Voltage-Gated Ion Channels as Drug Targets. Methods and Principles in Medicinal Chemistry, Vol. 29. Edited by David J. Triggle, Murali Gopalakrishnan, David Rampe and Wei Zheng.

2006 ◽  
Vol 45 (33) ◽  
pp. 5414-5414
Author(s):  
Philipp Reiß ◽  
Ulrich Koert
Keyword(s):  
Ion Channels ◽  
Drug Targets ◽  
Medicinal Chemistry ◽  
Voltage Gated ◽  
Voltage Gated Ion Channels ◽  
Gated Ion Channels

scholarly journals Optical electrophysiology for probing function and pharmacology of voltage-gated ion channels

eLife ◽  
2016 ◽  
Vol 5 ◽  
Author(s):  
Hongkang Zhang ◽  
Elaine Reichert ◽  
Adam E Cohen
Keyword(s):  
Ion Channels ◽  
Voltage Clamp ◽  
High Throughput Screening ◽  
Drug Targets ◽  
Inhibitory Effect ◽  
Optical Measurements ◽  
Voltage Gated ◽  
State Dependent ◽  
Voltage Gated Ion Channels ◽  
Gated Ion Channels

Voltage-gated ion channels mediate electrical dynamics in excitable tissues and are an important class of drug targets. Channels can gate in sub-millisecond timescales, show complex manifolds of conformational states, and often show state-dependent pharmacology. Mechanistic studies of ion channels typically involve sophisticated voltage-clamp protocols applied through manual or automated electrophysiology. Here, we develop all-optical electrophysiology techniques to study activity-dependent modulation of ion channels, in a format compatible with high-throughput screening. Using optical electrophysiology, we recapitulate many voltage-clamp protocols and apply to Nav1.7, a channel implicated in pain. Optical measurements reveal that a sustained depolarization strongly potentiates the inhibitory effect of PF-04856264, a Nav1.7-specific blocker. In a pilot screen, we stratify a library of 320 FDA-approved compounds by binding mechanism and kinetics, and find close concordance with patch clamp measurements. Optical electrophysiology provides a favorable tradeoff between throughput and information content for studies of NaV channels, and possibly other voltage-gated channels.

scholarly journals Drug targets: ligand and voltage gated ion channels

2017 ◽  
Vol 6 (2) ◽  
pp. 235 ◽  
Author(s):  
Nilan T. Jacob
Keyword(s):  
Drug Discovery ◽  
Ion Channels ◽  
Drug Targets ◽  
Target Identification ◽  
Ion Flow ◽  
Voltage Gated ◽  
Initial Stage ◽  
Voltage Gated Ion Channels ◽  
Channel Architecture ◽  
Gated Ion Channels

The elucidation of a drug target is one of the earliest and most important steps in the drug discovery process. Ion channels encompassing both the ligand gated and voltage gated types are the second most common drug targets after G-Protein Coupled Receptors (GPCR). Ion channels are basically pore forming membrane proteins specialized for conductance of ions as per the concentration gradient. They are further broadly classified based on the energy (ATP) dependence into active ion channels/pumps and passive ion channels. Gating is the regulatory mechanism of these ion channels by which binding of a specific molecule or alteration in membrane potential induces conformational change in the channel architecture to result in ion flow or its inhibition. Thus, the study of ligand and voltage gated ion channels becomes an important tool for drug discovery especially during the initial stage of target identification. This review aims to describe the ligand and voltage gated ion channels along with discussion on its subfamilies, channel architecture and key pharmacological modulators.

Voltage-Gated Ion Channels, New Targets in Anti-Cancer Research

2007 ◽  
Vol 2 (3) ◽  
pp. 189-202 ◽  
Author(s):  
Le Jean-Yves ◽  
Ouadid-Ahidouch Halima ◽  
Soriani Olivier ◽  
Besson Pierre ◽  
Ahidouch Ahmed ◽  
...  
Keyword(s):  
Cancer Research ◽  
Ion Channels ◽  
Voltage Gated ◽  
New Targets ◽  
Anti Cancer ◽  
Voltage Gated Ion Channels ◽  
Gated Ion Channels

scholarly journals Expression and Distribution of Voltage Gated Ion Channels in Ferret SA Node

2009 ◽  
Vol 96 (3) ◽  
pp. 261a
Author(s):  
Muugu V. Brahmajothi ◽  
Michael. J. Morales ◽  
Donald L. Campbell ◽  
Charles Steenbergen ◽  
Harold C. Strauss
Keyword(s):  
Ion Channels ◽  
Voltage Gated ◽  
Sa Node ◽  
Voltage Gated Ion Channels ◽  
Gated Ion Channels
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