EFMC-ISMC 2010
Printable version of the programme (01/09/2010 - 1592 KB)
05/09/2010
17:00Opening Ceremony
17:20Innovative Medicines Initiative - Europe and Biopharmaceutical Innovation
Michel GOLDMAN
(INNOVATIVE MEDICINES INITITATIVE JOINT UNDERTAKING, Brussels, Belgium)
17:35EFMC Award Ceremony
Chair
Gerhard ECKER
(EFMC, UNIVERSITY OF VIENNA, Vienna, Austria)
18:00The NAUTA AWARD for Pharmacochemistry Lecture
Camille G. WERMUTH
(PRESTWICK CHEMICAL, ILLKIRCH, France)
Chair
Henk TIMMERMAN
(VU UNIVERSITY AMSTERDAM, Oegstgeest, The Netherlands)
18:35Plenary Lecture
Genomes, Structural Biology and Drug Discovery: New Challenges from Difficult Targets and Neglected Diseases
Tom BLUNDELL
(UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom)
Chair
Edmond DIFFERDING
(DIFFERDING CONSULTING, Louvain-la-Neuve, Belgium)
19:20Welcome Reception
06/09/2010
08:30Plenary Lecture
A Chemical Approach to Controlling Cell Fate
Sheng DING
(THE SCRIPPS RESEARCH INSTITUTE, La Jolla, United States)
Chair
Rasmus Praetorius CLAUSEN
(DANISH UNIVERSITY OF PHARMACEUTICAL SCIENCES, Copenhagen, Denmark)
09:15Exhibition & Coffee
1. Chemical Strategies for Functional Proteomics - Activity-Based Protein Profiling2. Hot Topics in Cardiovascular Diseases3. Knowledge Enabled Drug Design
10:00Session Chair
Stephan A. SIEBER
(LUDWIG-MAXIMILIANS-UNIVERSITÄT MÜNCHEN, München, Germany)
10:05Activity Based Probes of Proteases: Applications to Functional Proteomics and Molecular Imaging
Matthew BOGYO
(STANFORD UNIVERSITY SCHOOL OF MEDECINE, Stanford, United States)
10:45Reactive Natural Products Probing Protein Complex Function
Hans-Dieter ARNDT
(THE MAX PLANCK INSTITUTE OF MOLECULAR PHYSIOLOGY, Dortmund, Germany)
11:05Transnuclear Mice Made by Somatic Cell Nuclear Transfer from B and T Lymphocytes
Hidde PLOEGH
(WHITEHEAD INSTITUTE, Cambridge, United States)
11:25Development Of Chemical Probes For The Study Of The Cb1 And Cb2 Cannabinoid Receptors
Silvia ORTEGA GUTIERREZ
(UNIVERSIDAD COMPLUTENSE DE MADRID, Madrid, Spain)
10:00Session Chair
Joachim MITTENDORF
(BAYER AG, Wuppertal, Germany)
10:05Canosimibe - Lowering of Atherogenic LDL by a Non-Systemic Cholesterol Absorption Inhibitor
Heiner GLOMBIK
(SANOFI AVENTIS, Frankfurt, Germany)
10:45Discovery of Riociguat: a Potent, Oral Stimulator of Soluble Guanylate Cyclase for the Treatment of Pulmonary Hypertension
Joachim MITTENDORF
(BAYER AG, Wuppertal, Germany)
11:25Design and Preparation of Potent, Nonpeptidic, Bioavailable Renin Inhibitors
Olivier BEZENCON
(ACTELION LTD, Allschwil, Switzerland)
10:00Session Chair
Mark BUNNAGE
(PFIZER, Boston, United States)
10:05Molecular Obesity, Potency and other addictions in Drug Discovery
Michael HANN
(GSK MEDICINES RESEARCH CENTRE, Stevenage, United Kingdom)
10:45Drug Guru - Encoding Tacit Knowledge from Experienced Medicinal Chemists
Kent STEWART
(ABBOTT LABORATORIES, ABBOTT PARK, United States)
11:05Bioisosteres from Ligand- and Structure-Based Data Analysis
James MILLS
(PFIZER, Canterbury, United Kingdom)
11:25Better Compounds Faster – The Development And Exploitation Of A Desktop Predictive Chemistry Toolkit
John CUMMING
(ASTRAZENECA, Macclesfield, United Kingdom)
11:45Poster Session 1 - Lunch
12:00ACCELRYS WORKSHOP
Staying Ahead Of Your Medicinal Chemistry Project Data
4. Chemical Approaches to Stem Cell Biology5. Molecular Therapies for Iinflammatory and Autoimmune Diseases: Ongoing Clinical Trials and Future Prospects6. Virtual Screening and Profiling
13:45Session Chair
Sheng DING
(THE SCRIPPS RESEARCH INSTITUTE, La Jolla, United States)
13:50Cardiovascular Derivatives of Human Pluripotent Stem Cells: Chemical Modulation and Use in Drug Discovery, Development, and Toxicology
Christine MUMMERY
(LEIDEN UNIVERSITY MEDICAL CENTER, Leiden, The Netherlands)
14:30Development of Small Molecule Therapeutics for Treating Endogenous Cells for Repair and Regeneration
Francine FAROUZ
(FATE THERAPEUTICS, La Jolla, United States)
15:10Phenotypic Screening using Human Neural Precursor Cells as a Translational in vitro Model to explore the Process of Neurogenesis
Ravi JAGASIA
(HOFFMANN - LA ROCHE, Basel, Switzerland)
13:45Session Chair
Sylviane MULLER
(IBMC-CNRS, Strasbourg, France)
13:50Molecular Therapies for Inflammatory and Autoimmune Diseases - Focus on Systemic Lupus Erythematosus
Sylviane MULLER
(IBMC-CNRS, Strasbourg, France)
14:30Generation and Development of a Series of MAPKAPK5 Inhibitors for the Treatment of Rheumatoid Arthritis
Martin ANDREWS
(GALAPAGOS NV, Mechelen, Belgium)
14:50Discovery And Optimization Of Highly Selective Btk Inhibitors That Bind To An Inactive Enzyme Conformation And Are Efficacious In Animal Models Of Arthritis And Lupus
Kevin CURRIE
(CGI PHARMACEUTICALS, INC., Branford, United States)
15:10Optimisation Of The Diaminopyrimidine Carboxamide Series Leading To Highly Potent, Selective And Orally Bioavailable Syk Inhibitors
Neil GARTON
(GLAXOSMITHKLINE, Stevenage, United Kingdom)
13:45Session Chair
Didier ROGNAN
(CNRS-UNIVERSITY OF STRASBOURG, Illkirch, France)
13:50Virtual Screening - Success Stories and Challenges
Jürgen BAJORATH
(UNIVERSITY OF BONN, Bonn, Germany)
14:30Targeting the Dynamic Nature of Protein-Protein Interfaces
Alessandro PADOVA
(SIENA BIOTECH, Siena, Italy)
14:50Cinderella’s Shoe For Virtual Drug Discovery, Screening And Design
Vladimir POTEMKIN
(CHELYABINSK STATE MEDICAL ACADEMY, Chelyabinsk, Russia)
15:10Discovery Of New Antimalarial Leads Through A Virtual Screening Approach
Tiago RODRIGUES
(IMED.UL. FACULTY PHARMACY, UNIVERSITY LISBON, Lisbon, Portugal)
15:30Exhibition & Coffee
7. Targeting Pathways8. Hot Topics in CNS Diseases9. Toxicity Challenges in Drug Design and Structure-Toxicity Relationships
16:15Session Chair
Nicholas COSFORD
(BURNHAM INSTITUTE FOR MEDICAL RESEARCH, La Jolla, United States)
16:20Discovery of Small Molecules for Myocardial Differentiation and Protection
Mark MERCOLA
(BURNHAM INSTITUTE FOR MEDICAL RESEARCH, La Jolla, United States)
17:00ASK-dependent Stress Signaling in Cell Death, Inflammation and Disease
Hidenori ICHIJO
(UNIVERSITY OF TOKYO, Tokyo, Japan)
17:20The Discovery of BKM120, a Pan Class I PI3 Kinase Inhibitor in Phase I/II Clinical Trials
Sabina PECCHI
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Emeryville, United States)
17:40Phenotypic Drug Discovery at Lilly: Merging Images, Informatics and Chemistry to Enable SAR
Thomas ENGLER
(ELI LILLY AND COMPANY, Indianapolis, United States)
16:15Session Chair
Benoit KENDA
(UCB, Braine-l'Alleud, Belgium)
16:20Identification of a PDE9 Clinical Candidate for the Treatment of Alzheimer's Disease utilizing Prospective Design and Novel Protocol Development
Patrick Robert VERHOEST
(PFIZER GLOBAL RESEARCH, Groton, United States)
17:00Synthesis and Characterization of 1,3-Dihydro-benzo[b][1,4]diazepin-2-one Derivatives as potent non-competitive metabotropic Glutamate Receptor 2/3 Antagonists
Thomas WOLTERING
(F. HOFFMANN-LA ROCHE AG, Basel, Switzerland)
17:20Discovery of Lu AE51090, an Allosteric Muscarinic M1 Agonist: Pro-cognitive Potential Alone and as Add-on to Antipsychotic Treatment
Anette GRAVEN SAMS
(H. LUNDBECK, Valby, Denmark)
17:40Identification of Functionally Selective Alpha2C-AR Agonists as Potential New Drugs for Treatment of Pain
Eric JNOFF
(UCB, Braine-l'Alleud, Belgium)
16:15Session Chair
Ferran SANZ
(UNIVERSITY POMPEU FABRA, Barcelona, Spain)
16:20In Silico Models for Toxicity: Predicting the Challenging Endpoints
Mark CRONIN
(LIVERPOOL JOHN MOORES UNIVERSITY, Liverpool, United Kingdom)
17:00A Multiscale Simulation System for the Prediction of Drug Cardiotoxicity
Manuel PASTOR
(UNIVERSITY POMPEU FABRA, Barcelona, Spain)
17:40Systems Chemical Biology and Toxicogenomics
Karine AUDOUZE
(TECHNICAL UNIVERSITY OF DENMARK, Lyngby, Denmark)
10. Sunset Session: Careers in Medicinal Chemistry
18:00Session Chair
Janet ROBERTSON
(TES PHARMA, Corciano , Italy)
18:05From Graduate Student to Group Leader in Academia
Lennart BUNCH
(UNIVERSITY OF COPENHAGEN, Copenhagen, Denmark)
18:20Medicinal Chemistry Careers, a CRO's Perspective
Matthew TOZER
(PEAKDALE MOLECULAR, Cambridge, United Kingdom)
18:35Size Matters: Working as a Medicinal Chemist in Big Pharm
Simona CECCARELLI
(F. HOFFMANN-LA ROCHE, BASEL, Switzerland)
18:50Career Evolution in the Med Chem Department of a Small Drug Discovery Company
Riccardo ZANALETTI
(SIENA BIOTECH, Siena, Italy)
20:30Concert
07/09/2010
08:302010 IUPAC-RICHTER Prize Lecture
Behind the Design of Darunavir for HIV/AIDS and β-Secretase Inhibitors for Alzheimer's Disease
Arun K. GHOSH
(PURDUE UNIVERSITY, West Lafayette, United States)
Chair
Robin GANELLIN
(UNIVERSITY COLLEGE LONDON, London, United Kingdom)
09:15EFMC Prize for a Young Medicinal Chemist in Industry
Antonio NARDI
(GRÜNENTHAL, Aachen, Germany)
Chair
Mark BUNNAGE
(PFIZER, Boston, United States)
09:40EFMC Prize for a Young Medicinal Chemist in Academia
Andreas BENDER
(UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom)
Chair
Danijel KIKELJ
(UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia)
10:00Exhibition & Coffee
11. Emerging Technologies12. Novel Treatments for Obesity and Metabolic Disorders13. Successful Strategies in Lead Discovery
10:30Session Chair
David PARRY
(CYCLOFLUIDIC LTD, Welwyn Garden City Herts, United Kingdom)
10:35Microfluidics in Chemistry and Biology
David PARRY
(CYCLOFLUIDIC LTD, Welwyn Garden City Herts, United Kingdom)
11:15Advances in Mass Spectrometry Based Screening Technologies
John CROSBY
(BRISTOL UNIVERSITY, Bristol, United Kingdom)
11:35Open Pharmacological Space, an Innovative Medicines Initiative Knowledge Management Project
Bryn I. WILLIAMS-JONES
(PFIZER, Kent, United Kingdom)
11:55Nanotools for Biomedical Targets – Nanobodies Stabilize Active State of G-Protein Coupled Receptors
Jan STEYAERT
(VUB-VIB, Brussels, Belgium)
10:30Session Chair
Roberto PELLICCIARI
(UNIVERSITY OF PERUGIA & EFMC, Corciano, Italy)
10:35BA Signaling and the Control of Metabolism
Johan AUWERX
(EPFL, Lausanne, Switzerland)
11:15Testing the Concept of ACC Inhibition for the Treatment of Metabolic Diseases
Alleyn T. PLOWRIGHT
(SANOFI, Frankfurt-Am-Main, Germany)
11:35Discovery of a Novel Gut-Targeted Microsomal Triglyceride Transfer Protein Inhibitor (JNJ-16269110) to Treat Obesity: Proof of Concept
Lieven MEERPOEL
(JOHNSON & JOHNSON PRD, Beerse, Belgium)
11:55Discovery of a Second Generation FBPase Inhibitor, MB07803, with Improved Oral Bioavailability
Qun DANG
(MERCK, Rahway, United States)
10:30Session Chair
Hans Peter MAERKI
(F. HOFFMANN-LA ROCHE, Basel, Switzerland)
10:35Examples for Recent Successes in Drug Discovery
Torsten HOFFMANN
(F. HOFFMANN-LA ROCHE, Basel, Switzerland)
11:15Fragment Based Lead Discovery for Lectin Targets
Beat ERNST
(UNIVERSITY OF BASEL, Basel, Switzerland)
11:35Ensemblins: A New Class of Therapeutic Macrocycles
Nick TERRETT
(MERCK SHARP & DOHME RESEARCH GMBH (MSD), Kriens, Switzerland)
11:55Ferroquine, the Archetype Compound of Bioorganometallic Chemistry
Christophe BIOT
(UNIVERSITÉ LILLE 1, Villeneuve d'Ascq Cédex, France)
12:15Poster Session 2 - Lunch
12:15BIOSOLVEIT WORKSHOP
Fragment Based Ligand Design for Medicinal Chemists
14. Innovative Drug Delivery Systems and Nanotechnologies - EUFEPS Session15. Oncology Case Studies16. Natural Products in Drug Discovery - Beyond Cytotoxics and Antiinfectives
13:45Session Chair
Daan CROMMELIN
(TI PHARMA, Leiden, The Netherlands)
13:50Targeted Nanomedicines - Recent Progress in EU Sponsored Research
Gert STORM
(UTRECHT UNIVERSITY, Utrecht, The Netherlands)
14:30Therapeutic Nanoparticles for Improved and Safe Delivery of Drugs
Lucienne JUILLERAT
(CENTRE HOSPITALIER UNIVERSITAIRE VAUDOIS, Lausanne, Switzerland)
15:10Thiomer Micro- and Nanoparticles in Drug Delivery
Andreas BERNKOP-SCHNÜRCH
(LEOPOLD-FRANZENS UNIVERSITY, Innsbruck, Austria)
13:45Session Chair
Peter ETTMAYER
(BOEHRINGER INGELHEIM, Vienna, Austria)
13:45Discovery of Small Molecule Inhibitors of IGF-1R
Mark WITTMAN
(BRISTOL-MYERS SQUIBB CO., Wallingford, United States)
14:20Inhibitors of the MDM2-p53 Interaction
Lutz WEBER
(NEXUSPHARMA, Langhorne, United States)
14:55Discovery of a Potent and Selective SMO Inhibitor
Stefan PEUKERT
(NOVARTIS, Cambridge MA, United States)
13:45Session Chair
Gloria SERRA
(UDELAR, Montevideo, Uruguay)
13:50From Natural Products to Mitochondrial Targeting Agents
Peter WIPF
(UNIVERSITY OF PITTSBURGH, Pittsburgh, United States)
14:30Marine Natural Products as Drug Source
Mercedes ÁLVAREZ
(UNIVERSITY OF BARCELONA, Barcelona, Spain)
15:10Antibiotic Clusters
Pal HERCZEGH
(UNIVERSITY OF DEBRECEN, Debrecen, Hungary)
15:30Exhibition & Coffee
17. Imaging Biomarkers18. Hot Topics in Anti-Infectives19. Covalent Inhibitors in Drug Discovery
16:15Session Chair
Gilles TAMAGNAN
(INSTITUTE FOR NEURODEGENERATIVE DISORDERS AND MOLECULAR NEUROIMAGING, LLC, New Haven, United States)
16:15PET Imaging in the Discovery of New Therapeutics
Terence HAMILL
(MERCK RESEARCH LABORATORIES, West Point, United States)
16:50The Next Generation of PET Cardiac Imaging Agents: Discovery of Flurpiridaz F 18 for Detection of Coronary Disease and LMI1195 for Sympathetic Neuronal Imaging
Simon ROBINSON
(LANTHEUS MEDICAL IMAGING, North Billerica, United States)
17:25PET Imaging for Oncology
Christer HALLDIN
(KAROLINSKA INSTITUTET PET CENTRE, Stockholm, Sweden)
16:15Session Chair
Lieven MEERPOEL
(JOHNSON & JOHNSON PRD, Beerse, Belgium)
16:20Advances in Bacterial Fatty Acid Synthesis Inhibitors for Use against Toxoplasma gondii and Bacillus anthracis
Alan KOZIKOWSKI
(UNIVERSITY OF ILLINOIS, Chicago, United States)
17:00Benzoxaboroles as Anti-Infective Agents
Stephen BAKER
(ANACOR PHARMACEUTICALS, Palo Alto, United States)
17:20Discovery of TMC-207, a Novel Antituberculosis Agent
Jérôme GUILLEMONT
(TIBOTEC, Val de Reuil, France)
17:40HDAC Inhibitors Able to Reduce Acquired Antifungal Resistance
Antonello MAI
(UNIVERSITA DEGLI STUDI DI ROMA, Rome, Italy)
16:15Session Chair
Tjeerd BARF
(MERCK, Oss, The Netherlands)
16:20Renaissance of Covalent Inhibitors
Tjeerd BARF
(MERCK, Oss, The Netherlands)
17:00Harnessing the Power of Reversible, Covalent Inhibitors: the Discovery of Odanacatib
Cameron BLACK
(MERCK FROSST CENTRE FOR THERAPHEUTIC RESEARCH, Pointe-Claire-Dorval, Canada)
17:40Targeting Drug Resistance in Protein Kinases with Irreversible Inhibitors
Daniel RAUH
(CHEMICAL GENOMICS CENTRE OF THE MAX-PLANCK-SOCIETY, Dortmund, Germany)
20. Sunset Session: Academic curricula and industrial careers
More info
18:00Session Chair
Henk TIMMERMAN
(VU UNIVERSITY AMSTERDAM, Oegstgeest, The Netherlands)
18:05
Klaus MÜLLER
(F. HOFFMANN-LA ROCHE, Switzerland)
18:40
Gary TRESADERN
(JOHNSON & JOHNSON PHARMACEUTICAL R&D, Toledo, Spain)
18:55
Anne VALADE
(UCB, Braine-l'Alleud, Belgium)
08/09/2010
08:30The UCB-EHRLICH AWARD for Excellence in Medicinal Chemistry Lecture
New HIV Therapies: the Discovery of Maraviroc and Lersivirine
Anthony WOOD
(PFIZER, Waltham, United States)
Chair
Christophe GENICOT
(UCB SA, Bruxelles, Belgium)
09:15 The PROUS INSTITUTE-OVERTON & MEYER Award for New Technologies in Drug Discovery Lecture
(R)Evolutions in Drug Discovery through Conceptual and Technological Innovations
Klaus MÜLLER
(F. HOFFMANN-LA ROCHE, Switzerland)
Chair
David PROUS
(PROUS INSTITUTE FOR BIOMEDICAL RESEARCH, Barcelona, Spain)
10:00Exhibition & Coffee
21. Process R&D and Scale-up: Chemistry, Crystals & More - Challenges and Success Stories22. Emerging Drugs - Case Studies of Recently Disclosed New Medicines23. The Challenges in Designing Multi-Targeted Ligands and Drugs - the Good, the Bad and the Ugly (ACS Session I)
10:30Session Chair
Herbert STARK
(SANOFI-AVENTIS, FRANKFURT/MAIN, Germany)
10:35Scale-up of API Processes - Challenges of Solid State Properties: Case Studies
Roland THIEME
(HOFFMANN-LA ROCHE, Basel, Switzerland)
11:15Salt Selection for Scale up & Development: “The 100 mg –Approach”
Stefan BALBACH
(SANOFI-AVENTIS, Frankfurt/Main, Germany)
11:55Attrition Induced Grinding for the Synthesis of Some Commercial Drugs
Richard KELLOGG
(SYNCOM B.V., Groningen, The Netherlands)
10:30Session Chair
Nicholas CARRUTHERS
(JOHNSON & JOHNSON R&D, San Diego, United States)
10:35Dapagliflozin, a Novel SGLT2 Inhibitor
William WASHBURN
(BMS, Princeton, United States)
11:15A Novel CHK1 Inhibitor in Advanced Clinical Trials
Timothy GUZI
(SCHERING-PLOUGH RESEARCH INSTITUTE, Cambridge, United States)
11:35TMC 435, a Novel HCV Protease Inhibitor in Advanced Clinical Trials
Pierre RABOISSON
(JANSSEN PHARMACEUTICAL COMPANIES, Beerse, Belgium)
11:55Discovery of a Novel Orexin Receptor Antagonist for the Treatment of Sleep Disorders
Paul COLEMAN
(MERCK RESEARCH LABORATORIES, West Point, United States)
10:30Session Chair
John BUTERA
10:35Multi-Targeted Drug Discovery: Strategies and Challenges for Medicinal Chemists
Richard MORPHY
(MERCK, Lanarkshire, United Kingdom)
11:15Serotonin/Noradrenaline Reuptake Inhibitors:A Case History in the Challenges of Multipharmacology Drug Discovery
Florian WAKENHUT
(PFIZER CENTRAL RESEARCH, Kent, United Kingdom)
11:55Design, synthesis and evaluation of a series of Biphenylsulfonamides as potent dual Angiotensin II and Endothelin A receptor antagonists
William WASHBURN
(BMS, Princeton, United States)
12:15Poster Session 3 - Lunch
12:30ELSEVIER WORKSHOP
REAXYS WORKSHOP: "GETTING TO KNOW REAXYS – ENHANCING YOUR CHEMISTRY RESEARCH"
15:00Excursion
20:00Gala Dinner
09/09/2010
24. G-Protein Coupled 7TM Receptors - New Insights into their Structure and Ligand Recognition25. First Time Disclosures26. Targeting Protein-Protein Interaction (AFMC Session)
08:30Session Chair
Hans BRAUNER-OSBORNE
(THE DANISH UNIVERSITY OF PHARMACEUTICAL SCIENCES, Copenhagen, Denmark)
08:35New G-Protein Coupled Receptor Crystal Structures: Insights and Limitations
Gebhard F.X. SCHERTLER
(PAUL SCHERRER INSTITUTE, Villigen, Switzerland)
09:15Activation Mechanism of class C GPCRs
Jean-Philippe PIN
(CNRS-UNIVERSITY OF MONTPELLIER, Montpellier, France)
09:55Dualsteric Gpcr Targeting: A Novel Route To Subtype Selective Agonists And Antagonists Of The Muscarinic Receptors
Ulrike HOLZGRABE
(UNIVERSITY OF WUERZBURG, Wuerzburg, Germany)
08:30Session Chair
Eckhard OTTOW
(BAYER HEALTHCARE, Berlin, Germany)
08:35Structural Design and Optimization of Orally Available Renin Inhibitors
David CLAREMON
(VITAE PHARMACEUTICAL, Fort Washington, United States)
09:00BGG492, a Competitive AMPA/kainate Antagonist in Clinical Development for the Treatment of Migraine and Epilepsy
Yves P. AUBERSON
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland)
09:25Discovery of a Potent, Selective and Orally Bioavailable Acidic 11betaHydroxysteroid Dehydrogenase Type 1 (11beta-HSD1) Inhibitor
Paul WHITTAMORE
(ASTRAZENECA, Macclesfield, United Kingdom)
09:50MK-1903: a Potent Niacin Receptor (GPR109a/ HCA2) Agonist
Douglas BOATMAN
(ARENA PHARMACEUTICALS, San Diego, United States)
08:30Session Chair
Javier FERNANDEZ
(JANSSEN R&D, Toledo, Spain)
08:35Protein-Protein Interactions and Apoptosis in Cancer Cells
John FLYGARE
(GENENTECH, California, United States)
09:15Small molecule inhibitors of the neuropilin-1 VEGF-A interaction
Ashley JARVIS
(DOMAINEX LTD, Cambridge, United Kingdom)
09:55Targeting Pdz Domains: From Computational Library Design, To Nmr And X-Ray, To In Vivo Studies
Dmytro KOVALSKYY
(KIEV NATIONAL UNIVERSITY, KIEV, Ukraine)
10:15Exhibition & Coffee
27. Finding the Right Binding Pockets: Allosteric Modulators of G-Protein Coupled Receptors for Non-CNS Diseases(ACS Session II)28. Recent Case Studies in DD and Development 29. New Medicines Beyond Small Molecules - Novel Biologics
10:45Session Chair
Robert A. FECIK
(UNIVERSITY OF MINNESOTA, Minneapolis, United States)
10:50The Discovery of Maraviroc, an Allosteric CCR5 Antagonist for HIV Infection
Patrick DORR
(SURREY UNIVERSITY, Surrey, United Kingdom)
11:30Allosteric, Small Molecule Agonists of the GLP-1 Receptor for Diabetes
Lotte KNUDSEN
(NOVO-NORDISK, Bagsværd, Denmark)
12:10Follicle Stimulating Hormone Receptor Negative Allosteric Modulators (Fshr Nam): Discovery And Development Of A New Series Of Orally Bioavailable Dimethoxy-Benzamides
Jean-Philippe ROCHER
(ADDEX THERAPEUTICS, Plan-les-Ouates, Switzerland)
10:45Session Chair
Gerhard ECKER
(EFMC, UNIVERSITY OF VIENNA, Vienna, Austria)
10:50The Medicinal Chemistry of Glucokinase Activators - Property-based Drug Discovery
Craig JOHNSTONE
(ASTRAZENECA, Macclesfield, United Kingdom)
11:15Lead Development Strategies Utilized For The Discovery Of Dgat-1 Inhibitors
David PIOTROWSKI
(PFIZER GLOBAL R&D, Groton, United States)
11:40Towards The Clinic : The Fragment-Based Discovery And Development Of AT13387AU. A Potent Inhibitor Of The Molecular Chaperone Hsp90
Martyn FREDERICKSON
(ASTEX THERAPEUTICS LTD, Cambridge, United Kingdom)
12:05Phthalazinone Pyrazoles as Potent, Selective and Orally Bio-available Inhibitors of Aurora-A Kinase
Mike PRIME
(EVOTEC, Oxfordshire, United Kingdom)
10:45Session Chair
Hans Ulrich STILZ
(SANOFI-AVENTIS, Malov, Denmark)
10:50Immunotherapy of cancer with trifunctional antibodies: From bench to approval
Michael JAEGER
(TRION PHARMA, Munich, Germany)
11:30Nanobodies, from Camels to Therapeutic Proteins
Hilde REVETS
(UNIVERSITY OF ANTWERP, Antwerpen , Belgium)
12:10Engineered Protein Scaffolds as Next Generation Therapeutics
Arne SKERRA
(TECHNICAL UNIVERSITY MUNICH, München, Germany)
12:30CLOSING LECTURE

Drugging the "Undruggable"

Gregory L. VERDINE
(HARVARD UNIVERSITY, Cambridge, United States)
Chair
André TARTAR
(UNIVERSITY LILLE 2, Lille, France)
13:15Poster Prizes
Closing Remarks
Welcome to ISMC 2012
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