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  • International Union of Basic and Clinical Pharmacology CIII: Chemerin Receptors CMKLR1 (Chemerin1) and GPR1 (Chemerin2) Nomenclature, Pharmacology, and Function
    Pharmacol. Rev. (IF 17.893) Pub Date : 2018-01-01
    Amanda J. Kennedy,Anthony P. Davenport,Eliot H. Ohlstein,ASSOCIATE EDITOR,Amanda J. Kennedy,Anthony P. Davenport,Amanda J. Kennedy,Anthony P. Davenport
    更新日期:2017-12-27
  • Ion Channels in Genetic Epilepsy: From Genes and Mechanisms to Disease-Targeted Therapies
    Pharmacol. Rev. (IF 17.893) Pub Date : 2018-01-01
    Julia Oyrer,Snezana Maljevic,Ingrid E. Scheffer,Samuel F. Berkovic,Steven Petrou,Christopher A. Reid,Patrick M. Sexton,ASSOCIATE EDITOR,Julia Oyrer,Snezana Maljevic,Ingrid E. Scheffer,Samuel F. Berkovic,Steven Petrou,Christopher A. Reid,Julia Oyrer,Snezana Maljevic,Ingrid E. Scheffer,Samuel F. Berkovic,Steven Petrou,Christopher A. Reid

    Epilepsy is a common and serious neurologic disease with a strong genetic component. Genetic studies have identified an increasing collection of disease-causing genes. The impact of these genetic discoveries is wide reaching—from precise diagnosis and classification of syndromes to the discovery and validation of new drug targets and the development of disease-targeted therapeutic strategies. About 25% of genes identified in epilepsy encode ion channels. Much of our understanding of disease mechanisms comes from work focused on this class of protein. In this study, we review the genetic, molecular, and physiologic evidence supporting the pathogenic role of a number of different voltage- and ligand-activated ion channels in genetic epilepsy. We also review proposed disease mechanisms for each ion channel and highlight targeted therapeutic strategies.

    更新日期:2017-12-21
  • WNT Signaling in Cardiac and Vascular Disease
    Pharmacol. Rev. (IF 17.893) Pub Date : 2018-01-01
    Sébastien Foulquier,Evangelos P. Daskalopoulos,Gentian Lluri,Kevin C. M. Hermans,Arjun Deb,W. Matthijs Blankesteijn,Martin C. Michel,ASSOCIATE EDITOR,Sébastien Foulquier,Evangelos P. Daskalopoulos,Gentian Lluri,Kevin C. M. Hermans,Arjun Deb,W. Matthijs Blankesteijn,Sébastien Foulquier,Evangelos P. Daskalopoulos,Gentian Lluri,Kevin C. M. Hermans,Arjun Deb,W. Matthijs Blankesteijn
    更新日期:2017-12-16
  • G Protein–Coupled Receptors Targeting Insulin Resistance, Obesity, and Type 2 Diabetes Mellitus
    Pharmacol. Rev. (IF 17.893) Pub Date : 2018-01-01
    Darren M. Riddy,Philippe Delerive,Roger J. Summers,Patrick M. Sexton,Christopher J. Langmead,Eric L. Barker,ASSOCIATE EDITOR,Darren M. Riddy,Philippe Delerive,Roger J. Summers,Patrick M. Sexton,Christopher J. Langmead,Darren M. Riddy,Philippe Delerive,Roger J. Summers,Patrick M. Sexton,Christopher J. Langmead

    G protein–coupled receptors (GPCRs) continue to be important discovery targets for the treatment of type 2 diabetes mellitus (T2DM). Many GPCRs are directly involved in the development of insulin resistance and β-cell dysfunction, and in the etiology of inflammation that can lead to obesity-induced T2DM. This review summarizes the current literature describing a number of well-validated GPCR targets, but also outlines several new and promising targets for drug discovery. We highlight the importance of understanding the role of these receptors in the disease pathology, and their basic pharmacology, which will pave the way to the development of novel pharmacological probes that will enable these targets to fulfill their promise for the treatment of these metabolic disorders.

    更新日期:2017-12-13
  • Anti-Inflammatory Effects of Omega-3 Fatty Acids in the Brain: Physiological Mechanisms and Relevance to Pharmacology
    Pharmacol. Rev. (IF 17.893) Pub Date : 2018-01-01
    Sophie Layé,Agnès Nadjar,Corinne Joffre,Richard P. Bazinet,Robert Dantzer,ASSOCIATE EDITOR,Sophie Layé,Agnès Nadjar,Corinne Joffre,Richard P. Bazinet,Sophie Layé,Agnès Nadjar,Corinne Joffre,Richard P. Bazinet

    Classically, polyunsaturated fatty acids (PUFA) were largely thought to be relatively inert structural components of brain, largely important for the formation of cellular membranes. Over the past 10 years, a host of bioactive lipid mediators that are enzymatically derived from arachidonic acid, the main n-6 PUFA, and docosahexaenoic acid, the main n-3 PUFA in the brain, known to regulate peripheral immune function, have been detected in the brain and shown to regulate microglia activation. Recent advances have focused on how PUFA regulate the molecular signaling of microglia, especially in the context of neuroinflammation and behavior. Several active drugs regulate brain lipid signaling and provide proof of concept for targeting the brain. Because brain lipid metabolism relies on a complex integration of diet, peripheral metabolism, including the liver and blood, which supply the brain with PUFAs that can be altered by genetics, sex, and aging, there are many pathways that can be disrupted, leading to altered brain lipid homeostasis. Brain lipid signaling pathways are altered in neurologic disorders and may be viable targets for the development of novel therapeutics. In this study, we discuss in particular how n-3 PUFAs and their metabolites regulate microglia phenotype and function to exert their anti-inflammatory and proresolving activities in the brain.

    更新日期:2017-12-10
  • RAL GTPases: Biology and Potential as Therapeutic Targets in Cancer
    Pharmacol. Rev. (IF 17.893) Pub Date : 2018-01-01
    Chao Yan,Dan Theodorescu,Richard Dequan Ye,ASSOCIATE EDITOR,Chao Yan,Dan Theodorescu,Chao Yan,Dan Theodorescu

    More than a hundred proteins comprise the RAS superfamily of small GTPases. This family can be divided into RAS, RHO, RAB, RAN, ARF, and RAD subfamilies, with each shown to play distinct roles in human cells in both health and disease. The RAS subfamily has a well-established role in human cancer with the three genes, HRAS, KRAS, and NRAS being the commonly mutated in tumors. These RAS mutations, most often functionally activating, are especially common in pancreatic, lung, and colorectal cancers. Efforts to inhibit RAS and related GTPases have produced inhibitors targeting the downstream effectors of RAS signaling, including inhibitors of the RAF-mitogen-activated protein kinase/extracellular signal-related kinase (ERK)-ERK kinase pathway and the phosphoinositide-3-kinase-AKT-mTOR kinase pathway. A third effector arm of RAS signaling, mediated by RAL (RAS like) has emerged in recent years as a critical driver of RAS oncogenic signaling and has not been targeted until recently. RAL belongs to the RAS branch of the RAS superfamily and shares a high structural similarity with RAS. In human cells, there are two genes, RALA and RALB, both of which have been shown to play roles in the proliferation, survival, and metastasis of a variety of human cancers, including lung, colon, pancreatic, prostate, skin, and bladder cancers. In this review, we summarize the latest knowledge of RAL in the context of human cancer and the recent advancements in the development of cancer therapeutics targeting RAL small GTPases.

    更新日期:2017-12-02
  • International Union of Basic and Clinical Pharmacology. CII: Pharmacological Modulation of H2S Levels: H2S Donors and H2S Biosynthesis Inhibitors
    Pharmacol. Rev. (IF 17.893) Pub Date : 2017-10-01
    Csaba Szabo,Andreas Papapetropoulos,Eliot H. Ohlstein,ASSOCIATE EDITOR,Csaba Szabo,Andreas Papapetropoulos,Csaba Szabo,Andreas Papapetropoulos
    更新日期:2017-10-05
  • Chemical Tools for Studying Lipid-Binding Class A G Protein–Coupled Receptors
    Pharmacol. Rev. (IF 17.893) Pub Date : 2017-07-01
    Anna Cooper,Sameek Singh,Sarah Hook,Joel D. A. Tyndall,Andrea J. Vernall,Stephen P. H. Alexander,ASSOCIATE EDITOR,Anna Cooper,Sameek Singh,Sarah Hook,Joel D. A. Tyndall,Andrea J. Vernall,Anna Cooper,Sameek Singh,Sarah Hook,Joel D. A. Tyndall,Andrea J. Vernall

    Cannabinoid, free fatty acid, lysophosphatidic acid, sphingosine 1-phosphate, prostanoid, leukotriene, bile acid, and platelet-activating factor receptor families are class A G protein–coupled receptors with endogenous lipid ligands. Pharmacological tools are crucial for studying these receptors and addressing the many unanswered questions surrounding expression of these receptors in normal and diseased tissues. An inherent challenge for developing tools for these lipid receptors is balancing the often lipophilic requirements of the receptor-binding pharmacophore with favorable physicochemical properties to optimize highly specific binding. In this study, we review the radioligands, fluorescent ligands, covalent ligands, and antibodies that have been used to study these lipid-binding receptors. For each tool type, the characteristics and design rationale along with in vitro and in vivo applications are detailed.

    更新日期:2017-08-24
  • Botulinum Neurotoxins: Biology, Pharmacology, and Toxicology
    Pharmacol. Rev. (IF 17.893) Pub Date : 2017-04-01
    Marco Pirazzini,Ornella Rossetto,Roberto Eleopra,Cesare Montecucco,Jeffrey M. Witkin,ASSOCIATE EDITOR,Marco Pirazzini,Ornella Rossetto,Roberto Eleopra,Cesare Montecucco,Marco Pirazzini,Ornella Rossetto,Roberto Eleopra,Cesare Montecucco
    更新日期:2017-08-24
  • Systems Chronotherapeutics
    Pharmacol. Rev. (IF 17.893) Pub Date : 2017-04-01
    Annabelle Ballesta,Pasquale F. Innominato,Robert Dallmann,David A. Rand,Francis A. Lévi,Stephanie W. Watts,ASSOCIATE EDITOR,Annabelle Ballesta,Pasquale F. Innominato,Robert Dallmann,David A. Rand,Francis A. Lévi,Annabelle Ballesta,Pasquale F. Innominato,Robert Dallmann,David A. Rand,Francis A. Lévi
    更新日期:2017-08-24
  • International Union of Basic and Clinical Pharmacology. CI. Structures and Small Molecule Modulators of Mammalian Adenylyl Cyclases
    Pharmacol. Rev. (IF 17.893) Pub Date : 2017-04-01
    Carmen W. Dessauer,Val J. Watts,Rennolds S. Ostrom,Marco Conti,Stefan Dove,Roland Seifert,Eliot H. Ohlstein,ASSOCIATE EDITOR,Carmen W. Dessauer,Val J. Watts,Rennolds S. Ostrom,Marco Conti,Stefan Dove,Roland Seifert,Carmen W. Dessauer,Val J. Watts,Rennolds S. Ostrom,Marco Conti,Stefan Dove,Roland Seifert
    更新日期:2017-08-24
Some contents have been Reproduced with permission of the American Chemical Society.
Some contents have been Reproduced by permission of The Royal Society of Chemistry.
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