Discovery And Development Of Selective, Orally Bioavailable Tyrosine Kinase Inhibitors For Targeted Treatment Of Human Cancers
Stephen K. BURLEY (ELI LILLY AND COMPANY, San Diego, United States)
14:45
Non-Competitive Inhibitors of MEK1: from Discovery to the Clinic
Jeffrey OHREN (PFIZER, Groton, United States)
15:15
The Discovery and Development of Allosteric Akt Inhibitors for the Treatment of Cancer
Philip E. SANDERSON (MERCK, Rahway, United States)
15:45
Coffee-break
Oral Communications
16:15
Understanding Kinase Selectivity Through Active Site Hydration Energetics
Jianxin DUAN (SCHRÖDINGER, MANNHEIM, Germany)
16:30
4-Aryl-7-Azaindoles as IKK2 Inhibitors
Michael BARKER (GLAXOSMITHKLINE, Stevenage, United Kingdom)
16:45
Targeted Kinase Inhibitors : Precision in Interaction and Efficacy
Eric HAAKSMA (BOEHRINGER INGELHEIM AUSTRIA, Wien, Austria)
17:00
Poster Session
18:30
End of Scientific Programme
19:30
Dinner
05/05/2009
Promises in GPCR Drug Discovery
09:00
ROB LEURS (LACDR, VU UNIVERSITY AMSTERDAM, Amsterdam, The Netherlands)
09:05
Structural Genomics of GPCRs; New Opportunities for Drug Discovery
Chris TATE (MRC LABORATORY OF MOLECULAR BIOLOGY, Cambridge, Belgium)
09:45
GPCR Hetero-Dimerisation: Contribution to Receptor Pharmacology and Function
Graeme MILLIGAN (UNIVERSITY OF GLASGOW, Glasgow, United Kingdom)
10:15
Discovery & Development of Allosteric Modulators: Hopes and Promises
Emmanuel LE POUL (ADDEX PHARMA, Plan-les-Ouates, Switzerland)
10:45
Coffee-break
Oral Communications
11:15
The 2.6 Angstrom Crystal Structure of a Human a2a Adenosine Receptor Bound to an Antagonist
Robert LANE (UNIVERSITY OF LEIDEN, Leiden, The Netherlands)
11:30
Fieldstere: Application to the Discovery of 5-HT1D Agonists
Tim CHEESERIGHT (CRESSET BMD LIMITED, Cambridgeshire, United Kingdom)
11:45
Transmembrane Helix Position 5.48 Involvement in the Dimer Interface Of Domain-Swapped GPCRS
Raymond BOOTH (UNIVERSITY OF FLORIDA, Gainesville, Florida, United States)
12:00
Lunch and Poster Session
Anti-Inflammatory Drug Discovery
14:00
Robin THURMOND (JOHNSON & JOHNSON, San Diego, United States)
14:05
Histamine H4 Antagonists as Future Anti-Inflammatory Drugs
Robin THURMOND (JOHNSON & JOHNSON, San Diego, United States)
14:45
JAK3 Kinase: a Molecular Target for Treatment of Inflammatory Diseases and Renal Transplant Rejection
Paul S. CHANGELIAN (CHANGELIAN BIOSCIENCE, LLC, United States)
15:15
Molecular Mechanim of Action for Chemokine and Other Anti-inflammatory Agents on 7TM Receptors
Thue W. SCHWARTZ (UNIVERSITY OF COPENHAGEN, Copenhagen, Denmark)
15:45
Coffee-break
Oral Communications
16:15
The Quest for the New Antihistamines: Discovery and Evaluation of Histamine H4 Receptor Ligands
Rogier SMITS (VU UNIVERSITY AMSTERDAM, Utrecht, The Netherlands)
16:30
Developing CCR5 Antagonists for HIV: the Story since Maraviroc
Chris BARBER (PFIZER, Sandwich, United Kingdom)
16:45
Discovery of Novel Small Molecule CXCR4 Antagonists
Daniel GREVE (LEO PHARMA, Ballerup, Denmark)
17:00
End of Scientific Programme (participants are requested to remove their posters)
19:00
Dinner
20:00
Concert
06/05/2009
Chemical and Enzymatic Modification of Therapeutic Peptides and Proteins to Improve their Mode of Action
09:00
Martin DE KORT (SCHERING-PLOUGH, Oss, The Netherlands)
09:05
Engineering of Proteins and Peptides to Tailor Structure–Function and Pharmacokinetic
Jesper LAU (NOVO NORDISK, Maaloev, Denmark)
09:45
Sugars and Proteins
Ben DAVIS (OXFORD UNIVERSITY, Oxford, United Kingdom)
10:15
CarboCarrier(TM): a Novel Technology to Extend the Half-life of Small Proteins and Peptides
Martin DE KORT (SCHERING-PLOUGH, Oss, The Netherlands)
10:45
Coffee-break
Oral Communications
11:15
Role of Sugar Moieties in Biological Activities of Glycopeptide Antibiotics of the Vancomycin and Teicoplanin Group
Maria PREOBRAZHENSKAYA (GAUSE INSTITUTE OF NEW ANTIBIOTICS, MOSCOW, Russia)
11:30
Miniproteins Targeting the Nuclear Receptor – Coactivator Interaction
Luc BRUNSVELD (EINDHOVEN UNIVERSITY OF TECHNOLOGY, Eindhoven, The Netherlands)
11:45
Conjugation of Synthetic Peptides to Toll-Like Receptor Ligands for Vaccine Development
Dmitri FILIPPOV (LEIDEN INSTITUTE OF CHEMISTRY, Leiden, The Netherlands)
12:00
Lunch
13:00
Excursion (dinner included)
07/05/2009
Drug Transporters: from Drug Resistance to Safety Science
09:00
Eric HAAKSMA (BOEHRINGER INGELHEIM AUSTRIA, Wien, Austria)
09:05
Predicting Substrate Properties for ABC-Transporter - Safety Sciences on the Molecular Level
Gerhard ECKER (EFMC, UNIVERSITY OF VIENNA, Vienna, Austria)
09:45
Drug Transport and Metabolism: Value of Knockout and Transgenic Mouse Models
Alfred SCHINKEL (HET NEDERLANDS KANKER INSTITUUT, Amsterdam, The Netherlands)
10:15
Insights from Structural Studies of Human ATP-Binding Cassette Drug Transporters
Robert FORD (THE UNIVERSITY OF MANCHESTER, Manchester, United Kingdom)
10:45
Coffee-break
Bioanalytical Approaches in Drug Discovery
11:15
Novel Approaches for Comprehensive Profiling of Metabolites in Lead Discovery: Integration of Screening Assays with Ion-trap Time of Flight Mass Spectrometry
Hubertus IRTH (FREE UNIVERSITY OF AMSTERDAM, AMSTERDAM, The Netherlands)
Oral Communication
11:30
Non-Covalent Mass Spectrometry Screening Technology: An “ESI” Approach to Support Drug Discovery
Paola CIAPETTI (NOVALIX, Illkirch-Cedex, France)
12:00
Lunch
14:00
Piero ANGELI (UNIVERSITÀ DI CAMERINO, Camerino, Italy)
Off-Target Effects
14:05
GPCR Antitargets – Prediction and Prevention of Side Effects
Thomas KLABUNDE (SANOFI-AVENTIS, Frankfurt am Main, Germany)
14:45
Understanding Ion Channels Using Computational Approaches
Marcel J. DE GROOT (PFIZER, Sandwich, United Kingdom)
15:15
The QSARome of the Receptorome: Development of Robust QSAR Models Capable of Predicting Compound Binding Profiles against Multiple Targets
Alexander TROPSHA (UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL, Chapel Hill, United States)
15:45
Coffee-break
Oral Communications
16:15
Erythromycin Analogs - More Than Just Antibacterials
Prabhavathi FERNANDES (CEMPRA PHARMA INC, Chapel Hill, NC, United States)
16:30
Mining A Global Literature Pharmacology Knowledgebase to Assess Drug Polypharmacology of Classical Chemical Scafolds
Ismail IJJAALI (PERKINELMER, Villebon sur Yvette, France)
16:45
Between Prometheus and Morpheus: Identifying Histamine Receptor Selectivity Switches
Chris DE GRAAF (VU UNIVERSITY AMSTERDAM, Amsterdam, The Netherlands)
17:00
End of the programme
19:00
Symposium Banquet
08/05/2009
Complimentary Workshop on Friday: "Virtual Screening and De Novo Design" Offered by BioSolveIT
09:00
Please click on the link below to register for the Workshop
