Maybridge's Hitfinder collection has helped scientists at the University of Minnesota identify and characterise a small-molecule inhibitor that could enable the development of anti-inflammatory drugs.
Prof David Bernlohr, head of the department of biochemistry, molecular biology and biophysics at the University of Minnesota, and his team used the Hitfinder screening compound collection in studies of fatty-acid-binding protein (FABP) inhibitors.
The collection helped the team to identify several strong leads - compounds that hold the potential for blocking FABP - which is part of the body's inflammatory and metabolic response pathway.
Ultimately, from this library they identified HTS01037, a pan-specific FABP inhibitor with broad anti-inflammatory properties.
'Molecular disruption of the lipid carrier AFABP/ap2 in mice has been found to result in improved insulin sensitivity, protection from atherosclerosis, as well as reduction in LPS-stimulated inflammation,' said Prof Bernlohr.
'We were therefore interested in investigating the efficacy of small-molecule inhibitors in defining the mechanisms of AFABP/aP2 action that could ultimately deliver a pharmacologically beneficial compound,' he said.
'To achieve this we required a good quality chemical screening library as an essential starting point,' he added.
Prof Bernlohr selected the Maybridge Hitfinder collection because of its ease of use, broad chemical coverage, high chemical and structural diversity, simplicity of format and organisation in 384-well formats.
From this initial study, the Bernlohr group has been able to expand its analysis of FABP inhibitors and use them to probe FABP function in a variety of cells and systems.
The Maybridge Hitfinder collection is an offering of drug-like screening compounds that maintains the structural diversity of the Maybridge Screening Collection by using an industry-standard clustering algorithm to select a statistically representative sample of the full collection.
