May 3, 2007 (Press Release) --
Dr. Frederick Monsma, Director of New Lead Discovery at Schering-Plough Research Institute in Kenilworth, NJ will present on “A Label-free, High Throughput Mass Spec Platform for Lipid Deacylase: BioTrove RapidFire” at GTCbio’s 2nd Assay Development & High Throughput Screening Conference on May 31-June 1 in Boston, MA.
Many robust methodologies have been developed over the years for assaying enzymatic reactions. In particular, the development of sophisticated fluorescent labeling and detection techniques have allowed the development of assays which are amenable to high throughput and low volumes. Nevertheless, certain enzymatic targets cannot be assayed in these formats due to the interference of fluorescent labels on enzymatic activity. And, while radioactive substrates may obviate this issue, the need for separation of substrate and product molecules, as well as a desire to reduce radioactive usage, has limited the utility of this approach as well. Thus in recent years, a number of approaches have been developed that do not rely on the use of labeled substrates or other probes or tracers, and have allowed the assay of previously intractable targets. The current study focuses on one such approach, which utilizes high throughput Mass Spec detection of enzyme substrate and product, the RapidFire HTMS system developed by BioTrove. This approach couples rapid sample cleanup with specific and quantitative detection of substrate and product molecules from an enzymatic reaction. We have utilized this approach to conduct a screening campaign of a lipid deacylase, whose activity could previously be quantitated only by a traditional, very slow LC/MS analysis. Data will be presented which demonstrates that the RapidFire system delivers robust, quantitative detection of this enzyme reaction, and can be used to identify enzyme inhibitors in a screening campaign. In addition, our data demonstrate that characterization of the identified inhibitors using HTMS yields affinity values which agree extremely well with another direct binding detection technique. These results indicate that the RapidFire HTMS system provides a robust and reliable high throughput assay approach for screening of previously intractable targets.
GTCbio’s 2nd Assay Development & High Throughput Screening Conference on May 31-June 1 will take place at the Omni Parker House in downtown Boston, MA. The meeting will be held concurrently with GTCbio’s 2nd Protein Kinases in Drug Discovery Conference.
For more information including a detailed agenda, exhibitor opportunities and registration information visit http://www.gtcbio.com/conference/conferenceDetails.aspx?id=94
Many robust methodologies have been developed over the years for assaying enzymatic reactions. In particular, the development of sophisticated fluorescent labeling and detection techniques have allowed the development of assays which are amenable to high throughput and low volumes. Nevertheless, certain enzymatic targets cannot be assayed in these formats due to the interference of fluorescent labels on enzymatic activity. And, while radioactive substrates may obviate this issue, the need for separation of substrate and product molecules, as well as a desire to reduce radioactive usage, has limited the utility of this approach as well. Thus in recent years, a number of approaches have been developed that do not rely on the use of labeled substrates or other probes or tracers, and have allowed the assay of previously intractable targets. The current study focuses on one such approach, which utilizes high throughput Mass Spec detection of enzyme substrate and product, the RapidFire HTMS system developed by BioTrove. This approach couples rapid sample cleanup with specific and quantitative detection of substrate and product molecules from an enzymatic reaction. We have utilized this approach to conduct a screening campaign of a lipid deacylase, whose activity could previously be quantitated only by a traditional, very slow LC/MS analysis. Data will be presented which demonstrates that the RapidFire system delivers robust, quantitative detection of this enzyme reaction, and can be used to identify enzyme inhibitors in a screening campaign. In addition, our data demonstrate that characterization of the identified inhibitors using HTMS yields affinity values which agree extremely well with another direct binding detection technique. These results indicate that the RapidFire HTMS system provides a robust and reliable high throughput assay approach for screening of previously intractable targets.
GTCbio’s 2nd Assay Development & High Throughput Screening Conference on May 31-June 1 will take place at the Omni Parker House in downtown Boston, MA. The meeting will be held concurrently with GTCbio’s 2nd Protein Kinases in Drug Discovery Conference.
For more information including a detailed agenda, exhibitor opportunities and registration information visit http://www.gtcbio.com/conference/conferenceDetails.aspx?id=94

Director of New Lead Discovery at Schering-Plough will present on “A Label-free, High Throughput Mass Spec Platform for Lipid Deacylase: BioTrove RapidFire” at GTCbio's Assay Development & HTS meeting
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