Nvoltage-gated ion channels as drug targets pdf

The elucidation of a drug target is one of the earliest and most important steps in the drug discovery process. Voltagegated sodium nav channels are a family of transmembrane ion channel proteins. Pdf the elucidation of a drug target is one of the earliest and most important steps in the drug discovery process. Voltagegated potassium channels as therapeutic drug targets. Ion channels encompassing both the ligand gated and voltage gated types are the.

Voltagegated ion channels as drug targets, volume 29. Ligandgated ion channels lgics mediate passive ion flux driven by the electrochemical gradient for the permeant ions. K v channels offer tremendous opportunities for the development of new drugs for cancer, autoimmune. Ion channels are important drug targets because they play a crucial role in controlling a very wide spectrum of physiological processes hille, 2001, and because their dysfunction can lead to pathophysiology ashcroft, 2000.

Lgics are gated by the binding of a specific ligand to an orthosteric sites that triggers a conformational change that results in the conducting state, or by binding of endogenous, or exogenous, modulators to allosteric sites. A section on assay technologies is followed by a section each on calcium, sodium and potassium channels. The voltagegated ion channel family consists of more than. These heteromeric poreforming structures are typically. Voltagegated ion channels as drug targets pdf free download. The human genome contains 40 voltagegated potassium channels k v which are involved in diverse physiological processes ranging from repolarization of neuronal or cardiac action potentials, over regulating calcium signaling and cell volume, to driving cellular proliferation and migration. They function by forming a gated, waterfilled pore. The elucidation of a drug target is one of the earliest and most important steps in the. Voltagegated ion channels as drug targets edited by d.

After an introduction to the topic, the authors evaluate the structure and function of ion channels, as well as related drug interaction. Voltage gated sodium channels as drug discovery targets. Voltagegated potassium channels as therapeutic targets. Ion channels are well recognized as important therapeutic targets for treating a number of different pathophysiologies. State dependence, voltage dependence, and the modulated receptor model 24 use dependence 28 physical meaning of state dependence 30 state dependence in drug discovery 31 future directions for ion channel drug discovery 33 voltagegated ion channels as drug targets. Ion channels as drug targets in central nervous system disorders.