J Enzyme Inhib Med Chem. 2017 Dec;32(1):203-207. doi: 10.1080/14756366.2016.1247055.

Screening assay for inhibitors of a recombinant Streptococcus pneumoniae UDP-glucose pyrophosphorylase.

Zavala A1, Kovacec V1, Levín G2, Moglioni A3, Miranda MV2, García E4, Bonofiglio L1, Mollerach M1.

Author information

Abstract

The UDP-glucose pyrophosphorylase of Streptococcus pneumoniae (GalUSpn) is absolutely required for the biosynthesis of capsular polysaccharide, the sine qua non virulence factor of pneumococcus. Since the eukaryotic enzymes are completely unrelated to their prokaryotic counterparts, we propose that the GalU enzyme is a critical target to fight the pneumococcal disease. A recombinant GalUSpnwas overexpressed and purified. An enzymatic assay that is rapid, sensitive and easy to perform was developed. This assay was appropriate for screening chemical libraries for searching GalU inhibitors. This work represents a fundamental step in the exploration of novel antipneumococcal drugs.

KEYWORDS:

Antibacterial target; UTP:glucose 1-phosphate uridylyltransferase; pneumococcus; virulence inhibitors

PMID: 28114831 DOI: 10.1080/14756366.2016.1247055

[PubMed - in process]