(SC1) Imaging Technologies for Target Discovery Over the last few years it has become evident, that imaging technologies are a very useful tool in drug discovery. This course is designed to provide information on optical and molecular imaging tools and the challenges, opportunities and limits will be discussed. An overview on optical and molecular imaging will be given. Topics to be covered:
9:00 am Richard M. Levenson, M.D., Vice President, CRI, Inc.
9:55 Anatomical and functional imaging using micro-CT and digital subtraction angiography in small animalsCristian Badea, PhD, Assistant Professor of Radiology, Center for In Vivo Microscopy, Duke University Medical Center
10:45am-11:00am Coffee Break
11:00 am imaging RNA in vivoNatalia E. Broude, Ph.D., Research Associate Professor, Department of Biomedical Engineering, Boston University
12:00 pm End of Short Course
(SC2) Understanding the Structural Biology of Ion Channels to Guide Drug DiscoveryDuring the past decade there have been two remarkable technological breakthroughs which have transformed ion channel-based drug discovery. The fi rst advance is using X-ray crystallography and solid-state NMR to solve the structures of ion channels, which enabled structure-guided drug design of ion-channel blockers. The other advance is the development of automated assays such as FLIPR and Ionworks which have high-throughput screening of ion channel blocking compounds a reality. This short course is an overview on the cutting-edge development of structure-based design of ion channel blockers. Several leading experts in the field will provide road maps to starters as well as contributing experiences of several complementary a proaches.Topics to be covered:
Tutors:Heike Wulff, Ph.D., Assistant Professor, University of California – Davis
(SC3) Advances in DNA Methylation AnalysisDNA methylation refers to the addition of methyl groups catalyzed by the enzyme, DNA methyltransferase to cytosines in CpG dinucleotides. This biochemical event has now come to be recognized as an important epigenetic phenomenon that affects gene expression. In recent years this field has been an area of intense activity and several new methodologies and applications for DNA methylation analysis have rapidly emerged. This course will cover the basics underlying the various techniques that have been developed and the context in which they have been successfully used. The advantages and limitations of the various methodologies will be discussed and appropriate case studies will be presented to demonstrate their use in biological, medical or epidemiological studies. The course will be offered in an informal, interactive setting to enable a free exchange of ideas and information.
8:30 am Pre-Conference Short Course Registration
9:00 Daniel Weisenberger, Ph.D., Laboratory Manager, Epigenome Center, University of Southern California
Techniques for DNA Methylation
9:35 Christoph Bock, Ph.D., Junior Group Leader for Computational Epigenetics, Max Planck Institute for Informatics
Bioinformatic Methods for DNA Methylation Analysis and Epigenetic Biomarker Discovery
10:10 Shannon Payne, Ph.D., Senior Scientist, Epigenomics Inc.
Clinical Applications of DNA Methylation
10:45 – 11:00 Networking Refreshment Break
11:00 – 11:45 Open discussion
11:45 – 12:00 Summary of key takeaways by the tutors
12:00 Course Adjourns
*separate registration required
(SC4) Tackling RNAi DeliveryThe course is designed to provide both the beginner and the expert, with a comprehensive overview of current and emerging delivery systems and formulations facilitating RNAi delivery. Various methods for RNAi delivery such as viral vectors, liposomes, nanoparticles, chemical conjugates and other commonly used techniques will be compared and contrasted for different applications. The instructors will also discuss the challenges associated with the delivery of a wide array of RNA molecules such as siRNAs, shRNAs, aptamers and miRNAs and offer guidance based on their knowledge and expertise in the fi eld. The course is offered in an informal and interactive setting to enable free exchange of ideas and information.
1:30 pm Pre-Conference Short Course Registration
2:00 Muthiah Manoharan, Ph.D., Vice President, Drug Discovery, Alnylam Pharmaceuticals
Improved Delivery by Chemical Modifications
2:35 Ian MacLachlan, Ph.D., Chief Scientific Officer, Tekmira Pharmaceuticals Inc.
Improved Delivery by Formulation Design
3:10 Speaker to be announced
Improved Delivery Using Viral Vectors
3:45 – 4:00 Networking Refreshment Break
4:00 – 4:45 Open discussion
4:45 – 5:00 Summary of key takeaways by the tutors
5:00 Course Adjourns
(SC5) Ion Channel Assays for Safety Screening Ion channels are involved in a complex and intricate signaling system that play an important role in affecting the cellular response to a drug and hence to the overall patient safety. For instance, the hERG potassium channel plays an important role in repolarization of cardiac myocytes and other sodium and calcium channels also control of ionic current fl ow in various cells. Drug-induced alterations in the translation and traffi cking of the ion channel proteins and drug-induced blockade of channels resulting in reductions in ionic current are all thought be contribute to drug-related adverse events. in vitro assays using isolated cells, cell lines, and expression systems cloned for specifi c ion channels are now routinely used to predict the drug response. Electrophysiology experiments, using conscious or anaesthetized animals, are also conducted to identify potential drug liabilities. Over the years there have been significant improvements in both the technology and in the scientifi c understanding of how ion channels can impact drug safety. This course provides a detailed overview of the types of ion channelbased screening assays and technologies that are in use and how they are being applied to effectively monitor and predict drug safety.
2:00 Harry Witchel, Ph.D., Senior Lecturer in Physiology, Brighton and Sussex Medical School
Cardiac Ion Channels and Their Role in Drug-Induced Toxicity
2:35 Laszlo Urban, M.D., Ph.D., Executive Director, Global Head, Preclinical Safety Profiling, Novartis Institutes for Biomedical Research Inc.
Addressing cardiac safety in drug discovery (up to clinical candidate)
3:10 Huabin Sun, M.D., Senior Research Investigator, Cardiovascular Safety Pharmacology, Discovery Toxicology, Bristol-Myers Squibb
Ex vivo and in vivo assays for assessing off-target ion channel liabilities
(SC6) Screening For Potential Drug Targets - Design Strategies for Novel-Generation Kinase InhibitorsThe structural coverage of the human kinome has signifi cantly increased in the last few years. This course will provide useful insights and information on how fragment-based design offers an opportunity for assembling novel inhibitors, monitoring their binding kinetics and improving the residence time. Specific focus on screening technologies such as X-rays will be given.Topics to be covered:
Agenda:
2pm IntroductionGerhard Müller, Ph.D., Chief Scientifi c Offi cer, Proteros Fragments, GmbH
2:10 Binding Kinetics in Drug DiscoveryGerhard Müller, Ph.D., Chief Scientifi c Offi cer, Proteros Fragments, GmbH
2:55 Design Principles of Novel Kinase InhibitorsPeter Sennhenn, Ph.D., Director, Med Chem, Proteros fragments, GmbH
3:40 – 4:00 Refreshment Break
4:00 Kinase Inhibitor – directed Chemistry and LibrariesFrank Leemhuis, Ph.D., Managing Director, MercaChem
4:45 Fragments, Kinetics and Kinase InhibitorsGerhard Müller, Ph.D., Chief Scientifi c Offi cer, Proteros Fragments GmbH 5:00 End of Course
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