LD Organisation

Scientific Conference Producers

Programme


Opening keynote lecture

18:00
Henk TIMMERMAN
VU UNIVERSITY AMSTERDAM, Oegstgeest, The Netherlands
18:15

Chemistry’s Role in Target Identification And Validation

Scott A. BILLER
NOVARTIS, Cambridge, United States
19:00

Welcome Reception

09:00
David BAILEY
IOTA PHARMACEUTICALS, Cambridge, United Kingdom

Fragment Based Drug Discovery

09:05

Experiences in Fragment-based Lead Discovery

Roderick E. HUBBARD
UNIVERSITY OF YORK / VERNALIS, York, United Kingdom
09:45

SPR Biosensor-Based Fragment Screening and Lead Characterization

U. Helena DANIELSON
UPPSALA UNIVERSITY, Uppsala, Sweden
10:15

Novel-Generation Kinase Inhibitors: Deep Pocket Binders by Fragment- Based Design

Gurrath MÜLLER
CSO PROTEROS FRAGMENTS, Munich/Martinsried, Germany
10:45

Coffee-break

11:15

The Use of Acetylcholine Binding Protein and FBDD Approaches in the Quest for Novel Nicotinic Receptor Ligands.

Iwan DE ESCH
VRIJE UNIVERSITEIT AMSTERDAM, Amsterdam, The Netherlands

Oral Communications

11:45

Fragment-Based Identification of Novel Hsp90 Inhibitors

Christian MONTALBETTI
EVOTEC, Abindgon, United Kingdom
12:00

Searching the Impossible – Designing Libraries from Large Virtual Chemistry Spaces

Christian LEMMEN
BIOSOLVEIT, St. Augustin, Germany
12:15

Lunch

Kinase Inhibitors: Targeting the Non-ATP Site

14:00
Edmond DIFFERDING
, Louvain-la-Neuve, Belgium
14:05

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

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, 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

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)

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, 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
AUREUS PHARMA, Villebon sur Yvette, France
16:45

Between Prometheus and Morpheus: Identifying Histamine Receptor Selectivity Switches

Chris DE GRAAF
VU UNIVERSITY AMSTERDAM, Cambridge, United Kingdom
17:00

End of the programme

19:00

Symposium Banquet

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


BIOSOLVEIT, Sankt Augustin, Germany
12:00

Late Departure - transportation will be provided by the organisers