Novel glyoxalase-I inhibitors possessing a "zinc-binding feature" as potential anticancer agents.

ABSTRACT:

Background

The glyoxalase system including two thiol-dependent enzymes, glyoxalase I (Glo-I) and glyoxalase II, plays an important role in a ubiquitous metabolic pathway involved in cellular detoxification of cytotoxic 2-oxoaldehydes. Tumor cells have high glycolytic activity, leading to increased cellular levels of these toxic metabolites. The increased activity of the detoxification system in cancerous cells makes this pathway a viable target for developing novel anticancer agents. In this study, we examined the potential utility of non-glutathione-based inhibitors of the Glo-I enzyme as novel anticancer drugs.

Methods

Computer-aided drug design techniques, such as customized pharmacophoric features, virtual screening, and flexible docking, were used to achieve the project

SUBMITTER: Al-Balas QA 

PROVIDER: S-EPMC4993257 | biostudies-literature | 2016

REPOSITORIES: biostudies-literature