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Speaker: Fernanda Laezza
Associate Professor, Department of Pharmacology and Toxicology

Keck Seminar, Fernanda Laezza, UTMB

Friday, February 24, 2017
4:00 PM  to 5:00 PM

Auditorium  BioScience Research Collaborative
Rice University
6500 Main St
Houston, Texas, USA

Redesigning Allostery for CNS Drug Discovery Growing appreciation that ion channels and receptors operate as macromolecular complexes, necessitates drug development strategies beyond conventional pharmacology. In the brain, proteinprotein interactions within ion channel complexes offer innovative opportunities in the drug discovery arena. Their highly specific and flexible interfaces define nanodomains that are associated with physiologically- and disease-relevant effects of the ion channels and can be targeted as allosteric surfaces for probe and drug development. During my talk, I will present the discovery and development of new allosteric modulators targeting the voltage-gated Na+ channel, the molecular determinant of the action potential in neurons. Cutting-edge methods ranging from medicinal chemistry, split-luciferase assays, nano LC-MS/MS, single cell and brain circuit electrophysiology to in vivo genetic silencing will be discussed. Inspired by a minimal functional domain top-down approach, our strategy is a paradigm shift in ion channel probe design that will provide a transformative platform to accelerate drug discovery in the CNS.

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