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PubMed Journals Articles About "Bacterial Efflux Pump Inhibitors Pipeline Insights 2017 Updated" RSS

18:02 EST 20th January 2019 | BioPortfolio

Bacterial Efflux Pump Inhibitors Pipeline Insights 2017 Updated PubMed articles on BioPortfolio. Our PubMed references draw on over 21 million records from the medical literature. Here you can see the latest Bacterial Efflux Pump Inhibitors Pipeline Insights 2017 Updated articles that have been published worldwide.

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Showing "Bacterial Efflux Pump Inhibitors Pipeline Insights 2017 Updated" PubMed Articles 1–25 of 14,000+

Efflux Pump Inhibitors, Alpha-Tocopherol and Aspirin: Role in Campylobacter jejuni and Campylobacter coli Fluoroquinolone Resistance.

This study aimed to investigate how efflux pump activity contributes to high fluoroquinolone (FQ) resistance in Campylobacter jejuni and Campylobacter coli isolates and to evaluate the modulatory effects of α-tocopherol and aspirin on FQ phenotypic resistance profiles. Minimum inhibitory concentration (MIC) values were obtained for different FQ agents following exposure to different efflux pump inhibitors (EPIs), including PaβN (50 μg/mL), which targets the cmeABC efflux system, and chlorpromazine (45...


Studies on 2-phenylquinoline Staphylococcus aureus NorA efflux pump inhibitors: New insights on the C-6 position.

The alarming and rapid spread of antimicrobial resistance among bacteria represents a high risk for global health. Targeting factors involved in resistance to restore the activity of failing antibiotics is a promising strategy to overcome this urgent medical need. Efflux pump inhibitors are able to increase antibiotic concentrations in bacteria, thus they can be considered true antimicrobial resistance breakers. In this work, continuing our studies on inhibitors of the Staphylococcus aureus NorA pump, we de...

Targeted Efflux Transporter Inhibitors - A Solution to Improve Poor Cellular Accumulation of Anti-Cancer Agents.

Efflux transporters function as vacuum cleaners of xenobiotics and therefore they hinder drugs to reach their targets at effective enough concentrations. Efflux pump inhibitors can be used to improve the cell accumulation of drugs, however all the current inhibitors lack selectivity towards cancer cells. L-Type amino acid transporter 1 (LAT1), which is expressed in many types of cancer cells can be utilized to target inhibitors of efflux transporters to these cells by converting the inhibitors into LAT1-uti...


2-Phenylquinoline S. aureus NorA Efflux Pump Inhibitors: Evaluation of the Importance of Methoxy Groups Introduction.

Antimicrobial resistance (AMR) represents a hot topic in drug discovery. Besides the identification of new antibiotics, the use of non-antibiotic molecules to block resistance mechanisms is a powerful alternative. Bacterial efflux pumps exert an early step in AMR development by allowing bacteria to grow at sub-inhibitorial drug concentrations. Thus, efflux pump inhibitors (EPIs) offer a great opportunity to fight AMR. Given our experience in developing Staphylococcus aureus NorA EPIs, in this work, starting...

Proton Pump Inhibitors and the Risk of Dementia: is There a Link?

Dementia is one of the most common neurodegenerative disorder among older populations around the world, and the incidence is increasing. Many epidemiologic studies have considered the association between proton-pump inhibitors and dementia, yet the relationship is still controversial.The objective of this study was to validate whether or not proton-pump inhibitors is indeed associated with dementia.Materials (Subjects) and Methods: We searched for articles on clinical studies of dementia and proton pump inh...

Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria.

Even though many GyrB and ParE inhibitors have been reported in the literature, few possess activity against Gram-negative bacteria. This is primarily due to limited permeability across Gram-negative bacterial membrane as well as bacterial efflux mechanisms. Permeability of compounds across Gram-negative bacterial membranes depends on many factors including physicochemical properties of the inhibitors. Herein, we show the optimization of pyridylureas leading to compounds with potent activity against Gram-ne...

Proton pump inhibitors are associated to minimal and overt hepatic encephalopathy and increase mortality in cirrhotics.

Minimal hepatic encephalopathy (MHE) is a subclinical cognitive impairment frequently observable in cirrhotics. Proton pump inhibitors (PPIs) can contribute to small-bowel bacterial overgrowth but no study investigated the link between PPIs and MHE.

Efflux pumps and antimicrobial resistance: Paradoxical components in systems genomics.

Efflux pumps play a major role in the increasing antimicrobial resistance rendering a large number of drugs of no use. Large numbers of pathogens are becoming multidrug resistant due to inadequate dosage and use of the existing antimicrobials. This leads to the need for identifying new efflux pump inhibitors. Design of novel targeted therapies using inherent complexity involved in the biological network modeling has gained increasing importance in recent times. The predictive approaches should be used to de...

Neutropenia and Thrombocytopenia Induced by Proton Pump Inhibitors: A Case Report.

An 85-year-old man was admitted to our hospital because of dysphagia, and was diagnosed with benign stricture of the esophagus. He was hospitalized repeatedly for balloon dilations. Pantoprazole sodium (80 mg, twice daily, intravenously) was administered each time when he was in hospital, while esomeprazole (20 mg/day, orally) was administered intermittently when he was at home. Reductions in both white blood cells and platelets were noticed about 4 months after proton pump inhibitors were introduced. Bo...

Resistance modulatory and efflux-inhibitory activities of capsaicinoids and capsinoids.

Capsaicinoids are reported to have a bunch of promising pharmacological activities, among them antibacterial effects against various strains of bacteria. In this study the effect on efflux pumps of mycobacteria was investigated. The importance of efflux pumps, and the inhibition of these, is rising due to their involvement in antibiotic resistance development. In order to draw structure and activity relationships we tested natural and synthetical capsaicinoids as well as synthetical capsinoids. In an accumu...

Adverse effects of proton pump inhibitors: fact or fake news?

The present review summarizes the past year's literature, both clinical and basic science, regarding potential adverse effects of proton pump inhibitors.

Isovalerylshikonin, a new resistance-modifying agent from Arnebia euchroma, supresses antibiotic resistance of drug-resistant Staphylococcus aureus.

Antimicrobial resistance is the greatest threat to the treatment of bacterial infectious diseases. The development of resistance-modifying agents represents a promising strategy to mitigate the spread of bacterial antibiotic resistance. A natural product, isovalerylshikonin (IVS), was isolated from traditional Chinese medicine Arnebia euchroma in this study, which exhibited marginal antibacterial activity against drug-resistant Staphylococcus aureus RN4220, with an MIC of 16 mg/L. In addition, a synergistic...

Role of the Klebsiella pneumoniae TolC porin in antibiotic efflux.

The major Gram-negative gated efflux channel TolC has been extensively characterized in Escherichia coli but there is minimal information about Klebsiella pneumoniae TolC. Using an arabinose-inducible plasmid-based expression system, we show that the K. pneumoniae TolC complements the efflux defect in an E. coli K-12 ΔtolC strain, restoring wild-type levels of resistance towards most antibiotics suggesting that it can interact with the E. coli AcrB efflux pump. We characterize the efflux properties of K. p...

Proton pump inhibitors use and risk of hepatocellular carcinoma.

One cohort study using the Taiwan's database conducted by Kao et al published in Hepatology reported that proton pump inhibitors use was not associated with the risk of developing hepatocellular carcinoma in patients with chronic hepatitis B infection or chronic hepatitis C infection. The findings were compatible with our cohort analysis using the Taiwan's database showing no association between proton pump inhibitors use and hepatocellular carcinoma. In contrast, a recent case-control study using the Taiw...

Lean body weight dosing avoids excessive systemic exposure to proton pump inhibitors for children with obesity.

Children with obesity are more likely to suffer gastroesophageal reflux disease, requiring acid-suppression therapy with proton pump inhibitors (PPIs) and no guidelines regarding dosing.

Use of proton pump inhibitors and risk of ischemic events in the general population.

A potential increased risk of cardiovascular events has been suggested for proton pump inhibitors (PPIs), the most commonly prescribed drugs for the management of upper gastrointestinal disorders. We aimed to estimate the risk of hospitalization for cardio/cerebrovascular (CV) events in a cohort of incident PPI users.

Expression analysis of 10 efflux pump genes in multi/extensively drug-resistant Mycobacterium tuberculosis isolates of clinical origin.

Active extrusion of antituberculosis (TB) drugs using efflux pumps (EPs) has been suggested as a conributing determinant of drug resistance in Mycobacterium tuberculosis (MTB). The present study was conducted to determine the role of 10 drug efflux transporters in devoloping drug resistance in a series of clinical MTB isolates.

Use of proton pump inhibitors among Danish children: a 16-year register-based nationwide study.

Proton pump inhibitors (PPI) are among the most frequently used drugs in the developed countries. In recent years, their use among children and adolescents has been on the increase. Guidelines recommend use for a period no longer than 4-8 weeks. The aim of this study was to describe time trends in prescribing patterns of PPI use among children, with emphasis on persistence to therapy.

Proton Pump Inhibitors (PPIs) are inhibitors or risk factor for Atrial Fibrillation?

A novel bi-functional chalcone inhibits multi-drug resistant Staphylococcus aureus and potentiates the activity of fluoroquinolones.

Staphylococcus aureus is the leading cause of bacteraemia and the dwindling supply of effective antibacterials has exacerbated the problem of managing infections caused by this bacterium. Isoliquiritigenin (ISL) is a plant flavonoid that displays therapeutic potential against S. aureus. The present study identified a novel mannich base derivatives of ISL, IMRG4, active against Vancomycin intermediate S. aureus (VISA). IMRG4 damages the bacterial membranes causing membrane depolarization and permeabilization...

Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors.

Bruton's tyrosine kinase (Btk) is a member of the Tec kinase family that is expressed in cells of hematopoietic lineage (e.g. B cells, macrophages, monocytes, and mast cells). Small molecule covalent irreversible Btk inhibitors targeting Cys481 within the ATP-binding pocket have been applied in the treatment of B-cell malignancies. Starting from a fragment, we discovered a novel series of potent covalent irreversible Btk inhibitors that bear N-linked groups occupying the solvent accessible pocket (SAP) of t...

Duration and dosing of Proton Pump Inhibitors associated with high incidence of chronic kidney disease in population-based cohort.

Proton Pump Inhibitors (PPIs) have been associated with chronic kidney disease (CKD). Our objective was to quantify the association between PPI use and incident CKD in a population-based cohort.

Update on the effects of the sodium pump α1 subunit on human glioblastoma: from the laboratory to the clinic.

Glioblastoma is a debilitating disease that is associated with poor prognosis and a very limited response to therapies; thus, molecularly targeted therapeutics and personalized therapy are urgently needed. The Na/K-ATPase sodium pump is a transmembrane protein complex that has recently been recognized as an important transducer and integrator of various signals. The sodium pump α1 subunit, which is highly expressed in most glioblastomas compared with that in normal brain tissues, is an emerging cancer targ...

H2 Receptor Antagonists versus Proton Pump Inhibitors in Patients on Dual Antiplatelet Therapy for Coronary Artery Disease: A Systematic Review.

Mitigating the gastrointestinal (GI) bleeding risks of dual antiplatelet therapy (DAPT) is a common clinical concern. While proton pump inhibitors (PPIs) remain the most effective therapy, their adverse events warrant considering alternatives, including Histamine 2 receptor antagonists (H2RAs).

Proton pump inhibitors therapy and risk of bone diseases: An update meta-analysis.

Large observational studies have yielded conflicting results regarding whether the use of proton pump inhibitors (PPI) increases the risk of bone diseases. Here, we performed a meta-analysis to examine the link between PPI and risk of bone fractures, osteoporosis and bone mineral density (BMD) loss.


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