2010 Archived Content

Pharmacology-Driven Assays for Current Targets Banner 

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Recommended Short Courses*

Monday, June 14
9:00 am – 12:00 pm(SC1) Reactive Metabolites in Drug Discovery and Development-A Critical Examination of the Issues

2:00 pm – 5:00 pm(SC5) Dealing with the Blood-Brain Barrier


11:00 am Registration



Michele Palmer, Ph.D., Director of Screening, Chemical Biology Platform, Broad Institute of Harvard and MIT


Peter Hodder, Ph.D., Senior Director, Lead Identification, Translational Research Institute, The Scripps Research Institute

Larry A. Sklar, Ph.D., Distinguished Regents Professor, Pathology; Associate Director, Basic Research, University of New Mexico Cancer Center; Director, University of New Mexico Center for Molecular Discovery

Chahrzad Montrose-Rafizadeh, Ph.D., Senior Research Advisor, Eli Lilly

Successful collaboration can be measured in many ways: movement of a compound forward in the pipeline, outsourcing to knowledge centers resulting in decreased project costs and the ability to focus on multiple targets without sacrificing timelines. Panel topics will include a basic review of what specialized opportunities are available at academic screening centers, including a brief description of the Molecular Libraries Probe Production Centers (MLPCN). In addition, a “success story” from the pharmaceutical industry will be presented that demonstrates either a positive movement forward of a candidate due to the screening performed or another similar example of success.

12:30 pm Lunch on Your Own


1:55 Chairperson's Opening Remarks

Gül Erdemli, M.D., Ph.D., Head of Ion Channel Group, Lead Finding Platform, Novartis Institute for Biomedical Research

2:00 Discovery of Potent and Selective T-Type Voltage-Gated Calcium Channel Antagonists

Victor UebeleVictor Uebele, Ph.D., Senior Research Biologist, Depression & Circadian Disorders, Merck Research Laboratories

T-type voltage-gated calcium channels may play a role in various diseases including epilepsy, pain, cancer, diet-induced obesity and heart failure. In the 25 years since the description of T-type currents, only recently have the most selective and potent T-type antagonists been described. This presentation reviews the methods used to identify and characterize T-type antagonists including pharmacophore modeling and unbiased screening.

2:30 Automated Electrophysiology Technologies for Ion Channel Drug Discovery and Safety Profiling

Gül Erdemli, M.D., Ph.D., Head of Ion Channel Group, Lead Finding Platform, Novartis Institute for Biomedical Research

Recent developments in automated electrophysiology platforms have revolutionized ion channel drug discovery and safety profiling. However, there is a clear need for cost effective solutions to close the gap between primary and secondary screening for ligand-gated ion channels. The industry is also searching for novel technologies to enhance existing preclinical safety profiling approaches. Emerging novel microfluidic technologies promise the next breakthrough in this fast developing field.

Sponsored byMolecularDevices_New3:00 Introduction to the IonWorks Barracuda System: An Automated Electrophysiology Platform for Measuring Ligand- or Voltage-Gated Channels Simultaneously in 384 Wells
Karen Cook, Field Application Scientist, Molecular Devices, Inc.
The IonWorks Barracuda™ system allows simultaneous and continuous measurement of rapidly desensitizing ligand- (LGIC) and voltage-gated ion channels (VGICs). IonWorks Barracuda™ system is equipped with 384 individual patch-clamp amplifiers together with a 384-channel fluidic pipettor.  Currents are measured using either the single hole or the Population Patch Clamp recording technique developed by Molecular Devices. Data presented include LGIC recordings of nicotinic acetylcholine (a1 nACh) receptors, acid sensing ion channels (ASIC1a), and GABA chloride channels; as well as VGIC recordings of NaV, KV and hERG channels.  Pharmacological blockade of ion channel activity is also presented to validate the use of this automated, high-throughput system for screening ion channel targets in a drug discovery setting.


3:30 Networking Refreshment Break, Poster and Exhibit Viewing

4:30 Medicinal Chemistry Studies Leading to the Discovery of CP-810,123, a Selective ALPHA7 nAChR Agonist for the Treatment of Schizophrenia

Christopher J. O’Donnell, Ph.D., Senior Director, Neuroscience Chemistry, Pfizer, Inc.

CP-810,123 (4-(5-methyl-oxazolo[4,5-b]pyridin-2-yl)-1,4-diaza-bicyclo[3.2.2]nonane) is a potent and selective ALPHA7 nAChR agonist, with an excellent in vitro selectivity profile. The compound is characterized by rapid brain penetration, high oral bioavailability, high levels of receptor occupancy, and demonstrates in vivo efficacy in models of cognition. The SAR studies along with preclinical in vitro and in vivo data supporting the advancement of this compound to the clinic will be discussed.

5:00 Novel Ion Channel-Based Assays for Detecting and Characterizing 7TM Receptor Modulators

Colleen Niswender, Ph.D., Research Assistant Professor, Pharmacology, Vanderbilt University

Seven transmembrane receptors (7TM receptors) are known to modulate numerous ion conductances. Such modulation is physiologically important and also provides a mechanism to measure 7TM receptor activity. Activation of the intracellular ion channel s (IP3R) indirectly via Gq-coupled receptors is one of the most common assay formats for 7TM receptors. This presentation will discuss other functional 7TM assays using ion channels as effectors.

5:30 End of Conference Day

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