Ion channels are well recognized as important therapeutic targets for treating a number of different pathophysiologies. Voltagegated potassium channels as therapeutic drug targets. Voltagegated sodium nav channels are a family of transmembrane ion channel proteins. Given the strong historical precedent that exists for discovering and commercializing successful drugs that modulate the activity of voltagegated sodium. 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. Edited by the most prominent person in the field and top researchers at us pharmaceutical companies, this is a unique resource for drug developers and physiologists seeking a molecularlevel understanding of ion channel pharmacology. Voltagegated ion channels as drug targets, volume 29. Ion channels as drug targets in central nervous system disorders. Voltagegated potassium channels as therapeutic targets. Ion channels are important drug targets because they.
Historically, however, development of drugs targeting this protein class has. 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. These heteromeric poreforming structures are typically. The elucidation of a drug target is one of the earliest and most important steps in the. Voltagegated ion channels as drug targets pdf free download. Voltage gated sodium channels as drug discovery targets. 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. 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. The voltagegated ion channel family consists of more than. After an introduction to the topic, the authors evaluate the structure and function of ion channels, as well as related drug interaction. K v channels offer tremendous opportunities for the development of new drugs for cancer, autoimmune. A section on assay technologies is followed by a section each on calcium, sodium and potassium channels. Ion channels are important drug targets because they play. The voltagegated sodium channels vgscs are heteromeric transmembrane proteins which open in response to alteration in membrane potential to provide.
They function by forming a gated, waterfilled pore. Ligandgated ion channels lgics mediate passive ion flux driven by the electrochemical gradient for the permeant ions. Voltagegated ion channels as drug targets edited by d. Voltagegated ion channels as drug targets methods and. Ion channels encompassing both the ligand gated and voltage gated types are the. The elucidation of a drug target is one of the earliest and most important steps in the drug discovery process. Pdf the elucidation of a drug target is one of the earliest and most important steps in the drug discovery process.