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International Union of Basic and Clinical Pharmacology. CXI. Pharmacology, Signaling, and Physiology of Metabotropic Glutamate Receptors Pharmacol. Rev. (IF 17.395) Pub Date : 2021-01-01 Karen J. Gregory; Cyril Goudet; Eliot H. Ohlstein
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International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function Pharmacol. Rev. (IF 17.395) Pub Date : 2021-01-01 Nicholas M. Barnes; Gerard P. Ahern; Carine Becamel; Joël Bockaert; Michael Camilleri; Severine Chaumont-Dubel; Sylvie Claeysen; Kathryn A. Cunningham; Kevin C. Fone; Michael Gershon; Giuseppe Di Giovanni; Nathalie M. Goodfellow; Adam L. Halberstadt; Rachel M. Hartley; Ghérici Hassaine; Katharine Herrick-Davis; Ruud Hovius; Enza Lacivita; Evelyn K. Lambe; Marcello Leopoldo; Finn Olav Levy; Sarah C
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Subcellular Organization of the cAMP Signaling Pathway Pharmacol. Rev. (IF 17.395) Pub Date : 2021-01-01 Manuela Zaccolo; Anna Zerio; Miguel J. Lobo; Christopher Garland
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Psychedelics in Psychiatry: Neuroplastic, Immunomodulatory, and Neurotransmitter Mechanisms Pharmacol. Rev. (IF 17.395) Pub Date : 2021-01-01 Antonio Inserra; Danilo De Gregorio; Gabriella Gobbi; Michael Nader
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Drug Addiction: Hyperkatifeia/Negative Reinforcement as a Framework for Medications Development Pharmacol. Rev. (IF 17.395) Pub Date : 2021-01-01 George F. Koob; Robert Dantzer
Compulsive drug seeking that is associated with addiction is hypothesized to follow a heuristic framework that involves three stages (binge/intoxication, withdrawal/negative affect, and preoccupation/anticipation) and three domains of dysfunction (incentive salience/pathologic habits, negative emotional states, and executive function, respectively) via changes in the basal ganglia, extended amygdala/habenula
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Cognitive Impairment in Older Adults and Therapeutic Strategies Pharmacol. Rev. (IF 17.395) Pub Date : 2021-01-01 Thomas J. Montine; Syed A. Bukhari; Lon R. White; VIVIAN HOOK
Cognitive impairment and its severe form dementia are increasingly prevalent in older adults and loom as a public health disaster unless effective interventions are developed. Cognitive impairment is a convergent trait caused by damage from an idiosyncratic mix of four prevalent diseases (Alzheimer disease; vascular brain injury; Lewy body diseases, such as Parkinson disease and dementia with Lewy
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Post-Translational Modifications of G Protein–Coupled Receptors Control Cellular Signaling Dynamics in Space and Time Pharmacol. Rev. (IF 17.395) Pub Date : 2021-01-01 Anand Patwardhan; Norton Cheng; JoAnn Trejo; Gunnar Schulte
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Mutations in G Protein–Coupled Receptors: Mechanisms, Pathophysiology and Potential Therapeutic Approaches Pharmacol. Rev. (IF 17.395) Pub Date : 2021-01-01 Torsten Schöneberg; Ines Liebscher; Paul Insel
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Pharmacological Manipulation of Translation as a Therapeutic Target for Chronic Pain Pharmacol. Rev. (IF 17.395) Pub Date : 2021-01-01 Muhammad Saad Yousuf; Stephanie I. Shiers; James J. Sahn; Theodore J. Price; Robert Dantzer
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E1 Enzymes as Therapeutic Targets in Cancer Pharmacol. Rev. (IF 17.395) Pub Date : 2021-01-01 Samir H. Barghout; Aaron D. Schimmer; Eric Barker
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International Union of Basic and Clinical Pharmacology. CIX. Differences and Similarities between Human and Rodent Prostaglandin E2 Receptors (EP1-4) and Prostacyclin Receptor (IP): Specific Roles in Pathophysiologic Conditions. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-10-01 Xavier Norel,Yukihiko Sugimoto,Gulsev Ozen,Heba Abdelazeem,Yasmine Amgoud,Amel Bouhadoun,Wesam Bassiouni,Marie Goepp,Salma Mani,Hasanga D Manikpurage,Amira Senbel,Dan Longrois,Akos Heinemann,Chengcan Yao,Lucie H Clapp
Prostaglandins are derived from arachidonic acid metabolism through cyclooxygenase activities. Among prostaglandins (PGs), prostacyclin (PGI2) and PGE2 are strongly involved in the regulation of homeostasis and main physiologic functions. In addition, the synthesis of these two prostaglandins is significantly increased during inflammation. PGI2 and PGE2 exert their biologic actions by binding to their
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Development of Novel, Value-Based, Digital Endpoints for Clinical Trials: A Structured Approach Toward Fit-for-Purpose Validation. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-10-01 M D Kruizinga,F E Stuurman,V Exadaktylos,R J Doll,D T Stephenson,G J Groeneveld,G J A Driessen,A F Cohen
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RNA Drugs and RNA Targets for Small Molecules: Principles, Progress, and Challenges. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-10-01 Ai-Ming Yu,Young Hee Choi,Mei-Juan Tu
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Is Oxytocin "Nature's Medicine"? Pharmacol. Rev. (IF 17.395) Pub Date : 2020-10-01 C Sue Carter,William M Kenkel,Evan L MacLean,Steven R Wilson,Allison M Perkeybile,Jason R Yee,Craig F Ferris,Hossein P Nazarloo,Stephen W Porges,John M Davis,Jessica J Connelly,Marcy A Kingsbury
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On the Clinical Pharmacology of Reactive Oxygen Species. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-10-01 Ana I Casas,Cristian Nogales,Hermann A M Mucke,Alexandra Petraina,Antonio Cuadrado,Ana I Rojo,Pietro Ghezzi,Vincent Jaquet,Fiona Augsburger,Francois Dufrasne,Jalal Soubhye,Soni Deshwal,Moises Di Sante,Nina Kaludercic,Fabio Di Lisa,Harald H H W Schmidt
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Sex Differences in the Epilepsies and Associated Comorbidities: Implications for Use and Development of Pharmacotherapies. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-10-01 Catherine A Christian,Doodipala Samba Reddy,Jamie Maguire,Patrick A Forcelli
The epilepsies are common neurologic disorders characterized by spontaneous recurrent seizures. Boys, girls, men, and women of all ages are affected by epilepsy and, in many cases, by associated comorbidities as well. The primary courses of treatment are pharmacological, dietary, and/or surgical, depending on several factors, including the areas of the brain affected and the severity of the epilepsy
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The Noncanonical Pathway for In Vivo Nitric Oxide Generation: The Nitrate-Nitrite-Nitric Oxide Pathway. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-07-01 V Kapil,R S Khambata,D A Jones,K Rathod,C Primus,G Massimo,J M Fukuto,A Ahluwalia
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Using Pharmacology to Squeeze the Life Out of Childhood Leukemia, and Potential Strategies to Achieve Breakthroughs in Medulloblastoma Treatment. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-07-01 Juwina Wijaya,Tomoka Gose,John D Schuetz
Eliminating cancer was once thought of as a war. This analogy is still apt today; however, we now realize that cancer is a much more formidable enemy than scientists originally perceived, and in some cases, it harbors a profound ability to thwart our best efforts to defeat it. However, before we were aware of the complexity of cancer, chemotherapy against childhood acute lymphoblastic leukemia (ALL)
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Strategies to Modulate MicroRNA Functions for the Treatment of Cancer or Organ Injury. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-07-01 Tae Jin Lee,Xiaoyi Yuan,Keith Kerr,Ji Young Yoo,Dong H Kim,Balveen Kaur,Holger K Eltzschig
Cancer and organ injury—such as that occurring in the perioperative period, including acute lung injury, myocardial infarction, and acute gut injury—are among the leading causes of death in the United States and impose a significant impact on quality of life. MicroRNAs (miRNAs) have been studied extensively during the last two decades for their role as regulators of gene expression, their translational
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Drug Resistance in Epilepsy: Clinical Impact, Potential Mechanisms, and New Innovative Treatment Options. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-07-01 Wolfgang Löscher,Heidrun Potschka,Sanjay M Sisodiya,Annamaria Vezzani
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International Union of Basic and Clinical Pharmacology. CVIII. Calcium-Sensing Receptor Nomenclature, Pharmacology, and Function. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-07-01 Katie Leach,Fadil M Hannan,Tracy M Josephs,Andrew N Keller,Thor C Møller,Donald T Ward,Enikö Kallay,Rebecca S Mason,Rajesh V Thakker,Daniela Riccardi,Arthur D Conigrave,Hans Bräuner-Osborne
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More than Smoke and Patches: The Quest for Pharmacotherapies to Treat Tobacco Use Disorder. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-04-01 M J Moerke,L R McMahon,J L Wilkerson
Tobacco use is a persistent public health issue. It kills up to half its users and is the cause of nearly 90% of all lung cancers. The main psychoactive component of tobacco is nicotine, primarily responsible for its abuse-related effects. Accordingly, most pharmacotherapies for smoking cessation target nicotinic acetylcholine receptors (nAChRs), nicotine's major site of action in the brain. The goal
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Targeting Janus Kinases and Signal Transducer and Activator of Transcription 3 to Treat Inflammation, Fibrosis, and Cancer: Rationale, Progress, and Caution. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-04-01 Uddalak Bharadwaj,Moses M Kasembeli,Prema Robinson,David J Tweardy
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Monocarboxylate Transporters (SLC16): Function, Regulation, and Role in Health and Disease. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-04-01 Melanie A Felmlee,Robert S Jones,Vivian Rodriguez-Cruz,Kristin E Follman,Marilyn E Morris
The solute carrier family 16 (SLC16) is comprised of 14 members of the monocarboxylate transporter (MCT) family that play an essential role in the transport of important cell nutrients and for cellular metabolism and pH regulation. MCTs 1-4 have been extensively studied and are involved in the proton-dependent transport of L-lactate, pyruvate, short-chain fatty acids, and monocarboxylate drugs in a
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Encoding, Consolidation, and Renormalization in Depression: Synaptic Homeostasis, Plasticity, and Sleep Integrate Rapid Antidepressant Effects. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-04-01 Tomi Rantamäki,Samuel Kohtala
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Transitioning from Basic toward Systems Pharmacodynamic Models: Lessons from Corticosteroids. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-04-01 Vivaswath S Ayyar,William J Jusko
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Protein Engineering in the Ubiquitin System: Tools for Discovery and Beyond. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-04-01 Bo Zhao,Yien Che Tsai,Bo Jin,Bufan Wang,Yiyang Wang,Han Zhou,Tomaya Carpenter,Allan M Weissman,Jun Yin
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Solute Carrier Transporters as Potential Targets for the Treatment of Metabolic Disease. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-01-01 Tina Schumann,Jörg König,Christine Henke,Diana M Willmes,Stefan R Bornstein,Jens Jordan,Martin F Fromm,Andreas L Birkenfeld
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Patient and Disease-Specific Induced Pluripotent Stem Cells for Discovery of Personalized Cardiovascular Drugs and Therapeutics. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-01-01 David T Paik,Mark Chandy,Joseph C Wu
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Organic Cation Transporters in Health and Disease. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-01-01 Hermann Koepsell
The organic cation transporters (OCTs) OCT1, OCT2, OCT3, novel OCT (OCTN)1, OCTN2, multidrug and toxin exclusion (MATE)1, and MATE kidney-specific 2 are polyspecific transporters exhibiting broadly overlapping substrate selectivities. They transport organic cations, zwitterions, and some uncharged compounds and operate as facilitated diffusion systems and/or antiporters. OCTs are critically involved
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Pharmacology and Therapeutics of Bronchodilators Revisited. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-01-01 M G Matera,C P Page,L Calzetta,P Rogliani,M Cazzola
Bronchodilators remain the cornerstone of the treatment of airway disorders such as asthma and chronic obstructive pulmonary disease (COPD). There is therefore considerable interest in understanding how to optimize the use of our existing classes of bronchodilator and in identifying novel classes of bronchodilator drugs. However, new classes of bronchodilator have proved challenging to develop because
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High-dimensionality Data Analysis of Pharmacological Systems Associated with Complex Diseases. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-01-01 Jhana O Hendrickx,Jaana van Gastel,Hanne Leysen,Bronwen Martin,Stuart Maudsley
It is widely accepted that molecular reductionist views of highly complex human physiologic activity, e.g., the aging process, as well as therapeutic drug efficacy are largely oversimplifications. Currently some of the most effective appreciation of biologic disease and drug response complexity is achieved using high-dimensionality (H-D) data streams from transcriptomic, proteomic, metabolomics, or
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Brothers in Arms: ABCA1- and ABCG1-Mediated Cholesterol Efflux as Promising Targets in Cardiovascular Disease Treatment. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-01-01 Sanne J C M Frambach,Ria de Haas,Jan A M Smeitink,Gerard A Rongen,Frans G M Russel,Tom J J Schirris
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The Psychopharmacology of Obsessive-Compulsive Disorder: A Preclinical Roadmap. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-01-01 Henry Szechtman,Brian H Harvey,Erik Z Woody,Kurt Leroy Hoffman
This review evaluates current knowledge about obsessive-compulsive disorder (OCD), with the goal of providing a roadmap for future directions in research on the psychopharmacology of the disorder. It first addresses issues in the description and diagnosis of OCD, including the structure, measurement, and appropriate description of the disorder and issues of differential diagnosis. Current pharmacotherapies
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G Protein-Coupled Receptors in Asthma Therapy: Pharmacology and Drug Action. Pharmacol. Rev. (IF 17.395) Pub Date : 2020-01-01 Stacy Gelhaus Wendell,Hao Fan,Cheng Zhang
Asthma is a heterogeneous inflammatory disease of the airways that is associated with airway hyperresponsiveness and airflow limitation. Although asthma was once simply categorized as atopic or nonatopic, emerging analyses over the last few decades have revealed a variety of asthma endotypes that are attributed to numerous pathophysiological mechanisms. The classification of asthma by endotype is primarily
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Cognitive Effects of MDMA in Laboratory Animals: A Systematic Review Focusing on Dose. Pharmacol. Rev. (IF 17.395) Pub Date : 2019-07-01 Madeline M Pantoni,Stephan G Anagnostaras
±3,4-Methylenedioxymethamphetamine (MDMA) is a synthetic, psychoactive drug that is primarily used recreationally but also may have some therapeutic value. At low doses, MDMA produces feelings of relaxation, empathy, emotional closeness, and euphoria. Higher doses can produce unpleasant psychostimulant- and hallucinogen-like adverse effects and therefore are usually not taken intentionally. There is
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5-HT3 Receptor Antagonists in Neurologic and Neuropsychiatric Disorders: The Iceberg Still Lies beneath the Surface. Pharmacol. Rev. (IF 17.395) Pub Date : 2019-07-01 Gohar Fakhfouri,Reza Rahimian,Jonas Dyhrfjeld-Johnsen,Mohammad Reza Zirak,Jean-Martin Beaulieu
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Correction to "Ketamine and Ketamine Metabolite Pharmacology: Insights into Therapeutic Mechanisms". Pharmacol. Rev. (IF 17.395) Pub Date : 2018-10-05
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Conjugate Vaccine Immunotherapy for Substance Use Disorder. Pharmacol. Rev. (IF 17.395) Pub Date : 2017-06-22 Paul T Bremer,Kim D Janda
Substance use disorder, especially in relation to opioids such as heroin and fentanyl, is a significant public health issue and has intensified in recent years. As a result, substantial interest exists in developing therapeutics to counteract the effects of abused drugs. A promising universal strategy for antagonizing the pharmacology of virtually any drug involves the development of a conjugate vaccine
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The Diverse Roles of Arrestin Scaffolds in G Protein-Coupled Receptor Signaling. Pharmacol. Rev. (IF 17.395) Pub Date : 2017-06-20 Yuri K Peterson,Louis M Luttrell
The visual/β-arrestins, a small family of proteins originally described for their role in the desensitization and intracellular trafficking of G protein-coupled receptors (GPCRs), have emerged as key regulators of multiple signaling pathways. Evolutionarily related to a larger group of regulatory scaffolds that share a common arrestin fold, the visual/β-arrestins acquired the capacity to detect and
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Emotional Modulation of Learning and Memory: Pharmacological Implications. Pharmacol. Rev. (IF 17.395) Pub Date : 2017-04-20 Ryan T LaLumiere,James L McGaugh,Christa K McIntyre
Memory consolidation involves the process by which newly acquired information becomes stored in a long-lasting fashion. Evidence acquired over the past several decades, especially from studies using post-training drug administration, indicates that emotional arousal during the consolidation period influences and enhances the strength of the memory and that multiple different chemical signaling systems
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Contrasting Regulation of Catecholamine Neurotransmission in the Behaving Brain: Pharmacological Insights from an Electrochemical Perspective. Pharmacol. Rev. (IF 17.395) Pub Date : 2017-03-08 Megan E Fox,R Mark Wightman
Catecholamine neurotransmission plays a key role in regulating a variety of behavioral and physiologic processes, and its dysregulation is implicated in both neurodegenerative and neuropsychiatric disorders. Over the last four decades, in vivo electrochemistry has enabled the discovery of contrasting catecholamine regulation in the brain. These rapid and spatially resolved measurements have been conducted
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International Union of Basic and Clinical Pharmacology. C. Nomenclature and Properties of Calcium-Activated and Sodium-Activated Potassium Channels. Pharmacol. Rev. (IF 17.395) Pub Date : 2017-03-08 Leonard K Kaczmarek,Richard W Aldrich,K George Chandy,Stephan Grissmer,Aguan D Wei,Heike Wulff
A subset of potassium channels is regulated primarily by changes in the cytoplasmic concentration of ions, including calcium, sodium, chloride, and protons. The eight members of this subfamily were originally all designated as calcium-activated channels. More recent studies have clarified the gating mechanisms for these channels and have documented that not all members are sensitive to calcium. This
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Synaptic Vesicle-Recycling Machinery Components as Potential Therapeutic Targets. Pharmacol. Rev. (IF 17.395) Pub Date : 2017-03-08 Ying C Li,Ege T Kavalali
Presynaptic nerve terminals are highly specialized vesicle-trafficking machines. Neurotransmitter release from these terminals is sustained by constant local recycling of synaptic vesicles independent from the neuronal cell body. This independence places significant constraints on maintenance of synaptic protein complexes and scaffolds. Key events during the synaptic vesicle cycle-such as exocytosis
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Vitamin D and Depression: Cellular and Regulatory Mechanisms. Pharmacol. Rev. (IF 17.395) Pub Date : 2017-02-17 Michael J Berridge
Depression is caused by a change in neural activity resulting from an increase in glutamate that drives excitatory neurons and may be responsible for the decline in the activity and number of the GABAergic inhibitory neurons. This imbalance between the excitatory and inhibitory neurons may contribute to the onset of depression. At the cellular level there is an increase in the concentration of intracellular
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Pharmacology of Modulators of Alternative Splicing. Pharmacol. Rev. (IF 17.395) Pub Date : 2017-01-01 David O Bates,Jonathan C Morris,Sebastian Oltean,Lucy F Donaldson
More than 95% of genes in the human genome are alternatively spliced to form multiple transcripts, often encoding proteins with differing or opposing function. The control of alternative splicing is now being elucidated, and with this comes the opportunity to develop modulators of alternative splicing that can control cellular function. A number of approaches have been taken to develop compounds that
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The Pharmacology of Autonomic Failure: From Hypotension to Hypertension. Pharmacol. Rev. (IF 17.395) Pub Date : 2016-12-25 Italo Biaggioni
Primary neurodegenerative autonomic disorders are characterized clinically by loss of autonomic regulation of blood pressure. The clinical picture is dominated by orthostatic hypotension, but supine hypertension is also a significant problem. Autonomic failure can result from impairment of central autonomic pathways (multiple system atrophy) or neurodegeneration of peripheral postganglionic autonomic
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The Proprotein Convertases in Hypercholesterolemia and Cardiovascular Diseases: Emphasis on Proprotein Convertase Subtilisin/Kexin 9. Pharmacol. Rev. (IF 17.395) Pub Date : 2016-12-07 Nabil G Seidah,Marianne Abifadel,Stefan Prost,Catherine Boileau,Annik Prat
The secretory proprotein convertase (PC) family comprises nine members, as follows: PC1/3, PC2, furin, PC4, PC5/6, paired basic amino acid cleaving enzyme 4, PC7, subtilisin kexin isozyme 1/site 1 protease (SKI-1/S1P), and PC subtilisin/kexin type 9 (PCSK9). The first seven PCs cleave their substrates at single/paired basic residues and exhibit specific and often essential functions during development
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Botanicals and Their Bioactive Phytochemicals for Women's Health. Pharmacol. Rev. (IF 17.395) Pub Date : 2016-09-30 Birgit M Dietz,Atieh Hajirahimkhan,Tareisha L Dunlap,Judy L Bolton
Botanical dietary supplements are increasingly popular for women's health, particularly for older women. The specific botanicals women take vary as a function of age. Younger women will use botanicals for urinary tract infections, especially Vaccinium macrocarpon (cranberry), where there is evidence for efficacy. Botanical dietary supplements for premenstrual syndrome (PMS) are less commonly used,
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Adolescent Alcohol Exposure Persistently Impacts Adult Neurobiology and Behavior. Pharmacol. Rev. (IF 17.395) Pub Date : 2016-09-30 Fulton T Crews,Ryan P Vetreno,Margaret A Broadwater,Donita L Robinson
Adolescence is a developmental period when physical and cognitive abilities are optimized, when social skills are consolidated, and when sexuality, adolescent behaviors, and frontal cortical functions mature to adult levels. Adolescents also have unique responses to alcohol compared with adults, being less sensitive to ethanol sedative-motor responses that most likely contribute to binge drinking and
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Proteinases, Their Extracellular Targets, and Inflammatory Signaling. Pharmacol. Rev. (IF 17.395) Pub Date : 2016-09-30 Rithwik Ramachandran,Christophe Altier,Katerina Oikonomopoulou,Morley D Hollenberg
Given that over 2% of the human genome codes for proteolytic enzymes and their inhibitors, it is not surprising that proteinases serve many physiologic-pathophysiological roles. In this context, we provide an overview of proteolytic mechanisms regulating inflammation, with a focus on cell signaling stimulated by the generation of inflammatory peptides; activation of the proteinase-activated receptor
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Targeting Immune Checkpoints in Hematologic Malignancies. Pharmacol. Rev. (IF 17.395) Pub Date : 2016-09-25 Gheath Alatrash,Naval Daver,Elizabeth A Mittendorf
The use of antibodies that target immune checkpoint molecules on the surface of T-lymphocytes and/or tumor cells has revolutionized our approach to cancer therapy. Cytotoxic-T-lymphocyte antigen (CTLA-4) and programmed cell death protein 1 (PD-1) are the two most commonly targeted immune checkpoint molecules. Although the role of antibodies that target CTLA-4 and PD-1 has been established in solid
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Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March to Therapeutic Successes. Pharmacol. Rev. (IF 17.395) Pub Date : 2016-09-16 Chris de Graaf,Dan Donnelly,Denise Wootten,Jesper Lau,Patrick M Sexton,Laurence J Miller,Jung-Mo Ahn,Jiayu Liao,Madeleine M Fletcher,Dehua Yang,Alastair J H Brown,Caihong Zhou,Jiejie Deng,Ming-Wei Wang
The glucagon-like peptide (GLP)-1 receptor (GLP-1R) is a class B G protein-coupled receptor (GPCR) that mediates the action of GLP-1, a peptide hormone secreted from three major tissues in humans, enteroendocrine L cells in the distal intestine, α cells in the pancreas, and the central nervous system, which exerts important actions useful in the management of type 2 diabetes mellitus and obesity, including
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Kinase-dependent Regulation of Monoamine Neurotransmitter Transporters. Pharmacol. Rev. (IF 17.395) Pub Date : 2016-09-04 Daniel P Bermingham,Randy D Blakely
Modulation of neurotransmission by the monoamines dopamine (DA), norepinephrine (NE), and serotonin (5-HT) is critical for normal nervous system function. Precise temporal and spatial control of this signaling in mediated in large part by the actions of monoamine transporters (DAT, NET, and SERT, respectively). These transporters act to recapture their respective neurotransmitters after release, and
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Lipid-Based Drug Delivery Systems in Cancer Therapy: What Is Available and What Is Yet to Come. Pharmacol. Rev. (IF 17.395) Pub Date : 2016-07-02 Phatsapong Yingchoncharoen,Danuta S Kalinowski,Des R Richardson
Cancer is a leading cause of death in many countries around the world. However, the efficacy of current standard treatments for a variety of cancers is suboptimal. First, most cancer treatments lack specificity, meaning that these treatments affect both cancer cells and their normal counterparts. Second, many anticancer agents are highly toxic, and thus, limit their use in treatment. Third, a number
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Manipulating Angiogenesis by Targeting Endothelial Metabolism: Hitting the Engine Rather than the Drivers-A New Perspective? Pharmacol. Rev. (IF 17.395) Pub Date : 2016-07-02 Lucas Treps,Lena-Christin Conradi,Ulrike Harjes,Peter Carmeliet
Excessive angiogenesis (i.e., the formation of new blood vessels) contributes to different pathologies, among them cancer and ocular disorders. Conversely, dysfunction of endothelial cells (ECs) contributes to cardiovascular complications, as is the case in diabetes. Inhibition of pathologic angiogenesis in blinding eye disease and cancer by targeting growth factors such as vascular endothelial growth
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Kinases as Novel Therapeutic Targets in Asthma and Chronic Obstructive Pulmonary Disease. Pharmacol. Rev. (IF 17.395) Pub Date : 2016-07-02 Peter J Barnes
Multiple kinases play a critical role in orchestrating the chronic inflammation and structural changes in the respiratory tract of patients with asthma and chronic obstructive pulmonary disease (COPD). Kinases activate signaling pathways that lead to contraction of airway smooth muscle and release of inflammatory mediators (such as cytokines, chemokines, growth factors) as well as cell migration, activation
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The Nucleus Accumbens: Mechanisms of Addiction across Drug Classes Reflect the Importance of Glutamate Homeostasis. Pharmacol. Rev. (IF 17.395) Pub Date : 2016-07-01 M D Scofield,J A Heinsbroek,C D Gipson,Y M Kupchik,S Spencer,A C W Smith,D Roberts-Wolfe,P W Kalivas
The nucleus accumbens is a major input structure of the basal ganglia and integrates information from cortical and limbic structures to mediate goal-directed behaviors. Chronic exposure to several classes of drugs of abuse disrupts plasticity in this region, allowing drug-associated cues to engender a pathologic motivation for drug seeking. A number of alterations in glutamatergic transmission occur
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Molecular Pharmacology of δ-Opioid Receptors. Pharmacol. Rev. (IF 17.395) Pub Date : 2016-06-28 Louis Gendron,Catherine M Cahill,Mark von Zastrow,Peter W Schiller,Graciela Pineyro
Opioids are among the most effective analgesics available and are the first choice in the treatment of acute severe pain. However, partial efficacy, a tendency to produce tolerance, and a host of ill-tolerated side effects make clinically available opioids less effective in the management of chronic pain syndromes. Given that most therapeutic opioids produce their actions via µ-opioid receptors (MOPrs)
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