory conditions. In preclinical studies, particularly in pancreatic cancer models, UK-101 has demonstrated the ability to decrease proteasomal proteolytic activity, leading to cell cycle arrest and the induction of apoptosis. It has shown potential in overcoming resistance to standard therapies like gemcitabine.

02

Targets

PSMB6 (Proteasome subunit beta type-6)PSMB7 (Proteasome subunit beta type-7)PSMB10 (Proteasome subunit beta type-10)PSMB5 (Proteasome subunit beta type-5)PSMB8 (Proteasome subunit beta type-8)PSMB9 (Immunoproteasome subunit beta type-1i)

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