Tuesday, 19 March 2013

08:00

Registration


Chemical Proteomics
Session SponsorsSession Sponsor

09:00

Hiroaki SugaKeynote Presentation

Discovery of Non-traditional Peptide Therapeutic Leads Accelerated by the RaPID System
Hiroaki Suga, Professor, The University of Tokyo, Japan

This lecture presents a novel technology that enables for the discovery of non-traditional peptide therapeutic leads against various drug targets.

10:00

Chemical Biology Approaches to Target Protein Modification in Disease
Edward Tate, Professor of Chemical Biology, Imperial College London, United Kingdom

I will highlight some of our recent advances in probing protein lipidation using chemical proteomics, and describe how we have applied this technology to identify and exploit novel drug targets in protein lipidation pathways in infectious disease and cancer.

10:30

Coffee Break and Networking in the Exhibition Hall

11:15

Chemical Biology of Ubiquitination, Proteolysis & Antigen Presentation
Huib Ovaa, Group Leader, Netherlands Cancer Institute, Netherlands

Latest developments in assay development will be discussed including chemical ubiquitination strategies. Assays to study proteasome activity and T-cell function will be also be discussed.

11:45

N-Acyliminium Ion Chemistry in Chemical Biology of the GPCR’s
Morten Meldal, Professor Head of Nano-Science Center, University of Copenhagen, Denmark

N-Acyl iminium ion chemistry proved extremely versatile in conversion of peptide library assemblies into small molecule libraries suitable for investigation of receptor signaling on solid support. Monoclonal GPCR - reporter gene cell lines were developed and grown in monolayers on solid phase small molecule libraries. The interaction of GPCR’s with supported ligands and receptor signaling was investigated.

12:15

Lunch and Networking in Exhibition Hall

13:30

Poster Viewing Session

14:15

Probing Host - Pathogen Interactions using Scaffolded and Assembled Peptides as Protein Binding Site Mimetics
Jutta Eichler, Professor, University of Erlangen-Nuremberg, Germany

Synthetic protein binding site mimics have proven excellent tools to explore HIV - host interactions. Such studies are aimed at providing insight into the molecular details of protein-protein interactions, as well as to explore novel routes of therapeutic intervention.


Synthetic and Computational Chemistry

14:45

Mining Off-targets of Network Drugs
Uwe Rix, Assistant Member/Professor, Moffitt Cancer Center, United States of America

On the example of the synergy of two multikinase inhibitors in BCR-ABLT315I mutant CML cells we present a comprehensive integration of three different large-scale -omics approaches with broad potential for elucidating complex cellular mechanisms of drug synergy in general.

15:15

Coffee Break and Networking in the Exhibition Hall

16:00

Chemical Modification of Proteins
Stephen Caddick, Vice Provost for Enterprise, University College London, United Kingdom

The ability to prepare chemical modified proteins is essential for fundamental chemical biology and the development of protein therapeutics. This presentation will provide an overview of recent studies directed toward developing novel chemical methods for the selective covalent modification of a variety of proteins. A discussion of broad ranging application in chemical biology and therapeutic innovation will be presented.

16:30

Towards the Systematic Exploration of Chemical Space: Design, Synthesis and Exploitation of Diverse Small Molecular Libraries
Richard Doveston, Researcher, Leeds University, United Kingdom

The presentation will focus on synthetic approaches that have been developed to enable the more systematic exploration of biologically-relevant chemical space.  The discovery and applications of specific novel bioactive small molecule probes will be highlighted.

17:00

Computational Methods for Chemical Biology
Jurgen Bajorath, Professor, Rheinische Friedrich Wilhelms University of Bonn, Germany

Computational approaches are beginning to impact research activities at the interface between chemistry and biology. Methods for computational chemical biology will be introduced and exemplary applications presented.

17:30

End of Day One

Wednesday, 20 March 2013


Chemical Biology and Drug Design

08:30

Barry PotterKeynote Presentation

Approaches to Drugging Nucleotide Ca2+- Mobilizing Second Messenger Pathways
Barry Potter, Professor, University of Bath, United Kingdom

Intracellular calcium stores can be mobilised in an agonist dependent and second messenger-mediated fashion by two nucleotides cyclic adenosine 5'-diphosphate ribose (cADPR) and nicotinic acid adenine 2'-dinucleotide phosphate (NAADP), unrelated to the well known myo-inositol 1,4,5-trisphosphate (IP3). Early synthetic strategies and potential for pharmacological intervention in such cell signalling pathways will be discussed.

09:30

Mark BradleyKeynote Presentation

Two Adventures in Chemical Biology - Palladium Medicated Cellular Chemistry and in vivo Imaging
Mark Bradley, Professor, Schools of Chemistry and Medicine, University of Edinburgh, United Kingdom

My group has developed a truly heterogeneous Pd0-catalysts with the ability to enter cells in culture and mediate efficient bioorthogonal organometallic chemistry.

10:30

Coffee Break and Networking in the Exhibition Hall

11:15

How to Make Yeast Tremble and Suffer Energy Loss: Yeast Models for Prion and Mitochondrial Diseases
Marc Blondel, Professor, University of Brest, France

The aim of my group is to develop yeast-based models for various human diseases, including prion-based diseases, mitochondrial diseases and EBV-linked cancers. These models are then used for isolating candidate drugs for these diseases as well as new cellular pathways involved in these pathologies.


Chemical Cell Biology and Cancer

11:45

Guiding Treatment Decisions in Cancer using Protein Biomarker Measurements: from Design to Utility
Stephen Pennington, Professor, University College Dublin, Ireland

The application of a range of proteomics strategies has resulted in the discovery of very large numbers of potential new protein biomarkers but few have reached clinical utility for (a) understanding the molecular mechanisms of cancer pathogenesis, (b) identifying new therapeutic targets, or (c) implementing biomarker based personalised treatment. Some of the challenges faced in the protein biomarker development process and potential solutions will be described from our recent studies on prostate cancer.

12:15

Lunch and Networking in Exhibition Hall

13:30

Poster Viewing Session

14:15

Positioning and Repurposing of Targeted Anti-cancer Compounds Using Ex Vivo Drug Sensitivity Testing on Primary Cancer Cells
Krister Wennerberg, Group Leader, Institute for Molecular Medicine Finland, Finland

This presentation will describe the strategy of positioning and repurposing oncology drugs as well as identifying resistance mechanisms and possible next line therapies using ex vivo drug sensitivity testing and molecular profiling of leukemic patient samples.


Enzyme Inhibition

14:45

Chemical Probes to Study ADP-ribosylation - Potent and Selective Inhibitors of the Human ADP-ribosyltransferase ARTD3/PARP3
Mikael Elofsson, Professor/Associate Head, Umea University, Sweden

ADP-ribosylation plays a critical role in cell differentiation, proliferation, genome integrity and cell-survival but the exact molecular mechanisms remain elusive. We develop small molecule inhibitors that target individual members of human diphtheria toxin-like ADP-ribose transferase (ARTD) family.

15:15

Coffee Break and Networking in the Exhibition Hall

15:45

A Tankyrase Specific PARP Inhibitor
Stefan Krauss, NCS Director, University of Oslo, Norway

Tankyrases 1 and 2 (TNKS1/2) are promising pharmacological biotargets with implications for developing novel anti-cancer therapeutics. Advances in developing specific tankyrase inhibitors will be presented, and their interactions with the catalytic domain of TNKS1 and TNKS2 will be discussed.

16:15

Using Chemical Proteomics to Reveal Drug Targets and Drug Selectivity, Drug Mechanism of Action and Resistance Formation
Guillaume Medard, Group Leader, Technical University of Munich, Germany

This presentation gives examples for how mass spectrometry based chemical proteomics can aid at various stages in the drug discovery process including the identification of new drug targets, the selectivity of kinase inhibitors, the elucidation of the mechanism of action of drugs targeting HSP90 and identify mechanisms of resistance against targeted kinase inhibitors.

16:45

Close of Conference