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The NJ ACS section is pleased to announce the first
symposium dedicated to: igh Throughput Biomolecular Screening Using Mass Spectrometric Detection?o:p> 3:00 to 8:00 PM on Tuesday, February 13, 2001
at the [Directions] A
collaborative effort between the The symposium will start with an
unabridged vendor fair and social period that includes an extensive dinner
buffet. After dinner, lectures will
be given by 3 world leaders in biomolecular screening using MS detection.
The lectures are as follows: "Biomolecular Screening Using Ultrafiltration Mass Spectrometry: Assays for Drug Discovery and Development" Richard B. van Breemen and Dejan Nikolic As a detector for high throughput screening assays, mass spectrometry offers
a unique combination of sensitivity, speed and selectivity. In particular, the
selectivity of the mass spectrometer facilitates the screening of combinatorial
libraries as mixtures instead of discreet compounds thereby increasing the
throughput of these assays. Another important aspect of screening mixtures is
the ability to screen natural product extracts which have become a neglected
source of molecular diversity and lead compounds. Although several mass
spectrometry-based assays have been developed for drug discovery and lead
optimization, few have been reported for drug development applications such as
metabolism screening or toxicity screening. One such method is pulsed
ultrafiltration which was invented and developed in our laboratory. Applications
of pulsed ultrafiltration mass spectrometry include the screening of natural
products and combinatorial libraries for drug discovery, the screening of
directed libraries during lead optimization, drug metabolism profiling, toxicity
screening of lead compounds for metabolic activation to electrophilic
intermediates, and measurement of affinity constants. In summary, the mass
spectrometry-based screening technique of pulsed ultrafiltration may be used to
facilitate multiple stages of drug discovery and development. "Using Frontal Affinity Chromatography - Mass Spectrometry (FAC/MS) N. Chan, D. Lewis, M. Middleditch, D. Schriemer The HTS community continues to require technological and assay innovation,
however novel approaches require a substantial development and validation period
before achieving the status of a reliable screening tool. Numerous assay
technologies exist, yet not all are suitable for HTS, primarily due to the high
standards of the field (better, faster, cheaper). Once an innovative approach is
identified, it needs to pass rigorous tests to ensure reliability, high
information content, ability to automate, and scalability. "High Performance ESI-FTICR Mass Spectrometry as a High Throughput Affinity Screen to Identify RNA-Binding Ligands" Steven A. Hofstadler, Jared J. Drader, Richard H. Griffey, Kristin A.
Sannes-Lowery, and Sheri Manalili Fourier transform ion cyclotron resonance (FTICR) mass spectrometry (MS) is increasingly being used in the drug discovery arena as a tool to characterize macromolecules. In this presentation we describe the development of a parallel high-throughput screening (HTS) strategy to identify small molecules that bind RNA targets using FTICR as an alternative to classical high-throughput screening of combinatorial libraries. The MASS (Multitarget Affinity/Specificity Screening) assay takes advantage of the "intrinsic mass" label of each compound and target RNA by employing high resolution, high precision mass measurements. The ability to analyze complex mixtures allows large mixtures to be screened in the presence of multiple RNA targets simultaneously. The identity of the small molecule(s) which bind, the RNA target to which it binds, the compound-specific binding affinity, and the location of the binding site on the RNA can be determined in one set of rapid experiments. The MASS assay detects noncovalent complexes with dissociation constants of < ~5 mM, with high sensitivity and is presently being employed to screen large compound collections against multiple RNA targets.
Vendor Fair 3:00-6:00PM Menu: Extensive Buffet Pre-registration is required. Admission is free of charge for this meeting, but pre-registration is required and can be completed on-line at http://www.njacs.org/msregis.html or by E-mailing your name and affiliation to [email protected] during the period from January 15, 2001 to February 6, 2001. Please note that there is a space limit of 400 attendees for this symposium and registration will be cut off when the limit is reached. So, register early to get your spot at this "first of its kind event!" |
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