Drug intelligence / Profile preview

Na-AuPT

Development stage
Preclinical
Modality
Light/Condition-Responsive Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules
Administration
Not Specified (preclinical In Vitro And In Vivo Studies Used Intraperitoneal Injection In Mice)[1]
01

Overview

Na-AuPT is a **novel, water-soluble gold(I) complex** developed as a **metal-based proteasome inhibitor** for anticancer therapy. It inhibits both 20S proteasome catalytic subunits and 19S proteasome-associated deubiquitinases (DUBs), thereby **blocking the ubiquitin-proteasome system (UPS)** which is essential for protein degradation in cells. Na-AuPT exerts significant in vitro and in vivo antitumor activity by inducing cell death and apoptosis in a variety of cancer cell lines, and in animal models this compound demonstrated tumor growth inhibition. Mechanistic studies show accumulation of ubiquitinated proteins and activation of apoptosis-related proteins (cleaved caspase 3, Bax). Na-AuPT is a preclinical candidate and, to date, has not been approved or included in advanced clinical trials for human therapy.

Other names
sodium gold(I) complex Na-AuPT
02

Targets

UCHL5 (Ubiquitin carboxyl-terminal hydrolase isozyme L5)USP14 (Ubiquitin carboxyl-terminal hydrolase 14)26S proteasome

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