DNAprint Genomics (DNAG)

[mingwan0]

SBS 10th Anniversary Conference & Exhibition
September 11-15, 2004
Orlando, FL

http://www.sbsonline.org/04conf/posters/index.php

#P03003 - Biochemical and Structural Diversity in a Natural Products Library

Authors: Peter Eckard, Iris Grün-Wollny and Friedrich G. Hansske, Biofrontera Discovery GmbH
Presenter: Peter Eckard, Biofrontera Discovery GmbH - Germany

Diversity is of utmost importance in a compound library which is expected to deliver leads for a wide range of molecular targets by high-throughput screening.

Diversity of a compound library is usually regarded as structural diversity but in the end biochemical diversity is required in the sense that a screening campaign results in hits and leads against a broad range of target classes, e.g. proteases, kinases, phosphatases, GPCRs, protein-protein interactions and ion channels.

In a library based on secondary metabolites from microbial sources genetic diversity is regarded as important factor determining the structural and biochemical diversity.

Biofrontera uses a library of prepurified extracts from rare actinomycetes and fungi for lead discovery. We have screened our library against a panel of targets and show that our library is based on high genetic diversity and delivers compounds with excellent structural and - most importantly - biochemical diversity.

#P04003 - Functional, Cellular GPCR Screening for Drug Profiling and Screening of Natural Compound Libraries

Authors: Julia Sommer, Mirella Gwarek, Anna Pecoraro, Peter Eckard, Harry F. Abts, Biofrontera Pharmaceuticals GmbH
Presenter: Harry Frank Abts, Biofrontera GmbH - Germany

GPCRs are one of the most prominent target classes for drug development.

To identify novel GPCR-related drug candidates and subsequently establish their potency, efficacy and selectivity we have generated more than 40 stable cell lines expressing different human GPCRs (including all monoaminergic receptors) in CHO-DUKX and KNRK cells.

Functional interaction of a compound with a GPCR is monitored by activity of a luciferase reporter-gene. These functional cellular assay systems therefore constitute screening tools with maximum sensitivity.

The assay cells have been successfully used for screening of natural compound libraries.

In addition the profiling of the compound activity on all relevant human receptors, provides the best possible prediction of GPCR-mediated drug effects and side effects in man.

Finally the established cell lines have proven to provide fast and reproducibly a reliable basis for ranking of drug candidates, and for designing and monitoring lead development and optimization.