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Pharmacological Reviews

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https://www.readbyqxmd.com/read/29669750/current-challenges-and-opportunities-in-treating-glioblastoma
#1
Andrea Shergalis, Armand Bankhead, Urarika Luesakul, Nongnuj Muangsin, Nouri Neamati
Glioblastoma multiforme (GBM), the most common and aggressive primary brain tumor, has a high mortality rate despite extensive efforts to develop new treatments. GBM exhibits both intra- and intertumor heterogeneity, lending to resistance and eventual tumor recurrence. Large-scale genomic and proteomic analysis of GBM tumors has uncovered potential drug targets. Effective and "druggable" targets must be validated to embark on a robust medicinal chemistry campaign culminating in the discovery of clinical candidates...
July 2018: Pharmacological Reviews
https://www.readbyqxmd.com/read/29514871/interindividual-differences-in-caffeine-metabolism-and-factors-driving-caffeine-consumption
#2
REVIEW
Astrid Nehlig
Most individuals adjust their caffeine intake according to the objective and subjective effects induced by the methylxanthine. However, to reach the desired effects, the quantity of caffeine consumed varies largely among individuals. It has been known for decades that the metabolism, clearance, and pharmacokinetics of caffeine is affected by many factors such as age, sex and hormones, liver disease, obesity, smoking, and diet. Caffeine also interacts with many medications. All these factors will be reviewed in the present document and discussed in light of the most recent data concerning the genetic variability affecting caffeine levels and effects at the pharmacokinetic and pharmacodynamic levels that both critically drive the level of caffeine consumption...
April 2018: Pharmacological Reviews
https://www.readbyqxmd.com/read/29507103/transcription-factor-nrf2-as-a-therapeutic-target-for-chronic-diseases-a-systems-medicine-approach
#3
REVIEW
Antonio Cuadrado, Gina Manda, Ahmed Hassan, María José Alcaraz, Coral Barbas, Andreas Daiber, Pietro Ghezzi, Rafael León, Manuela G López, Baldo Oliva, Marta Pajares, Ana I Rojo, Natalia Robledinos-Antón, Angela M Valverde, Emre Guney, Harald H H W Schmidt
Systems medicine has a mechanism-based rather than a symptom- or organ-based approach to disease and identifies therapeutic targets in a nonhypothesis-driven manner. In this work, we apply this to transcription factor nuclear factor (erythroid-derived 2)-like 2 (NRF2) by cross-validating its position in a protein-protein interaction network (the NRF2 interactome) functionally linked to cytoprotection in low-grade stress, chronic inflammation, metabolic alterations, and reactive oxygen species formation. Multiscale network analysis of these molecular profiles suggests alterations of NRF2 expression and activity as a common mechanism in a subnetwork of diseases (the NRF2 diseasome)...
April 2018: Pharmacological Reviews
https://www.readbyqxmd.com/read/29500312/etiology-and-pharmacology-of-neuropathic-pain
#4
REVIEW
Sascha R A Alles, Peter A Smith
Injury to or disease of the nervous system can invoke chronic and sometimes intractable neuropathic pain. Many parallel, interdependent, and time-dependent processes, including neuroimmune interactions at the peripheral, supraspinal, and spinal levels, contribute to the etiology of this "disease of pain." Recent work emphasizes the roles of colony-stimulating factor 1, ATP, and brain-derived neurotrophic factor. Excitatory processes are enhanced, and inhibitory processes are attenuated in the spinal dorsal horn and throughout the somatosensory system...
April 2018: Pharmacological Reviews
https://www.readbyqxmd.com/read/29496890/neuroimmune-axes-of-the-blood-brain-barriers-and-blood-brain-interfaces-bases-for-physiological-regulation-disease-states-and-pharmacological-interventions
#5
REVIEW
Michelle A Erickson, William A Banks
Central nervous system (CNS) barriers predominantly mediate the immune-privileged status of the brain, and are also important regulators of neuroimmune communication. It is increasingly appreciated that communication between the brain and immune system contributes to physiologic processes, adaptive responses, and disease states. In this review, we discuss the highly specialized features of brain barriers that regulate neuroimmune communication in health and disease. In section I , we discuss the concept of immune privilege, provide working definitions of brain barriers, and outline the historical work that contributed to the understanding of CNS barrier functions...
April 2018: Pharmacological Reviews
https://www.readbyqxmd.com/read/29487084/biomarkers-for-in-vivo-assessment-of-transporter-function
#6
REVIEW
Fabian Müller, Ashish Sharma, Jörg König, Martin F Fromm
Drug-drug interactions are a major concern not only during clinical practice, but also in drug development. Due to limitations of in vitro-in vivo predictions of transporter-mediated drug-drug interactions, multiple clinical Phase I drug-drug interaction studies may become necessary for a new molecular entity to assess potential drug interaction liabilities. This is a resource-intensive process and exposes study participants, who frequently are healthy volunteers without benefit from study treatment, to the potential risks of a new drug in development...
April 2018: Pharmacological Reviews
https://www.readbyqxmd.com/read/29487083/drugs-for-insomnia-beyond-benzodiazepines-pharmacology-clinical-applications-and-discovery
#7
REVIEW
Tobias Atkin, Stefano Comai, Gabriella Gobbi
Although the GABAergic benzodiazepines (BZDs) and Z-drugs (zolpidem, zopiclone, and zaleplon) are FDA-approved for insomnia disorders with a strong evidence base, they have many side effects, including cognitive impairment, tolerance, rebound insomnia upon discontinuation, car accidents/falls, abuse, and dependence liability. Consequently, the clinical use of off-label drugs and novel drugs that do not target the GABAergic system is increasing. The purpose of this review is to analyze the neurobiological and clinical evidence of pharmacological treatments of insomnia, excluding the BZDs and Z-drugs...
April 2018: Pharmacological Reviews
https://www.readbyqxmd.com/read/29279348/international-union-of-basic-and-clinical-pharmacology-ciii-chemerin-receptors-cmklr1-chemerin-1-and-gpr1-chemerin-2-nomenclature-pharmacology-and-function
#8
Amanda J Kennedy, Anthony P Davenport
Chemerin, a chemoattractant protein and adipokine, has been identified as the endogenous ligand for a G protein-coupled receptor encoded by the gene CMKLR1 (also known as ChemR23), and as a consequence the receptor protein was renamed the chemerin receptor in 2013. Since then, chemerin has been identified as the endogenous ligand for a second G protein-coupled receptor, encoded by the gene GPR1 Therefore, the International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification recommends that the official name of the receptor protein for chemokine-like receptor 1 (CMKLR1) is chemerin receptor 1, and G protein-coupled receptor 1 is chemerin receptor 2 to follow the convention of naming the receptor protein after the endogenous ligand...
January 2018: Pharmacological Reviews
https://www.readbyqxmd.com/read/29263209/ion-channels-in-genetic-epilepsy-from-genes-and-mechanisms-to-disease-targeted-therapies
#9
REVIEW
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...
January 2018: Pharmacological Reviews
https://www.readbyqxmd.com/read/29247129/wnt-signaling-in-cardiac-and-vascular-disease
#10
REVIEW
Sébastien Foulquier, Evangelos P Daskalopoulos, Gentian Lluri, Kevin C M Hermans, Arjun Deb, W Matthijs Blankesteijn
WNT signaling is an elaborate and complex collection of signal transduction pathways mediated by multiple signaling molecules. WNT signaling is critically important for developmental processes, including cell proliferation, differentiation and tissue patterning. Little WNT signaling activity is present in the cardiovascular system of healthy adults, but reactivation of the pathway is observed in many pathologies of heart and blood vessels. The high prevalence of these pathologies and their significant contribution to human disease burden has raised interest in WNT signaling as a potential target for therapeutic intervention...
January 2018: Pharmacological Reviews
https://www.readbyqxmd.com/read/29233848/g-protein-coupled-receptors-targeting-insulin-resistance-obesity-and-type-2-diabetes-mellitus
#11
REVIEW
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...
January 2018: Pharmacological Reviews
https://www.readbyqxmd.com/read/29217656/anti-inflammatory-effects-of-omega-3-fatty-acids-in-the-brain-physiological-mechanisms-and-relevance-to-pharmacology
#12
REVIEW
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...
January 2018: Pharmacological Reviews
https://www.readbyqxmd.com/read/29196555/ral-gtpases-biology-and-potential-as-therapeutic-targets-in-cancer
#13
REVIEW
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...
January 2018: Pharmacological Reviews
https://www.readbyqxmd.com/read/28978633/international-union-of-basic-and-clinical-pharmacology-cii-pharmacological-modulation-of-h-2-s-levels-h-2-s-donors-and-h-2-s-biosynthesis-inhibitors
#14
REVIEW
Csaba Szabo, Andreas Papapetropoulos
Over the last decade, hydrogen sulfide (H2 S) has emerged as an important endogenous gasotransmitter in mammalian cells and tissues. Similar to the previously characterized gasotransmitters nitric oxide and carbon monoxide, H2 S is produced by various enzymatic reactions and regulates a host of physiologic and pathophysiological processes in various cells and tissues. H2 S levels are decreased in a number of conditions (e.g., diabetes mellitus, ischemia, and aging) and are increased in other states (e.g., inflammation, critical illness, and cancer)...
October 2017: Pharmacological Reviews
https://www.readbyqxmd.com/read/28931623/small-molecule-screens-a-gateway-to-cancer-therapeutic-agents-with-case-studies-of-food-and-drug-administration-approved-drugs
#15
REVIEW
Nathan P Coussens, John C Braisted, Tyler Peryea, G Sitta Sittampalam, Anton Simeonov, Matthew D Hall
High-throughput screening (HTS) of small-molecule libraries accelerates the discovery of chemical leads to serve as starting points for probe or therapeutic development. With this approach, thousands of unique small molecules, representing a diverse chemical space, can be rapidly evaluated by biologically and physiologically relevant assays. The origins of numerous United States Food and Drug Administration-approved cancer drugs are linked to HTS, which emphasizes the value in this methodology. The National Institutes of Health Molecular Libraries Program made HTS accessible to the public sector, enabling the development of chemical probes and drug-repurposing initiatives...
October 2017: Pharmacological Reviews
https://www.readbyqxmd.com/read/28931622/connexins-in-cardiovascular-and-neurovascular-health-and-disease-pharmacological-implications
#16
REVIEW
Luc Leybaert, Paul D Lampe, Stefan Dhein, Brenda R Kwak, Peter Ferdinandy, Eric C Beyer, Dale W Laird, Christian C Naus, Colin R Green, Rainer Schulz
Connexins are ubiquitous channel forming proteins that assemble as plasma membrane hemichannels and as intercellular gap junction channels that directly connect cells. In the heart, gap junction channels electrically connect myocytes and specialized conductive tissues to coordinate the atrial and ventricular contraction/relaxation cycles and pump function. In blood vessels, these channels facilitate long-distance endothelial cell communication, synchronize smooth muscle cell contraction, and support endothelial-smooth muscle cell communication...
October 2017: Pharmacological Reviews
https://www.readbyqxmd.com/read/28878030/the-hyperpolarization-activated-cyclic-nucleotide-gated-channels-from-biophysics-to-pharmacology-of-a-unique-family-of-ion-channels
#17
REVIEW
Laura Sartiani, Guido Mannaioni, Alessio Masi, Maria Novella Romanelli, Elisabetta Cerbai
Hyperpolarization-activated, cyclic nucleotide-gated (HCN) channels are important members of the voltage-gated pore loop channels family. They show unique features: they open at hyperpolarizing potential, carry a mixed Na/K current, and are regulated by cyclic nucleotides. Four different isoforms have been cloned (HCN1-4) that can assemble to form homo- or heterotetramers, characterized by different biophysical properties. These proteins are widely distributed throughout the body and involved in different physiologic processes, the most important being the generation of spontaneous electrical activity in the heart and the regulation of synaptic transmission in the brain...
October 2017: Pharmacological Reviews
https://www.readbyqxmd.com/read/28655732/chemical-tools-for-studying-lipid-binding-class-a-g-protein-coupled-receptors
#18
REVIEW
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...
July 2017: Pharmacological Reviews
https://www.readbyqxmd.com/read/28634286/conjugate-vaccine-immunotherapy-for-substance-use-disorder
#19
REVIEW
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, wherein a hapten structurally similar to the target drug is conjugated to an immunogenic carrier protein...
July 2017: Pharmacological Reviews
https://www.readbyqxmd.com/read/28626043/the-diverse-roles-of-arrestin-scaffolds-in-g-protein-coupled-receptor-signaling
#20
REVIEW
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 bind activated GPCRs on the plasma membrane, which enables them to control GPCR desensitization, internalization, and intracellular trafficking...
July 2017: Pharmacological Reviews
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