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Current Medicinal Chemistry

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https://www.readbyqxmd.com/read/28641558/bis-2-aminoimidazolines-and-bisguanidines-synthetic-approaches-antiparasitic-activity-and-dna-binding-properties
#1
Christophe Dardonville, J Jonathan Nué Martínez
BACKGROUND: Parasitic diseases caused by protozoan parasites of the genus Trypanosoma and Plasmodium cause some of the deadliest and disabling human infections in tropical and subtropical areas. Diphenyl-based bis(2-phenylimino)imidazolidines and bisguanidines are extremely potent antiparasitic agents against Trypanosoma brucei (etiological agent of African trypanosomiasis) and Plasmodium falciparum (etiological agent of severe malaria). Many of these compounds are also curative in mouse models of stage 1 African trypanosomiasis representing promising leads for the development of antitrypanosomal drugs...
June 22, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28641557/cyclic-dipeptides-secondary-metabolites-isolated-from-different-microorganisms-with-diverse-biological-activities
#2
Aurelio Ortiz, Estibaliz Sansinenea
Cyclic dipeptides are the simplest peptide derivatives commonly found in nature. These chiral molecules are easily synthesized from readily available α-amino acids using a simple methodology. They are privileged structures with the ability to bind to a wide range of receptors and have a broad variety of biological and pharmacological activities. We will give a brief overview of their status giving and interesting reference list about the last works.
June 22, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28641556/pharmacogenetic-and-pharmacokinetic-dose-individualization-of-the-taxane-chemotherapeutic-drugs-paclitaxel-and-docetaxel
#3
Natália Bordin Andriguetti, Suziane Raymundo, Marina Venzon Antunes, Magda Susana Perasolo, Simone Gasparin Verza, Edna Sayuri Suyenaga, Rafael Linden
The taxane drugs paclitaxel and docetaxel, widely used on cancer chemotherapy, are currently dosed mainly based on body-surface area. This approach is associated with wide interindividual variability in drug exposure, leading to suboptimal dosing for many patients. We reviewed the available evidence supporting dose individualization strategies for paclitaxel and docetaxel, focusing mainly on the application of therapeutic drug monitoring by a priori pharmacogenetic data or a posteriori drug measurements in biological fluids...
June 22, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28641555/supervised-machine-learning-methods-applied-to-predict-ligand-binding-affinity
#4
Gabriela Sehnem Heck, Val Oliveira Pintro, Richard Rene Pereira, Mauricio Boff de Ávila, Nayara Maria Bernhardt Levin, Walter Filgueira de Azevedo
BACKGROUND: Calculation of ligand-binding affinity is an open problem in computational medicinal chemistry. The ability to computationally predict affinities has a beneficial impact in the early stages of drug development, since it allows a mathematical model to assess protein-ligand interactions. Due to the availability of structural and binding information, machine learning methods have been applied to generate scoring functions with good predictive power. OBJECTIVE: Our goal here is to review recent developments in the application of machine learning methods to predict ligand- binding affinity...
June 22, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28625152/lipid-oxidation-products-in-the-pathogenesis-of-inflammation-related-gut-diseases
#5
Barbara Sottero, Daniela Rossin, Giuseppe Poli, Fiorella Biasi
A defective mucosal barrier function is the principal cause of the uncontrolled onset and progression of a number of human inflammatory gut diseases, most of which are characterized by chronic intermittent immune and inflammatory responses leading to structural intestinal damage, which can represent a potential risk for colorectal cancer development. During the active disease phase the production of pro-inflammatory cytokines and chemokines, and the induction of oxidative reactions by activated leukocytes and epithelial cells represent the main event in intestinal inflammation...
June 19, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28625151/na-k-atpase-as-a-target-for-treatment-of-tissue-fibrosis
#6
Sergei N Orlov, Jenifer La, Larisa V Smolyaninova, Nickolai O Dulin
Myofibroblast activation is a critical process in the pathogenesis of tissue fibrosis accounting for 45% of all deaths. No effective therapies are available for the treatment of fibrotic diseases. We focus our mini-review on recent data showing that cardiotonic steroids (CTS) that are known as potent inhibitors of Na+,K+-ATPase affect myofibroblast differentiation in a cell type-specific manner. In cultured human lung fibroblasts (HLF), epithelial cells, and cancer-associated fibroblasts, CTS blocked myofibroblast differentiation triggered by profibrotic cytokine TGF-β...
June 19, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28625150/update-on-the-molecular-mechanisms-underlying-the-effect-of-cholecystokinin-and-cholecystokinin-1-receptor-on-the-formation-of-cholesterol-gallstones
#7
Helen H Wang, Piero Portincasa, David Q-H Wang
Cholecystokinin (CCK) is an important neuro-intestinal peptide hormone produced by the enteroendocrine I-cells in the upper part of small intestine. Protein- and fat-enriched food plays an important role in triggering CCK secretion from the intestine. Carbohydrates stimulate only small amounts of CCK release. The CCK-1 receptor (CCK-1R) is largely localized in the gallbladder, sphincter of Oddi, pancreas, small intestine, gastric mucosa, and pyloric sphincter, where it is responsible for CCK to regulate multiple digestive processes including gallbladder contraction, pancreatic secretion, small intestinal transit, and gastric emptying...
June 19, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28618999/biomarkers-for-diagnosing-and-staging-of-fabry-disease
#8
Johannes Krämer, Frank Weidemann
BACKGROUND: Fabry disease is a X-linked lysosomal storage disorder caused by deficient activity of α -galactosidase A which leads to progressive intracellular accumulation of globotriaosylceramide in tissues and organs including heart, kidney, vascular endothelium, the nervous system, the eyes and the skin. Cardiac involvement is common, leads to fatal complications and is mainly responsible for reduced life expectancy in Fabry disease. The exact staging of disease progression and timely initiation of treatment is essential in Fabry disease...
June 16, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28618998/the-role-of-mitochondrial-dysfunction-in-the-progression-of-alzheimer-s-disease
#9
Claus Desler, Meryl S Lillenes, Tone Tønjum, Lene Juel Rasmussen
The current molecular understanding of Alzheimer's disease (AD) has still not resulted in successful interventions. Mitochondrial dysfunction of the AD brain is currently emerging as a hallmark of this disease. One mitochondrial function often affected in AD is oxidative phosphorylation responsible for ATP production, but also for production of reactive oxygen species (ROS) and for the de novo synthesis of pyrimidines. This paper reviews the role of mitochondrial produced ROS and pyrimidines in the aetiology of AD and their proposed role in oxidative degeneration of macromolecules, synthesis of essential phospholipids and maintenance of mitochondrial viability in the AD brain...
June 16, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28618997/vdac1-as-a-player-in-mitochondria-mediated-apoptosis-and-target-for-modulating-apoptosis
#10
Varda Shoshan-Barmatz, Yakov Krelin, Quan Chen
The voltage-dependent anion channel 1 (VDAC1), an outer mitochondria membrane protein, functions as a mitochondrial governor, controlling transport of metabolites in and out of the mitochondria and energy production, while also coordinating glycolysis and oxidative phosphorylation (OXPHOS). . VDAC1 plays a key role in mitochondria-mediated apoptosis by functioning in the release of apoptotic proteins located in the inter-membranal space (IMS) and due to its association with pro- and anti-apoptotic proteins...
June 16, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28618996/the-influence-of-obese-insulin-resistance-on-the-outcome-of-the-ischemia-reperfusion-insult-to-the-heart
#11
Krekwit Shinlapawittayatorn, Siriporn C Chattipakorn, Nipon Chattipakorn
BACKGROUND: Obese insulin-resistance is one of the most important risk factor for cardiovascular diseases including ischemic heart disease (IHD). Growing evidences suggest that the susceptibility to myocardial ischemia-reperfusion (I/R) injury is increased in an obese insulin-resistance condition. Based on the currently available evidence from human and animal studies, this review mainly focuses on the influence of obese insulin-resistance on the outcome of the I/R insult to the heart...
June 16, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28618995/the-complexity-of-omega-3-fatty-acids-modulation-of-signaling-pathways-related-to-pancreatic-cancer
#12
Carolina Torres, Andrew M Diaz, Daniel R Principe, Paul J Grippo
Cancer is a major public health problem worldwide and is the second leading cause of death in the United States. Although cancer death rate has dropped by 23% since 1991, there are certain types of cancer for which death rates are still increasing such as, pancreatic cancer. There is an urgent need to find new therapies that could help improve this dreadful outcome. In this regard, the role of nutrition in health and disease has attracted much attention. Several dietary ingredients are involved in metabolic, physiological, and cellular signaling affecting tumor growth and progression...
June 16, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28618994/role-of-anti-pcsk9-antibodies-in-the-treatment-of-patients-with-statin-intolerance
#13
Julia Schreml, Ioanna Gouni-Berthold
Statin intolerance is usually defined as the inability of a patient to tolerate statin-treatment due to muscle-related complaints. While randomised trials show that these complaints occure with similar frequency in patients receiving placebo, namely in up to ~5% of the subjects, data from registries as well as clinical experience indicate a much higher frequency of up to ~30%. The lack of standard definition or of a diagnostic marker of statin intolerance confounds the problem. The diagnosis remains subjective based on the symptoms the patient reports...
June 16, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28618993/new-perspectives-on-biomedical-applications-of-iron-oxide-nanoparticles
#14
Massimiliano Magro, Davide Baratella, Emanuela Bonaiuto, Jessica de Almeida Roger, Fabio Vianello
Iron oxide nanomaterials are considered promising tools for improved therapeutic efficacy and diagnostic applications in biomedicine. Accordingly, engineered iron oxide nanomaterials are increasingly proposed in biomedicine, and the interdisciplinary researches involving physics, chemistry, biology (nanotechnology) and medicine have led to exciting developments in the last decades. The progresses of the development of magnetic nanoparticles with tailored physico-chemical and surface properties produced a variety of clinically relevant applications, spanning from magnetic resonance imaging (MRI), drug delivery, magnetic hyperthermia, to in vitro diagnostics...
June 16, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28618992/modulating-mitophagy-in-mitochondrial-disease
#15
Eszter Dombi, Heather Mortiboys, Joanna Poulton
Mitochondrial diseases may result from mutations in the maternally-inherited mitochondrial DNA (mtDNA) or from mutations in nuclear genes encoding mitochondrial proteins. Their bi-genomic nature makes mitochondrial diseases a very heterogeneous group of disorders that can present at any age and can affect any type of tissue. The autophagic-lysosomal degradation pathway plays an important role in clearing dysfunctional and redundant mitochondria through a specific quality control mechanism termed mitophagy. Mitochondria could be targeted for autophagic degradation for a variety of reasons including basal turnover for recycling, starvation induced degradation, and degradation due to damage...
June 16, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28618991/effects-of-polyphenolic-derivatives-on-heme-oxygenase-system-in-metabolic-dysfunctions
#16
Valeria Pittala, Luca Vanella, Loredana Salerno, Giuseppe Romeo, Agostino Marrazzo, Claudia Di Giacomo, Valeria Sorrenti
BACKGROUND: The aim of this review is to summarize the effects of various naturally occurring polyphenols in the management of metabolic dysfunctions. This cluster of metabolic abnormalities comprises insulin resistance, increased levels of free fatty acids, hypercholesterolemia, obesity, hyperglycemia and hypertension, diabetes mellitus (DM) type 1 (T1DM) and type 2 (T2DM) along with DM-induced complications. Most of them are included in the well-known metabolic syndrome (MS). These metabolic dysfunctions in turn are tightly associated to a high risk of development of cardiovascular diseases...
June 16, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28618990/biological-roles-of-the-eclectic-chromogranin-a-derived-peptide-catestatin
#17
Teresa Pasqua, Tommaso Angelone, Angela Spena, Maria Carmela Cerra
Research on Chromogranin A (CGA) and its derived fragments convincingly demonstrated the multifunctional activity of the 21 amino acid peptide named Catestatin (CST: human CGA352-372, bovine CGA344-364, rat CGA367-387). It is mainly known as an inhibitor of the nicotinic-dependent Catecholamine (CA) release, and an anti-hypertensive peptide, but its role includes a modulation of antioxidant and immune defense, epidermal function, and adipose tissue homeostasis. CST influences the cardiocirculatory system acting both indirectly, via the autonomic nervous system, and directly by influencing the basal cardiac function, and the stretch-dependent myocardial performance...
June 16, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28606041/mechanisms-of-action-resistance-and-toxicity-of-insecticides-targeting-gaba-receptors
#18
Steven Buckingham, Makoto Ihara, David B Sattelle, Kazuhiko Matsuda
Ionotropic γ-aminobutyric acid (GABA)-gated chloride channels belong to the cys-loop superfamily of ligand-gated ion channels (cys-loop LGICs) and mediate fast inhibitory synaptic transmission in the nervous system and at neuromuscular junctions of insects. Insect GABA-gated cation channels have also been described. The sequencing of insect genomes has enhanced our understanding of the subunits that make up GABA receptor gene families of many species, including a genetic model organism (Drosophila melanogaster) as well as pest, vector and beneficial (pollinator) species...
June 12, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28595554/sulphur-containing-amino-acids-protective-role-against-free-radicals-and-heavy-metals
#19
Mirjana B Čolović, Vesna M Vasić, Dragan M Djuric, Danijela Z Krstić
Sulphur is an abundant element in biological systems, which plays an important role in processes essential for life as a constituent of proteins, vitamins and other crucial biomolecules. The major source of sulphur for humans is plants being able to use inorganic sulphur in the purpose of sulphur-containing amino acids synthesis. Sulphur-containing amino acids include methionine, cysteine, homocysteine, and taurine. Among them, methionine and cysteine are classified as proteinogenic, canonic amino acids incorporated in proteins structure...
June 8, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28595553/sulfur-containing-amino-acids-homocysteine-and-taurine-in-seizures-current-state-of-the-art
#20
Dragan Hrncic, Aleksandra Rasic-Markovic, Duro Macut, Dusan Mladenovic, Veselinka Susic, Dragan Djuric, Olivera Stanojlovic
Homocysteine and taurine are non-proteinogenic sulfur-containing amino acids with numerous important physiological roles. Homocysteine and taurine are considered to be neurotransmitters and neuromodulators, the first showing clear hyperexcitability role, while the second is known by its inhibitory and neuroprotective properties. In this article we addressed the role of homocysteine and its related metabolite homocysteine thiolactone in the development of seizures, focusing on its experimental models in vivo, potential mechanisms of proepileptogenic activity via interactions with glutamatergic neurotransmission, sodium pump activity, oxidative stress, cholinergic system and NO-mediated neuronal signaling, as well as the pharmacological and non-pharmacological approaches to modulate its proconvulsive activity...
June 8, 2017: Current Medicinal Chemistry
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