QBI Life Sciences: Preservex™ Polymeric Micelles Reduce False Positives In HTS
Contact: Ralph Kauten (608) 441-2950 or RalphK@qbilifesci.com
Second screening of drug compounds affirms reduced promiscuous inhibition
MADISON, Wis. – QBI Life Sciences announced today results of a second drug compound screen, reinforcing the utility of PreserveX™ Polymeric Micelles in high-throughput screening. The announcement was made during a presentation by Vladimir Trubetskoy, QBI Life Sciences’ Director of Polymer Chemistry, at the Society of Biomolecular Sciences (SBS) Annual Meeting in Seattle , Washington .
A second screen of compounds from the University of Wisconsin-Madison Keck Small Molecule Screening Center supports earlier findings that show using PreserveX™ Polymeric Micelles in high-throughput screening reduces promiscuous inhibition resulting in fewer false positives.
The screen resulted in identifying several novel substrates and inhibitors of UGT1A1 in addition to several confirmed structures. These newly identified substrates and inhibitors are being further investigated for building structure activity relationship (SAR) models for this enzyme by QBI Life Sciences and their research collaborators.
UGT1A1 is an important human drug metabolizing enzyme involved into metabolism of many important drugs and molecules including bilirubin, dietary supplements and anticancer agents, such as irinotecan used for colon cancer treatment. Mutations in UGT1A1 are linked to many diseases including Gilbert Syndrome, neonatal bilirubinemia, breast milk jaundice, adverse drug reactions (ADRs) and susceptibility to certain cancers.
This study followed an earlier screen of compounds from the UW-Madison Keck Small Molecule Screening Center , which demonstrated that incorporation of UGT1A1 into PreserveX™ Polymeric Micelles stabilizes UGT, resulting in reduced background and expanded assay dynamic range. It also showed minimized light scattering.
A third screen is scheduled for the end of September.
“By reducing the number of false positives, researchers can focus time and energy on the most promising compounds,” said Ralph Kauten, CEO of QBI Life Sciences. “We believe the incorporation of PreserveX™ Polymeric Micelles into high-throughput screening will result in productivity gains for the drug discovery industry as a whole.”
The work resulting in this discovery is being funded under a grant from the National Institutes of Health (NIH) under the NIH’s Roadmap for Medical Research.
QBI Life Sciences, a division of Quintessence Biosciences, Inc., is the first company to offer novel polymeric micelle solutions to study membrane proteins. QBI Life Sciences has developed valuable drug discovery tools including membrane protein stabilizing reagents, as well as surface coatings for membrane proteins and optimal media for cell-surface proteins. For more information about PreserveX™ Polymeric Micelles or to learn more about QBI Life Sciences, log on to http://www.qbilifesci.com.