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Screening Track 1: Screening Methods
Day 1 |
| 08:00 |
Registration
Session Title: High Content Screening and Cell-Based Assays |
| 09:30 |
High-Content Screening Using Recombinant Antibody Microarrays
Christer Wingren, Associate Professor, Lund University
A high-content proteome screening tool, based on recombinant antibody microarrays, will be presented using Systemic Lupus Erythematosus (SLE) and Pre-eclampsia as case studies. |
| 10:00 |
A Chemical Biology Approach to Identify New Microtubules Dynamics Regulators
Laurence Lafanechère, Université Joseph Fourier, Grenoble
Using a multiplexed cell-based assay, we have screened for compounds that target, directly or not, microtubule dynamics. We have selected several molecules, and a few that stabilize microtubules. We will compare this approach with high content imaging screening. |
| 10:30 |
Coffee and Networking |
| 11:15 |
Live Cell High Content Screen Assay of Late Endocytic Events
Milan Esner, High-Throughput Technology Development Studio of the Max-Planck Institute in Dresden
We developed a quantitative approach to study the movement of late endosomes and lysosomes in living cells. Technical aspects of developing live cell high content assays will be discussed and results of RNAi and chemical
compounds screens will be presented. |
| 11:45 |
Putting HCS into hESC: Identifying Small Molecules to Control Human Embryonic Stem Cell Behaviour Using High Content Screening
Paul Andrews, University of Dundee
We have developed capabilities to grow and plate sufficient quantities of hESC in feeder-free conditions to enable us to successfully execute several high content screening campaigns to identify small molecules that either promote cell survival, pluripotency or differentiation. |
| 12:15 |
Lunch & Networking |
| 14:15 |
Profluorescent and Chemiluminescent Probes for In-Vivo Protease Imaging
Pierre-Yves Renard, Professor, University of Rouen
Strategies aiming at the preparation of in vivo imaging smart probes for the sensing of proteases will be described, involving the use of either FRET fluorescent pairs or self-immolative linkers associated to original chemiluminescent and Near Infra Red pro-fluorescent species. |
| 14:45 |
High Content Screening of Cellular Networks
Vytaute Starkuviene, University of Heidelberg
Our recently established group of “Screening of cellular networks” at BIOQUANT – System Biology Research Institute – aims to obtain a global and dynamic regulatory network of differential trafficking machineries operating in cells, and to associate it to complex cellular changes. A number of assays are being developed to work under conditions of RNAi, cDNA over-expression and modulation of microRNA levels. Moreover, we are developing strategies for ultra-fast fluorescent microscopy imaging to make observation of secretory processes in living cells in parallel fashion possible. |
| 15:15 |
High Throughput Approaches to Systems Biology Screening
Wayne Bowen, CSO, TTP LabTech
Whist screening against individual therapeutic proteins can identify ‘hit’ compounds, a systems biology approach is more ideally suited for target validation and mechanism of action studies. High content methodologies are addressing this need in a higher throughput environment. |
| 15:45 |
Coffee and Networking |
| 16:30 |
Targeted Metabolomic Screening in Low Sample Volumes
Therese Koal, Director Research, Biocrates Life Sciences
High throughput multiparametric targeted tandem mass spectrometry methods play the key role in targeted metabolomic screening. The method development, validation and disease application by means of analytical quantification even in small biological sample volumes will be presented. |
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17:00
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Ultra-High Throughput Screening For Activity And Affinity On A Single-Cell Basis
Harald Kolmar, Professor, Technische Universität Darmstadt
We use E. coli bacteria not only as producers of a protein of interest but also as living particles that display these biomolecules on their cell surface. This allows for the direct screening of large libraries exceeding 109 different variants on a single cell basis using fluorescence activated cell sorting. Cell surface display strategies and examples for single-cell screening of miniprotein libraries for binders to various targets as well as screening of enzyme libraries for enhanced substrate enantioselectivity will be presented in the talk. |
| 17:30 |
Drinks Reception –
Sponsorship available, please contact paul.raggett@selectbiosciences.com |
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Day 2
Session Title: Advances in Screening Techniques |
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09:30
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Virtual Screening: New Approaches and Applications
Joannis Apostolakis, Ludwig-Maximilians-University Munich
In this talk I will give a short overview of the current status of virtual screening approaches and applications. The talk will focus on our recent work both on methodological issues such as sampling and scoring as well as on new applications such as inverse screening and structural metabolomics. |
| 10:00 |
Reactive Intermediate Screen for Early Identification of Idiosyncratic Drug Reactions
Katya Tsaioun, CEO, Apredica Pharmaceuticals
A new high-throughput reactive intermediate screen and its application in lead optimization and clinical candidate selection programs are described. Case studies will be presented. |
| 10:30 |
Coffee & Networking in Main Exhibition Hall |
| 11:15 |
Fluorescence-Lifetime as a Novel, High-Quality Readout Technology for Compound Profiling and Screening of Proteases
Lorenz Mayr, Executive Director/Senior Unit Head, Head of Biology Unit, Protease Platform, Novartis Pharma AG
Summary to follow |
| 11:45 |
The NIH Chemical Genomics Center (NCGC): bridging basic research and chemical probe development using quantitative high-throughput screening
Natasha Thorne, NIH Chemical Genomics Centre
The purpose of NCGC is to make HTS and chemical probe discovery and development accessible to basic researchers. We utilize a novel screening paradigm called quantitative HTS (qHTS) to generate concentration response curves for each compound in our 300K library. Current efforts at NCGC include developing assays for non-traditional targets, maintaining PubChem, and accelerating probe development technologies. |
| 12:15 |
Lunch & Poster Presentations |
| 14:15 |
Profiling Environmental Chemicals in the Cellular Stress Pathway using Quantitative High-Throughput Screening
Sunita Shukla, NIH Chemical Genomics Centre
Quantitative high-throughput screening, developed at the NIH Chemical Genomics Center, has proven to profile compounds of interest quickly and efficiently in vitro. Thus, we will discuss the application of qHTS to cell-based assays which were utilized for toxicological profiling of compounds that stimulate the antioxidant response element (ARE) cellular stress pathway. |
| 14:45 |
Simultaneous Measurement of many Protein/Small Molecule Binding Events in Small Sample Volumes.
Marchella Chiari, Head of Analytical Microsystem Laboratory, Institute of Molecular Recognition in Milan
The lecture will address technical challenges and bottlenecks in protein array technology, one of the most promising high throughput tools to assess small molecule-protein interactions, relaying on the surface immobilization of purified proteins, followed by incubation with the binding partners. |
| 15:15 |
A Human Protein Atlas
Fredrik Ponten, Department of Genetics and Pathology, Uppsala University
The presentation will describe a multi-disciplinary research program to create a “Human Proteome Resource” to allow for systematic exploration of the human proteome using antibody-based tissue proteomics, combining high-throughput generation of mono-specific antibodies (affinity-purified) with protein profiling in human tissues and cells using tissue microarrays |
| 15:45 |
Coffee & Networking in Main Exhibition Hall |
| 16:30 |
Double-Layer Microfludic Screening Platforms
Petra Dittrich, Assistant Professor for Bioanalytics, ETH Zurich
In this contribution, microchips consisting of two microfluidic layers are presented, which are designed for the systematic study of cellular response towards soluble factors. Moreover, those platforms are useful tools for formation and analysis of artificial, cell-like objects. |
|
17:00 |
Iterative Screening with High Density Peptidomimetic Arrays
Volker Stadler, Head of Research Group/CEO, German Cancer Research Center/PEPperPRINT GmbH
A new combinatorial laser printing technology enables the synthesis of consecutive and customized peptidomimetic arrays. Very large numbers of sequence variants derived from initial hits are used to optimize target binders in unprecedented speed by iterative screens |
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Day 3
Session Title: Label-Free Screening |
| 09:30 |
Filling In The Gaps Of Early Drug Discovery With High-Throughput Label-Free Biosensors: Hope, Hype Or Truth?
Julio Martin, Manager ultra-HTS, GSK
Label-free optical biosensors are emerging as a new HTS platform enabling a broad range of applications. Nevertheless, there are still uncertainties about whether it will live up to the high expectations raised. We will revise applications in early drug discovery and current challenges to face. |
| 10:00 |
Impedance-Based Measurement of GPCR Modulators in Drug Discovery – Characterization of Signalling Pathways in Recombinant and Non-Recombinant Cells
John Gatfield, Senior Lab Head Molecular Biology, Actelion Pharmaceuticals
Analysis of prototypic GPCR activation response patterns in recombinant and non-recombinant cells and use for the characterization of coupling pathways of natural and synthetic ligands. |
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10:30 |
Coffee & Networking in Main Exhibition Hall |
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11:15 |
Imaging Reflectometric Interference Spectroscopy (iRIfS): A Versatile Tool For Array Based Biomolecular Interaction Analysis
Guenther Proll, Post Doc, University of Tuebingen
Imaging Reflectometric Interference Spectroscopy allows the investigation of biomolecular interactions on free scalable arrays with up to 1000 spots with unmatched flexibility and high performance. iRIfS is extremely robust against temperature changes and can handle all transparent transducer materials. |
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11:45 |
MS Binding Assays - A New Concept for Drug Screening
Klaus T. Wanner, Professor, Ludwig-Maximilians-University Munich
MS Binding Assays represent a universally applicable concept for affinity studies based on the quantification of native markers by mass spectrometry. As a result of recent modifications they can be performed with a significantly
improved throughput now. |
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12:15 |
Lunch & Poster Presentations |
|
14:15 |
A Versatile New Label-free, Microparticle-based SPR Bioassay Platform.
Carl Norman, Principal Research Scientist, Toshiba Research Europe Limited
We present a versatile new bioassay platform, which combines the joint advantages of i) discretely functionalised, code-bearing, microparticles, and ii) the label-free detection method of GC-SPR. Using coded particles overcomes some key limitations of spotted microarrays; diverse biomolecules under test can each be immobilised using its own preferred attachment chemistry and stored under its own optimum hydration conditions, prior to inclusion in a single multiplexed bioassay. |
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14:45
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Liquid Crystal-Based Microfluidic Immunoassays for High Throughput Screening
Kun-Lin Yang, Assistant Professor, National University of Singapore
A microfluidic screening platform which allows the label-free screening of antibodies will be presented. The novel label-free detection mechanism is based on the disruption of a thin layer of liquid crystals supported on the platform. |
|
15:15 |
Aptamers as recognition elements for label-free analytical devices
Noemí de-los-Santos-Alvarez, Oviedo University
In spite of the impressive advances in aptasensing the development of label-free devices is still a challenge especially when dealing with small molecules. We will revise the state of the art of this emerging and promising field with special stress on the potential for high throughput analysis/screening. |
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Screening Track 2: Drug Targets
Day 1
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| 08:00 |
Registration
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09:00
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Advancing Drug Discovery in an Academic Setting
Julie Frearson, Professor, Director of Hit Discovery, Drug Discovery Unit, Dundee
The presentation will focus on the increasingly popular paradigm of conducting early stage drug discovery within academic institutions. The tools and technologies we use within the Drug Discovery Unit at Dundee will be reviewed and the Tropical Disease Initiative will be used as a case in point to demonstrate how progressive early stage drug discovery can be enabled in this setting. |
| 09:30 |
Drug Development and Discovery in 2009
Christopher Bianca, Chemistry Instructor, Keystone College
Chemical, Clinical, and Analytical Consultant,Argonne/UC Chemical and Analytical Labs
The new era of drug development, what really takes to have a drug out in the market.
Session Title: Ion Channels as Drug Targets |
| 10:00 |
The Calcium Channel α2δ Subunit and its Role as a Therapeutic Target in Neuropathic Pain.
Claudia Bauer, University College London
The anti-allodynic action of Gabapentin and Pregabalin depends on their binding to the accessory calcium channel subunit α2δ but the molecular mechanism is not well understood. Our data indicate that these drugs affect the trafficking of calcium channels to their target membrane. |
| 10:30 |
Coffee and Networking |
| 11:15 |
vHTS Versus HTS in Ion Channel Research
Stefan Tasler, Senior Scientist, 4SC
The virtue of vHTS for the identification of potassium channel blockers will be emphasized by comparison to HTS technologies available for this target class. |
| 11:45 |
Structural Insights into Antagonist-K+ Channel Interactions
Olaf Pongs, Professor, University Hamburg
Combining solid-state NMR, biochemical and electrophysiological methods we have investigated structural principles underlying interaction of voltagedependent and voltage-independent potassium channel interaction with
antagonists. |
| 12:15 |
Lunch & Networking |
| 14:15 |
Ligand Gated Ion Channels Studies Using Rapid Screening
Sarah Lummis, University of Cambridge
Electrophysiology is the ‘gold standard’ to examine LGIC, but it is slow and technically difficult. Here we describe the use of two HTS electrophysiological techniques to study LGIC, and an alternative functional assay using fluorescent dyes. |
| 14:45 |
Kv10.1 (Eag1) as a target for tumor management
Luis Pardo, Group Leader, Max-Planck Institute for Experimental Medicine
We describe different tumor theragnostics approaches taking advantage of the selective expression profile of Eag1 channels in tumors together with its role in tumor biology. |
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15:15 |
Acid-Sensing Ion Channels (ASICs) as targets in pain
Eric Lingueglia, Group Leader, CNRS Institute for Molecular and Cellular Pharmacology/Institute for Molecular NeuroMedicine, Sophia Antipolis
Our data demonstrate a role for Acid-Sensing Ion Channels (ASICs) in the central modulation of pain through the regulation of the enkephalin system, and in the sensation of peripheral acidic and primary inflammatory pain, making them promising targets for pain relief. |
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15:45 |
Coffee & Networking in Main Exhibition Hall |
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16:30
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Multiple Applications of Automated Electrophysiology Systems in Early Drug Discovery
Joseph McGivern, Research Director, Lead Discovery, Amgen
Summary to follow |
| 17:30 |
Drinks Reception –
Sponsorship available, please contact paul.raggett@selectbiosciences.com |
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Day 2
Session Title: Kinases as Drug Targets |
| 09:30 |
Kinase Drug Discovery from Academic Research.
Tim Hammonds, Head of Biochemistry and HTS, Cancer Research Technology
This presentation will describe Cancer Research Technology Discovery Laboratory’s ongoing programme to design potent and selective small molecule inhibitors of protein kinases for use as a therapeutic agents. |
| 10:00 |
A Structural View on Protein Kinase CK2 and its Potential Role as a Target for Small Molecules
Karsten Niefind, University of Cologne
Recent structural data suggest novel concepts to target protein kinase CK2: Can the quaternary structure of the enzyme be disrupted? Can inactive conformations be enforced? |
| 10:30 |
Coffee & Networking in Main Exhibition Hall |
| 11:15 |
Non-ATP Competitive Kinase Inhibitors: Potentials and Limitations
Doriano Fabbro, Head of Kinase Biology, Novartis Pharma AG
This present review will highlight the different inhibitor design approaches in the context of inhibition mechanism efficiency and compound novelty including target selectivity, binding kinetics, and resistance formation with particular emphasis on non-ATP competitive inhibitors. In particular the non-ATP competitive inhibitors of the Abl kinase activity will be discussed in more details |
| 11:45 |
Oncogene Addiction, Pathway Addiction and the Response of Tumour Cells to ERK1/2 Pathway Inhibitors
Simon Cook, Head of Laboratory of Molecular Signaling, The Babraham Institute
This presentation will review the validation of the ERK1/2 pathway as a therapeutic target in cancer, describe inhibitors of this pathway and describe cell intrinsic determinants of drug sensitivity and drug resistance based on studies in human colorectal cancer lines. |
| 12:15 |
Lunch & Poster Presentations |
| 14:15 |
Development of the Paullones, a Unique Protein Kinase Inhibitor Family
Conrad Kunick, Professor, Technische Universitaet Carolo-Wilhelmina Zu Braunschweig
Identified originally by data mining from the NCI’ s data base, the paullones have been developed as inhibitors of glycogen synthase kinase-3. The talk will highlight current uses of paullones in diverse research areas, e.g. Alzheimer’s disease, diabetes, and tropical infectious diseases. |
| 14:45 |
Targeting Cell Cycle Kinases: A Validated Approach for Anticancer Therapy?
Jurgen Moll, Director Cell Biology Dep., Nerviano Medical Sciences
An update on the characteristics of some of the advanced small molecule inhibitors of critical cell cycle regulating kinases developed at NMS will be given, including Aurora, PLK and CDC-7 kinase inhibitors. |
| 15:15 |
Targeting Protein Kinase CK2 as a Multi-Potential Strategy in Signal Transduction Therapy.
Lorenzo A. Pinna, Professor, University of Padova
The implication of CK2 in neoplasia is not due to genetic alterations, but to its intrinsic ability to generate a cellular environment predisposed to cancer. Consequently attenuation of abnormally high CK2 activity could prove beneficial in several neoplastic diseases. |
| 15:45 |
Coffee & Networking in Main Exhibition Hall |
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Day 3
Session Title: GPCRs as Drug Targets |
| 09:30 |
High Throughput Screening for GPCR Ligands; Strategies, Successes and Future Challenges
GSK
This talk will describe the implementation of GPCR assay technologies for HTS and SAR screening, and the application of these technologies for the identification of classical GPCR agonist and antagonist ligands and increasingly the identification of molecules with novel mechanisms of action. |
| 10:00 |
Investigation of G-Protein-Coupled Receptor Desensitisation Using Fluorescence Resonance Energy Transfer
Cornelius Krasel, Lecturer, University of Reading
Monitoring of GPCR-arrestin interactions is being used as an alternative to more conventional signalling pathways in drug screening. Can this technique also be used to gain information about kinetics of agonist binding and dissociation? |
| 10:30 |
Coffee & Networking in Main Exhibition Hall |
| 11:15 |
“Universal” Screening Technologies in the Light of Evolution: From Promiscuous G Proteins to ß-Arrestin Translocation to Cutting Edge Optical Techniques
Evi Kostenis, Director Molecular Cellular and Pharmacobiology, University of Bonn
The talk will give an overview about past and present universal screening technologies for GPCRs and present specific examples for advantages and pitfalls, limitations and opportunities particularly for the novel label-free real time dynamic mass redistribution assays (Corning Epic® biosensor). |
| 11:45 |
Mathematical Modelling of GPCR Binding and Function
Jesús Giraldo, Institut de Neurociències and Unitat de Bioestadistica, Universitat Autònoma de Barcelona.
Mathematical models can be useful tools for the understanding of physiological function, and for classifying receptors and ligands. In this communication, some of the main characteristics of GPCRs such as oligomerization and cooperativity will be addressed for a quantitative description of receptor binding and function. |
| 12:15 |
Lunch & Poster Presentations |
| 14:15 |
Pharmacological Characterization of GPRC6A – a 7TM Receptor Activated by L-a-Amino Acids and Positively Modulated by Divalent Cations.
Petrine Wellendorph, University of Copenhagen
GPRC6A is a novel L-a-amino acid-sensitive family C 7TM receptor for which deorphanization and development of efficient cell-based functional assays have been extremely challenging. L-Arg, L-Lys, L-ornithine and derivatives
thereof are the only agonists (ligands) reported to date. |
| 14:45 |
Fluorescent Approaches to Studying G Protein-Coupled Receptors
Steve Hill, University of Nottingham
The talk will explore the opportunities provided by new fluorescent probes to study the pharmacological properties of GPCRs. Some examples will be given of the use of bimolecular fluorescence complementation to study receptor-arrestin interactions and to study the properties of receptor homo- and hetero- dimers. In addition, recent work with fluorescent ligands (both agonists and antagonists) and the application of fluorescence correlation spectroscopy will be highlighted in the study of receptors in membrane microdomains of single living cells |
| 15:15 |
Mining the Amphibian Skin Peptidome for Therapeutically-Relevant Target Ligands
Chris Shaw, Professor, Queen’s University, Belfast
Amphibian skin secretions contain natural peptide libraries with a largely untapped potential for discovery of novel ligands for therapeutically-relevant targets such as GPCRs. Peptides may be agonists or antagonists, novel analogues of known ligands or new entities unique in Nature. |
| 15:45 |
Coffee & Networking in Main Exhibition Hall |
| 16:30 |
GPCRs: Real Structures and Virtual Screens.
Ad P. IJzerman, Professor, Leiden/Amsterdam Center for Drug Research
In the last year tremendous progress has been made in the structure elucidation of G protein-coupled receptors. Will this exciting information be helpful in virtual and/or ‘wet’ screening of ligand libraries on these important drug targets? |
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