Read by QxMD icon Read

inhibitors pump

Jinshan Jin, Ying-Hsin Hsieh, Jianmei Cui, Krishna Damera, Chaofeng Dai, Arpana S Chaudhary, Hao Zhang, Hsiuchin Yang, Nannan Cao, Chun Jiang, Martti Vaara, Binghe Wang, Phang C Tai
With the widespread emergence of drug resistance, there is an urgent need to search for new antimicrobials, especially those against Gram-negative bacteria. Along this line, the identification of viable targets is a critical first step. The protein translocase SecA is commonly believed to be an excellent target for the development of broad-spectrum antimicrobials. In recent years, we developed three structural classes of SecA inhibitors that have proven to be very effective against Gram-positive bacteria. However, we have not achieved the same level of success against Gram-negative bacteria, despite the potent inhibition of SecA in enzyme assays by the same inhibitors...
October 18, 2016: ChemMedChem
Meghan MacKenzie, Richard Hall
PURPOSE: Knowledge of how alterations in pharmacogenomics and pharmacogenetics may affect drug therapy in the intensive care unit (ICU) has received little study. We review the clinically relevant application of pharmacogenetics and pharmacogenomics to drugs and conditions encountered in the ICU. SOURCE: We selected relevant literature to illustrate the important concepts contained within. PRINCIPAL FINDINGS: Two main approaches have been used to identify genetic abnormalities - the candidate gene approach and the genome-wide approach...
October 17, 2016: Canadian Journal of Anaesthesia, Journal Canadien D'anesthésie
M D'Alessandro, P Turina, B A Melandri, S D Dunn
The ε-subunit of ATP-synthase is an endogenous inhibitor of the hydrolysis activity of the complex and its α-helical C-terminal domain (εCTD) undergoes drastic changes among at least two different conformations. Even though this domain is not essential for ATP synthesis activity, there is evidence for its involvement in the coupling mechanism of the pump. Recently, it was proposed that coupling of the ATP synthase can vary as a function of ADP and Pi concentration. In the present work, we have explored the possible role of the εCTD in this ADP- and Pi-dependent coupling, by examining an εCTD-lacking mutant of Escherichia coli...
October 14, 2016: Biochimica et Biophysica Acta
Tomasz Wołkowicz, Jan Andrzej Patzer, Wanda Kamińska, Rafał Gierczyński, Danuta Dzierżanowska
This study aimed to analyse the distribution of carbapenem resistance mechanisms among Pseudomonas aeruginosa clinical isolates. Fifty-five P. aeruginosa isolates, resistant both to imipenem and meropenem, from children hospitalised in 2009-2010 were studied. All strains were genotyped by pulsed-field gel electrophoresis (PFGE). Mutations in the oprD gene and the occurrence of insertion sequences (ISs) were determined by DNA sequencing. Mex efflux systems were determined by analysis using the efflux pump inhibitor Phe-Arg β-naphthylamide...
October 8, 2016: Journal of Global Antimicrobial Resistance
Isabelle Récoché, Vanessa Rousseau, Robert Bourrel, Maryse Lapeyre-Mestre, Leila Chebane, Fabien Despas, Jean-Louis Montastruc, Emmanuelle Bondon-Guitton
Many patients treated with imatinib, used in cancer treatment, are using several other drugs that could interact with imatinib. Our aim was to study all the drug-drug interactions (DDIs) observed in patients treated with imatinib.We performed 2 observational studies, between the 1st January 2012 and the 31st August 2015 in the Midi-Pyrénées area (South Western France), using the French health insurance reimbursement database and then the French Pharmacovigilance Database (FPVD).A total of 544 patients received at least 1 reimbursement for imatinib...
October 2016: Medicine (Baltimore)
Shuitu Feng, Zhigao Zheng, Lihua Feng, Lihong Yang, Zuhong Chen, Yubiao Lin, Yingqin Gao, Yide Chen
The cancer stem cell (CSC) model suggests that a small subset of cancer cells possess stem cell properties and plays a crucial role in tumor initiation, metastasis and resistance to anticancer therapy. Exploration of the specific therapies targeting at CSCs has been a crucial issue in antitumor research. Gastric cancer (GC) cells often exist in an ischemic microenvironment with acidic conditions in vivo, thus maintenance of cellular pH homeostasis is important for the survival and function of GC cells. Proton pump inhibitors (PPIs) may prevent intracellular proton extrusions which consequently reduce cancer cell survival under acidic conditions...
October 7, 2016: Oncology Reports
Krystina Parker, Willy Aasebø, Knut Stavem
BACKGROUND: Polypharmacy is commonly applied to elderly haemodialysis patients for treating terminal renal failure and multiple co-morbidities. Potentially inappropriate medications (PIMs) in multidrug regimens in geriatric populations can be identified using specially designed screening tools. OBJECTIVE: The aims of this study were to estimate the prevalence of PIMs by applying the Screening Tool of Older Persons' Prescriptions (STOPP) criteria and the Beers criteria to elderly haemodialysis patients and to assess the association of some risk factors with the presence of PIMs...
September 2016: Drugs—Real World Outcomes
Cristina Varas-Lorenzo, Alejandro Arana, Catherine B Johannes, Lisa J McQuay, Kenneth J Rothman, Daniel Fife
BACKGROUND: The ascertainment of sudden cardiac death (SCD) in electronic health databases is challenging. OBJECTIVES: Our objective was to evaluate the applicability of the validated computer definition of SCD developed by Chung et al. in a retrospective study of SCD and domperidone exposure in the Clinical Practice Research Datalink (CPRD). METHODS: We assessed out-of-hospital SCD by applying the validated computer definition and linking data with Hospital Episode Statistics and death certificates...
September 2016: Drugs—Real World Outcomes
Yusuf Haydar Ertekin, Burkay Yakar, Hülya Ertekin, Ayşegül Uludağ, Murat Tekin
BACKGROUND: Drugs represent one of the etiologic causes of acute rhabdomyolysis (AR) with drug-induced rhabdomyolysis most commonly associated with HMG-CoA reductase inhibitors. AR etiology can also result from the use of diclofenac, a non-steroidal anti-inflammatory drug, and omeprazole, a proton pump inhibitor. Cases of AR triggered by pantoprazole have never before been reported, although it has been observed that its inclusion in multiple drug therapies can result in muscle events...
December 2015: Drug Saf Case Rep
Amr Shaaban Hanafy, Amr Talaat El Hawary
Objectives: Evaluation of the outcome and experience in 2 years of management of portal hypertensive gastropathy (PHG) by argon plasma coagulation (APC) in a cohort of Egyptian cirrhotic patients. Methods: This study was conducted over a 2-year period from January 2011 to February 2013. Upper gastrointestinal endoscopy was performed to evaluate the degree and site of PHG. APC was applied to areas with mucosal vascular lesions. Results: In total, 200 cirrhotic patients were enrolled; 12 patients were excluded due to death (n = 6) caused by hepatic encephalopathy (n = 3), hepatorenal syndrome (n = 2), or chronic lymphatic leukemia (n = 1), or did not complete the treatment sessions (n = 6), so 188 patients completed the study...
October 2016: Endoscopy International Open
Dujuan Zhao, Huiyuan Zhang, Shengfeng Yang, Wenxiu He, Yuxia Luan
The main cause of multidrug resistance (MDR) is overexpression of active efflux transporters, such as P-glycoprotein (P-gp). To reverse MDR and improve the chemotherapy effect of paclitaxel (PTX), we propose a new drug delivery system based on mixed micelles constructed with D-α-tocopheryl poly(ethylene glycol) 1000 succinate (TPGS) and the mPEG-SS-PTX conjugate with consideration that TPGS is a P-gp inhibitor that can block the cancer cell action of pumping drugs outside of cells and can enhance the anticancer effect...
October 13, 2016: International Journal of Pharmaceutics
Frank Zerbib
Eosinophilic esophagitis is a major cause of dysphagia and esophageal food impaction in young adults, although the diagnostic can be made in older patients. The diagnosis of eosinophilic esophagitis is suspected on endoscopic abnormalities of esophageal mucosa and confirmed by esophageal biopsy samples. Approximately 50% of patients with eosinophilic esophagitis do respond to proton pump inhibitors therapy. The first line therapy for eosinophilic esophagitis is proton pump inhibitor therapy. Ingested topical steroids represent a second-line therapy...
October 10, 2016: La Presse Médicale
Ari Garber, Sunguk Jang
Non-variceal upper gastrointestinal bleeding, the most common etiology of which is peptic ulcer disease, remains a persistent challenge despite a reduction in both its incidence and mortality. Both pharmacologic and endoscopic techniques have been developed to achieve hemostasis, with varying degrees of success. Among the pharmacologic therapies, proton pump inhibitors remain the mainstay of treatment, as they reduce the risk of rebleeding and requirement for recurrent endoscopic evaluation. Tranexamic acid, a derivative of the amino acid lysine, is an antifibrinolytic agent whose role requires further investigation before application...
September 2016: Clinical Endoscopy
Zaheer Nabi, D Nageshwar Reddy
Gastroesophageal reflux disease (GERD) is defined by the presence of troublesome symptoms resulting from the reflux of gastric contents. The prevalence of GERD is increasing globally. An incompetent lower esophageal sphincter underlies the pathogenesis of GERD. Proton pump inhibitors (PPIs) form the core of GERD management. However, a substantial number of patients do not respond well to PPIs. The next option is anti-reflux surgery, which is efficacious, but it has its own limitations, such as gas bloating, inability to belch or vomit, and dysphagia...
September 2016: Clinical Endoscopy
Nicole A Huijgen, Maria A J de Ridder, Katia M Verhamme, Gert R Dohle, Ann M Vanrolleghem, Miriam C J M Sturkenboom, Joop S E Laven, Régine P M Steegers-Theunissen
OBJECTIVE: To determine associations between proton-pump inhibitor (PPI) use and semen parameters in young men of couples who are planning pregnancy. DESIGN: Case-control study of a population-based registry. SETTING: Not applicable. PATIENT(S): General practitioner patients comprising 2,473 men from couples planning pregnancy with a recorded semen analysis: 241 with a low total motile sperm count (TMSC ≤1) and 714 with TMSC >1 as matched controls...
October 12, 2016: Fertility and Sterility
Mario Iannaccone, Fabrizio D Ascenzo, Ovidio De Filippo, Marco Gagliardi, Danielle A Southern, Sergio Raposeiras-Roubín, Emad Abu-Assi, Jose Paulo Simao Henriques, Jorge Saucedo, José Ramón González-Juanatey, Stephen B Wilton, Wouter J Kikkert, Iván Nuñez-Gil, Albert Ariza-Sole, Xiantao Song, Dimitrios Alexopoulos, Christoph Liebetrau, Tetsuma Kawaji, Zenon Huczek, Shao-Ping Nie, Toshiharu Fujii, Luis Correia, Masa-Aki Kawashiri, José María García-Acuña, Emilio Alfonso, Belén Terol, Alberto Garay, Dongfeng Zhang, Yalei Chen, Ioanna Xanthopoulou, Neriman Osman, Helge Möllmann, Hiroki Shiomi, Michal Kowara, Krzysztof Filipiak, Xiao Wang, Yan Yan, Jing-Yao Fan, Yuji Ikari, Takuya Nakahashi, Kenji Sakata, Masakazu Yamagishi, Claudio Moretti, Fiorenzo Gaita, Oliver Kalpak, Sasko Kedev
OBJECTIVE: Our objective was to define the most appropriate treatment for acute coronary syndrome (ACS) in patients with malignancy. METHODS AND RESULTS: The BleeMACS project is a worldwide multicenter observational prospective registry in 16 hospitals enrolling patients with ACS undergoing percutaneous coronary intervention. Primary endpoints were death, re-infarction, and major adverse cardiac events (MACE; composite of death and re-infarction) after 1 year of follow-up...
October 13, 2016: American Journal of Cardiovascular Drugs: Drugs, Devices, and Other Interventions
Dennis Åsberg, Marek Leśko, Jörgen Samuelsson, Anders Karlsson, Krzysztof Kaczmarski, Torgny Fornstedt
The adsorption of the proton-pump inhibitor omeprazole was investigated using RP-LC with chemometric models combined with adsorption isotherm modelling to study the effect of pH and type of organic modifier (i.e., acetonitrile or methanol). The chemometric approach revealed that omeprazole was tailing with methanol and fronting with acetonitrile along with increased fronting at higher pH. The increased fronting with higher pH for acetonitrile was explored using a pH-dependent adsorption isotherm model that was determined using the inverse method and it agreed well with the experimental data...
2016: Chromatographia
Tal Lorberbaum, Kevin J Sampson, Jeremy B Chang, Vivek Iyer, Raymond L Woosley, Robert S Kass, Nicholas P Tatonetti
BACKGROUND: QT interval-prolonging drug-drug interactions (QT-DDIs) may increase the risk of life-threatening arrhythmia. Despite guidelines for testing from regulatory agencies, these interactions are usually discovered after drugs are marketed and may go undiscovered for years. OBJECTIVES: Using a combination of adverse event reports, electronic health records (EHR), and laboratory experiments, the goal of this study was to develop a data-driven pipeline for discovering QT-DDIs...
October 18, 2016: Journal of the American College of Cardiology
Juan Manuel Belardinelli, Amira Yazidi, Liang Yang, Lucien Fabre, Wei Li, Benoit Jacques, Shiva Kumar Angala, Isabelle Rouiller, Helen I Zgurskaya, Jurgen Sygusch, Mary Jackson
The MmpL family of proteins translocates complex (glyco)lipids and siderophores across the cell envelope of mycobacteria and closely related Corynebacteriaceae and plays important roles in the biogenesis of the outer membrane of these organisms. Despite their significance in the physiology and virulence of Mycobacterium tuberculosis, and from the perspective of developing novel antituberculosis agents, little is known about their structure and mechanism of translocation. In this study, the essential mycobacterial mycolic acid transporter, MmpL3, and its orthologue in Corynebacterium glutamicum, CmpL1, were investigated as prototypical MmpL proteins to gain insight into the transmembrane topology, tertiary and quaternary structures, and functional regions of this transporter family...
October 14, 2016: ACS Infectious Diseases
Malkeet Kumar, Kawaljit Singh, Krupa Naran, Fahreta Hamzabegovic, Daniel F Hoft, Digby F Warner, Peter Ruminski, Getahun Abate, Kelly Chibale
Efflux pumps are considered a major potential contributor to the development of various forms of resistance in Mycobacterium tuberculosis leading to the emergence of multidrug-resistant tuberculosis (TB). Verapamil (VER) and tricyclic chemosensitizers such as the phenothiazines are known to possess efflux pump inhibition properties and have demonstrated significant efficacy in various TB disease models. Novel hybrid molecules based on fusion of the VER substructure with various tricyclic, as well as nontricyclic, chemosensitizer cores or their structural motifs are described...
October 14, 2016: ACS Infectious Diseases
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"