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Ion Channels


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George ChandyGeorge K. Chandy, Ph.D., Professor, Physiology & BioPhysics, School of Medicine, University of California - Irvine




Michael DabrowskiMichael Dabrowski, Ph.D., Head of Global Ion Channel Initiative, AstraZeneca




Laszlo KissLaszlo Kiss, Ph.D., Senior Research Fellow, Merck Research Laboratories





Ion Channels as Therapeutic Targets: An Industry Minireview
Peter Haddock, Ph.D., Group Leader, Ion Channel Group & CNS Biology, Pfizer

Anindya Bhattacharya, Ph.D., Johnson & Johnson Pharmaceutical Research and Development LLC

Neil A. Castle, Ph.D., Icagen Inc.

George K. Chandy, M.D., Ph.D., University of California - Irvine

Mark (Mao Xiang) Chen, Ph.D., GlaxoSmithKline Research and Development

Chuan-Chu Chou, Ph.D., Schering Plough Research Institute

Michael Dabrowski, Ph.D., AstraZeneca

Gary Desir, M.D., Yale University School of Medicine

Jesus ‘Tito’ Gonzalez, Ph.D., Vertex Pharmaceuticals

Akihiko Kato, Ph.D., Eli Lilly and Company

Laszlo Kiss, Ph.D., Merck Research Laboratories

Roland Kozlowski, Ph.D., Lectus

Michael Mayer, Ph.D., University of Michigan

Dinah Misner, Ph.D., Roche Palo Alto

Birgit T. Priest, Ph.D., Merck Research Laboratories

Ken Stauderman, Ph.D., CalciMedica

Nuria Tamayo, Ph.D., Amgen



Understanding the Structural Biology of Ion Channels to Guide Drug Discovery
Heike Wulff, Ph.D., University of California - Davis
Boris S. Zhorov, Ph.D., D.Sc., McMaster University

Ion Channel Assays for Safety Screening
Gary Gintant, Ph.D., Abbott Laboratories
Laszlo Urban, M.D., Ph.D., Novartis Institutes for Biomedical Research
Harry Witchel, Ph.D., Brighton and Sussex Medical School




(SC2) Understanding the Structural Biology of Ion Channels to Guide Drug Discovery

During the past decade there have been two remarkable technological breakthroughs which have transformed ion channel-based drug discovery.  The first 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 approaches.

Topics to be covered:

  • Pinpointing ion channel domains critical for specificity and activity
  • Looking at 3-D structure for selectivity and specificty
  • Oligomerization of ion channels – implications for tissue specificity
  • Designing expression systems that produce truly representative channels for screening

Tutors: Heike Wulff, Ph.D., Assistant Professor, University of California - Davis
Boris S. Zhorov, Ph.D., D.Sc., Professor, Department of Biochemistry and Biomedical Sciences, McMaster University

1:30 – 2:00 Afternoon Pre-Conference Registration

2:00 – 5:00
(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 flow in various cells. Drug-induced alterations in the translation and trafficking 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 specific 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 scientific understanding of how ion channels can impact drug safety. This course provides a detailed overview of the types of ion channel-based screening assays and technologies that are in use and how they are being applied to effectively monitor and predict drug safety.

Topics to be covered:

  • Overview of current and emerging assays and methodologies
  • Discussion on when and how to use these assays
  • Use of automation and high-throughput techniques
  • Comparison of platforms and applications
  • Factors affecting sensitivity and specificity
  • Emerging applications such as determining off-target adverse drug effects, looking beyond hERG channels, using action potentials as integrated test systems

Moderator: J. Rick Turner, Ph.D., PGCE, MICR, Chairman, Department of Clinical Research and Director, Cardiac Safety Education Center, Campbell University School of Pharmacy

Tutors: Gary Gintant, Ph.D., Senior Group Leader, Department of Integrative Pharmacology, Abbott Laboratories
Laszlo Urban, M.D., Ph.D., Executive Director and Global Head, Preclinical Safety Profiling, Novartis Institutes for Biomedical Research Inc.
Harry Witchel, Ph.D., Senior Lecturer in Physiology, Brighton and Sussex Medical School

*separate registration required


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Targeting RB