The concise guide to PHARMACOLOGY 2013/14: Ion channels
Stephen P.H. Alexander,Helen E. Benson,Elena Faccenda,Adam J. Pawson,Joanna L. Sharman,William A. Catterall,Michael Spedding,John A. Peters,Anthony J. Harmar +8 more
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TLDR
The Concise Guide to PHARMACOLOGY 2013/14 provides concise overviews of the key properties of over 2000 human drug targets with their pharmacology, plus links to an open access knowledgebase of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties.Abstract:
Class II PI3Ks (EC 2.7.1.154) phosphorylate phosphatidylinositol to generate phosphatidylinositol 3-phosphate (and possibly phosphatidylinositol 4-phosphate to generate phosphatidylinositol 3,4-bisphosphate). Three monomeric members exist, PI3K-C2α, β and γ, and include Ras-binding, Phox homology and two C2domains.read more
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Are cannabidiol and Δ9‐tetrahydrocannabivarin negative modulators of the endocannabinoid system? A systematic review
TL;DR: The evidence indicates that CBD and THCV are not rimonabant‐like in their action and thus appear very unlikely to produce unwanted CNS effects, illustrating how in vitro mechanistic studies do not always predict in vivo pharmacology and underlie the necessity of testing compounds in vivo before drawing any conclusion on their functional activity at a given target.
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Dopamine receptors – IUPHAR Review 13
TL;DR: An update of the current knowledge regarding the complex biology, signalling, physiology and pharmacology of dopamine receptors is provided.
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Mechanisms of Action of Antiseizure Drugs and the Ketogenic Diet
TL;DR: The ketogenic diet leads to increases in circulating ketones, which may contribute to the efficacy in treating pharmacoresistant seizures, and is one treatment option for drug-resistant patients.
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International Union of Basic and Clinical Pharmacology. XCI. Structure, Function, and Pharmacology of Acid-Sensing Ion Channels and the Epithelial Na+ Channel
TL;DR: The analysis of the homologies between ENaC and ASICs and the relation between functional and structural information shows many parallels between these channels, suggesting that some mechanisms that control channel activity are shared between ASICs
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Novel lead structures and activation mechanisms for CO‐releasing molecules (CORMs)
TL;DR: This review explores solid storage and delivery forms for CO, and the attachment of CORMs to hard and soft nanomaterials to confer additional target specificity to such systems is critically assessed, and analytical methods for the study of the stoichiometry and kinetics of CO release are surveyed.
References
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International Union of Pharmacology: Approaches to the Nomenclature of Voltage-Gated Ion Channels
William A. Catterall,K. G. Chandy,David E. Clapham,George A. Gutman,Franz Hofmann,Anthony J. Harmar,Darrell R. Abernethy,Michael Spedding +7 more
TL;DR: This issue of Pharmacological Reviews includes a new venture in the collaboration between the International Union of Pharmacology (IUPHAR) and the American Society for Pharmacology and Experimental Therapeutics (ASPET), in that a new classification of voltage-gated ion channels is outlined.
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How many drug targets are there
TL;DR: A consensus number of current drug targets for all classes of approved therapeutic drugs is proposed, and an emerging realization of the importance of polypharmacology and also the power of a gene-family-led approach in generating novel and important therapies is highlighted.
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ANKTM1, a TRP-like Channel Expressed in Nociceptive Neurons, Is Activated by Cold Temperatures
Gina M. Story,Andrea M. Peier,Alison J. Reeve,Samer R. Eid,Johannes Mosbacher,Todd R. Hricik,Taryn J. Earley,Anne C. Hergarden,David Andersson,Sun Wook Hwang,Peter McIntyre,Timothy Jegla,Stuart Bevan,Ardem Patapoutian,Ardem Patapoutian +14 more
TL;DR: The characterization of ANKTM1 is described, a cold-activated channel with a lower activation temperature compared to the cold and menthol receptor, TRPM8, which is found in a subset of nociceptive sensory neurons where it is coexpressed with TRPV1/VR1 (the capsaicin/heat receptor) but not TRPM 8.
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International Union of Pharmacology. XLVIII. Nomenclature and Structure-Function Relationships of Voltage-Gated Calcium Channels
TL;DR: The molecular relationships and physiological functions of these calcium channel proteins are presented and comprehensive information on their molecular, genetic, physiological, and pharmacological properties is provided.
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From Ionic Currents to Molecular Mechanisms: The Structure and Function of Voltage-Gated Sodium Channels
TL;DR: Together, these studies showed that the mechanisms of sodium channel function and regulation, purified sodium channel protein contained the essential and gives a perspective for future research on the ex-elements for ion conduction and voltage-dependent panding family of Sodium channel proteins.