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TUESDAY, NOVEMBER 3
7:30 am Continental Breakfast Breakout Discussion Sessions
8:30 Chairperson’s Remarks
8:40 Target Occupancy Studies - Preclinical Decision-making Data Amenable to Clinical Translation
Sarah Grimwood, Ph.D., Group Lead, Neuroscience Translational Biomarkers, Pfizer, Inc.
What percentage of target binding sites must be occupied by drugs to trigger therapeutic effects in patients? This talk will review clinical literature data available to help answer this question for ion channel drug targets, obtained using positron emission tomography (PET). In addition, the preclinical methodology available for target occupancy studies will be discussed, providing examples towards building an understanding of the target occupancy required to provide efficacy in preclinical models and how to translate this to the clinic.
9:10 Evaluation of Available Technologies for Ligand-gated Ion Channel Safety Profiling and Screening
Gul Erdemli, M.D., Ph.D., Head, Ion Channel Group, Novartis Institutes for BioMedical Research, Inc.
9:40 Networking Coffee Break in the Exhibit Hall
10:40 CRAC Channels in Lymphocyte Function: Lessons from STIM1 and ORAI1 Deficient Human Patients and Mice
Stefan Feske, M.D., Assistant Professor, Department of Pathology, New York University, Langone Medical Center
Store-operated Ca2+ influx through Ca2+-release activated Ca2+ (CRAC) channels is arguably the most important mechanism to generate Ca2+ signals in lymphocytes. ORAI1 functions as pore subunit of the CRAC channel which is activated by stromal interaction molecule 1 (STIM1) in response to depletion of ER Ca2+ stores. The pathway is essential for functional immune responses involving T cells, mast cells and potentially other cells in the immune system. I discuss mechanisms of CRAC channel activation, phenotypes of human patients and mice lacking functional ORAI1 and STIM1 and the potential role of this pathway in inflammatory disease.
11:10 Perspectives on TRPA1 as a Pain Target: Challenges and Progress
Regina Reilley, Ph.D., Senior Group Leader, Neuroscience Discovery, Abbott Laboratories
11:40 Chloride Channels are Drug Targets
Alan S. Verkman, M.D., Ph.D., Professor, Department of Medicine and Physiology, University of California, San Francisco
Chloride channels represent a relatively underexplored target class for drug discovery, as elucidation of their identity and physiological roles has lagged behind many other drug targets. They are involved in a wide variety of biological functions, and mutations in chloride channels cause human diseases, including cystic fibrosis, macular degeneration, myotonia, kidney stones, renal salt wasting, hyperekplexia, and others. Chloride channel modulators have potential applications in the therapy of some of these disorders, as well as in secretory diarrheas, polycystic kidney disease, osteoporosis and hypertension.
12:10 pm Ion Channels as Mediators of Urinary Bladder Overactivity
Kevin S. Thorneloe, Ph.D., Investigator, Metabolic Pathways CEDD, GlaxoSmithKline Pharmaceuticals
12:40 Close of Conference
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