Πλοήγηση ανά Θέμα "antagonists and inhibitors"
Αποτελέσματα 21-40 από 47
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High consistency of structure-based design and X-ray crystallography: Design, synthesis, kinetic evaluation and crystallographic binding mode determination of biphenyl-n-acyl-β-d-glucopyranosylamines as glycogen phosphorylase inhibitors
(2019)Structure-based design and synthesis of two biphenyl-N-acyl-β-D-glucopyranosylamine derivatives as well as their assessment as inhibitors of human liver glycogen phosphorylase (hlGPa, a pharmaceutical target for type 2 ... -
IDO decreases glycolysis and glutaminolysis by activating GCN2K, while it increases fatty acid oxidation by activating AhR, thus preserving CD4+ T-cell survival and proliferation
(2018)It is generally hypothesized in the literature that indoleamine 2,3-dioxygenase (IDO), by degrading L-tryptophan along the kynurenine pathway, suppresses CD4+ T-cell function by inducing apoptosis, inhibiting proliferation ... -
Indoleamine 2,3-dioxygenase, by degrading L-tryptophan, enhances carnitine palmitoyltransferase i activity and fatty acid oxidation, and exerts fatty acid-dependent effects in human alloreactive CD4+ T-cells
(2016)Indoleamine 2,3-dioxygenase (IDO) is expressed in antigen presenting cells and by degrading L-tryptophan along the kynurenine pathway suppresses CD4+ T-cell proliferation, induces apoptosis and promotes differentiation ... -
Inflammaging and Skeletal Muscle: Can Protein Intake Make a Difference?
(2016)Inflammaging is the chronic low-grade inflammatory state present in the elderly, characterized by increased systemic concentrations of proinflammatory cytokines. It has been shown that inflammaging increases the risk of ... -
Influence of AQP1 on cell adhesion, migration, and tumor sphere formation in malignant pleural mesothelioma is substratum-and histological-type dependent
(2016)Malignant pleural mesothelioma (MPM) is an aggressive cancer. MPM cells express aquaporin-1 (AQP1) that in other cancers has been shown to participate in the tumor metastasis processes. However, in MPM patients AQP1 ... -
Istaroxime Inhibits Motility and Down-Regulates Orai1 Expression, SOCE and FAK Phosphorylation in Prostate Cancer Cells
(2017)Background/Aims: Istaroxime is a validated inotropic Na + /K + ATPase inhibitor currently in development for the treatment of various cardiac conditions. Recent findings established that this steroidal drug exhibits potent ... -
Kynurenine, by activating aryl hydrocarbon receptor, decreases erythropoietin and increases hepcidin production in HepG2 cells: A new mechanism for anemia of inflammation
(2016)It is known that inadequate erythropoietin (EPO) production contributes to the pathogenesis of anemia of inflammation, although the exact molecular mechanism is unknown. Aryl hydrocarbon receptor (AhR) may compete with ... -
Lipid-lowering treatment in peripheral artery disease
(2018)Peripheral artery disease (PAD) is characterized by increased cardiovascular (CV) risk, limb morbidity and all-cause mortality. According to the current guidelines (2016) of the American Heart Association/American College ... -
Medical management of gastric cancer: a 2017 update
(2018)Gastric cancer remains a considerable health burden throughout the world. The Cancer Genome Atlas (TCGA) analysis has recently unveiled 4 genotypes of gastric cancer with data not ready to change treatment strategy yet. A ... -
The metabolism of imidacloprid by aldehyde oxidase contributes to its clastogenic effect in New Zealand rabbits
(2018)Imidacloprid (IMI) is a systemic, chloro-nicotinyl insecticide classified in Regulation N° 1272/2008 of the European Commision as “harmful if swallowed and very toxic to aquatic life, with long-lasting effects”. IMI is ... -
A multidisciplinary study of 3-(β-D-glucopyranosyl)-5-substituted-1,2,4-triazole derivatives as glycogen phosphorylase inhibitors: Computation, synthesis, crystallography and kinetics reveal new potent inhibitors
(2018)3-(β-D-Glucopyranosyl)-5-substituted-1,2,4-triazoles have been revealed as an effective scaffold for the development of potent glycogen phosphorylase (GP) inhibitors but with the potency very sensitive to the nature of the ... -
Nanomolar Inhibitors of Glycogen Phosphorylase Based on β- D -Glucosaminyl Heterocycles: A Combined Synthetic, Enzyme Kinetic, and Protein Crystallography Study
(2017)Aryl substituted 1-(β-d-glucosaminyl)-1,2,3-triazoles as well as C-β-d-glucosaminyl 1,2,4-triazoles and imidazoles were synthesized and tested as inhibitors against muscle and liver isoforms of glycogen phosphorylase (GP). ... -
Neuroimaging and clinical outcomes of oral anticoagulant–associated intracerebral hemorrhage
(2018)Objective: Whether intracerebral hemorrhage (ICH) associated with non–vitamin K antagonist oral anticoagulants (NOAC-ICH) has a better outcome compared to ICH associated with vitamin K antagonists (VKA-ICH) is uncertain. ... -
The nitric oxide donor sodium nitroprusside attenuates recognition memory deficits and social withdrawal produced by the NMDA receptor antagonist ketamine and induces anxiolytic-like behaviour in rats
(2016)Rationale: Experimental evidence indicates that the non-competitive N-methyl-d-aspartate (NMDA) receptor antagonist ketamine impairs cognition and can mimic certain aspects of positive and negative symptoms of schizophrenia ... -
Phytogenic polyphenols as glycogen phosphorylase inhibitors: The potential of triterpenes and flavonoids for glycaemic control in type 2 diabetes
(2017)Glycogen phosphorylase (GP) is a validated pharmaceutical target for the development of antihyperglycaemic agents. Phytogenic polyphenols, mainly flavonoids and pentacyclic triterpenes, have been found to be potent inhibitors ... -
Probing the β-pocket of the active site of human liver glycogen phosphorylase with 3-(C-β-D-glucopyranosyl)-5-(4-substituted-phenyl)-1, 2, 4-triazole inhibitors
(2018)Human liver glycogen phosphorylase (hlGP), a key enzyme in glycogen metabolism, is a valid pharmaceutical target for the development of new anti-hyperglycaemic agents for type 2 diabetes. Inhibitor discovery studies have ... -
Proprotein convertase subtilisin kexin 9 (PCSK9) inhibitors to treat hypercholesterolemia: Effect on stroke risk
(2016)Background/purpose A reduction of cardiovascular events has been reported in phase 2 and 3 trials of the proprotein convertase subtilisin kexin 9 (PCSK9) inhibitors alirocumab and evolocumab. We aimed to investigate the ... -
RecA: A universal drug target in pathogenic bacteria
(2018)The spread of bacterial infectious diseases due to the development of resistance to antibiotic drugs in pathogenic bacteria is an emerging global concern. Therefore, the efficacious management and prevention of bacterial ... -
Replication of PTPRC as genetic biomarker of response to TNF inhibitors in patients with rheumatoid arthritis
(2016)Genetic biomarkers could be useful for orienting treatment of patients with rheumatoid arthritis (RA), but none has been convincingly validated yet. Putative biomarkers include 14 single nucleotide polymorphisms that have ... -
The role of nitric oxide synthase inhibitors in schizophrenia
(2016)Close to 1% of the world population suffer from schizophrenia. Current medications for this chronic mental disorder have greatly improved treatment over the last half century or more, but, the newer atypical antipsychotics ...