Drug intelligence / Profile preview

UIC novel inhibitor

Development stage
Preclinical
Lead developer
University of Illinois College of Medicine
Modality
Small Molecules
01

Overview

UIC novel inhibitor is a small molecule metabolic inhibitor targeting pyruvate dehydrogenase kinase 1 (PDK1), developed by researchers at the University of Illinois College of Medicine (Peoria). It is currently in preclinical development for the treatment of glioblastoma (GBM). The compound works by inhibiting PDK1, which is a key regulator in the metabolic reprogramming of cancer cells, effectively shifting the metabolism of GBM cells from glycolysis (the Warburg effect) to oxidative phosphorylation. This shift results in increased reactive oxygen species (ROS) production, decreased lactate release, and induction of G2/M cell cycle arrest. In preclinical studies, the UIC novel inhibitor has demonstrated the ability to significantly reduce cell viability, migration, and invasion in U87 glioblastoma models, showing superior efficacy compared to the PDK1 inhibitor dichloroacetate (DCA). In vivo mouse models have shown that treatment leads to reduced tumor burden and prolonged survival.

02

Targets

PDK (Pyruvate dehydrogenase kinase isoform 1)

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