biotechnology symposium 2005 abstracts - Universität Leipzig

1.4 TRANSIL ® technology – Immobilized proteins for
innovative assays and for ADME prediction in
drug discovery
Joachim Nöller
NIMBUS’ TRANSIL ® platform is a proprietary bead based assay technology allowing for
the biofunctionalization of solid supports. Based on this platform, we are providing bead
based assays for important stages in drug discovery.
About 40 % of late-stage failures are associated with poor pharmacokinetic properties
leading to a huge loss in time and money. Early profi ling of drug like properties provides
important information to screen out insoluble, poor absorbing and toxic compounds.
As one contribution of NIMBUS to this bottleneck in drug discovery the TRANSIL ®
technology allows the functional immobilization of serum proteins (e.g. Human Serum
Albumin) on solid supports. After surface passivation, protein molecules are covalently
attached on the bead surface taking care that important pharmacologically binding
sites are freely accessible and therefore suitable for the determination of the unspecifi c
binding to serum proteins, as an important ADME related parameter. This parameter for a
compound is used in combination with the membrane affi nity and the molecular weight for
the prediction ADME parameters like volume of distribution or plasma organ partitioning
coeffi cients.
Furthermore technology enables also binding assays for transmembrane proteins which
will be described for the measuring the binding of AGEs (Advanced Glycation Endproducts)
to the plasma membrane of Caco-2 cells.
Dr. Joachim Nöller
Nimbus Biotechnologie GmbH
E-Mail: jnoeller@nimbus-biotech.com
www.nimbus-biotech.com
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