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https://www.readbyqxmd.com/read/28616949/monitoring-atpase-induced-ph-changes-in-single-proteoliposomes-with-the-lipid-coupled-fluorophore-oregon-green-488
#1
Miriam Schwamborn, Johannes Schumacher, Jeremias Sibold, Nikolas K Teiwes, Claudia Steinem
Monitoring the proton pumping activity of proteins such as ATPases in reconstituted single proteoliposomes is key to quantify the function of proteins as well as potential proton pump inhibitors. However, most pH-detecting assays available are either not quantitative, require well-adapted reconstitution protocols or are not appropriate for single vesicle studies. Here, we describe the quantitative and time-resolved detection of F-type ATPase-induced pH changes across vesicular membranes doped with the commercially available pH sensitive fluorophore Oregon Green 488 DHPE...
June 15, 2017: Analyst
https://www.readbyqxmd.com/read/28584158/identification-of-novel-efflux-proteins-rv0191-rv3756c-rv3008-and-rv1667c-involved-in-pyrazinamide-resistance-in-mycobacterium-tuberculosis
#2
Yumeng Zhang, Jia Zhang, Peng Cui, Wenhong Zhang, Ying Zhang
Pyrazinamide (PZA) is a critical drug used for the treatment of tuberculosis (TB). PZA is a prodrug that requires conversion to the active component pyrazinoic acid (POA) by pyrazinamidase (PZase) encoded by the pncA gene. Although resistance to PZA is mostly caused by pncA mutations and less commonly by rpsA, panD, and clpC1, clinical strains without these mutations are known to exist. While efflux of POA was demonstrated in Mycobacterium tuberculosis previously, the efflux proteins involved have not been identified...
June 5, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28570027/structure-activity-relationship-studies-on-6-7-dimethoxy-2-phenethyl-1-2-3-4-tetrahydroisoquinoline-derivatives-as-multidrug-resistance-mdr-reversers
#3
Elisabetta Teodori, Silvia Dei, Gianluca Bartolucci, Maria Grazia Perrone, Dina Manetti, Maria Novella Romanelli, Marialessandra Contino, Nicola Antonio Colabufo
A series of derivatives were synthesized and studied with the aim to investigate the structure-activity relationships of the two P-glycoprotein (P-gp) modulators elacridar and tariquidar. Then different aryl substituted amides were inserted and to explore the effects of varying the amide function, the corresponding isosteric ester derivatives and some alkylamine analogues were synthesized. The new compounds were studied to evaluate their P-gp interaction profile and selectivity towards the two other ABC transporters, Multidrug-Resistance-associated Protein-1 (MRP-1) and Breast Cancer Resistance Protein (BCRP)...
June 1, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28560953/nelfinavir-and-ritonavir-kill-bladder-cancer-cells-synergistically-by-inducing-endoplasmic-reticulum-stress
#4
Akinori Sato, Takako Asano, Kazuki Okubo, Makoto Isono, Tomohiko Asano
The human immunodeficiency virus (HIV) protease inhibitor nelfinavir acts against malignancies by inducing endoplasmicreticulum (ER) stress. The HIV protease inhibitor ritonavir, on the other hand, not only induces ER stress but also inhibits P-glycoprotein's pump activity and thereby enhances the effects of its substrate drugs. We therefore postulated that ritonavir in combination with nelfinavir would kill bladder cancer cells effectively by inducing ER stress cooperatively and also enhancing nelfinavir's effect...
May 26, 2017: Oncology Research
https://www.readbyqxmd.com/read/28560291/gastrin-and-gastric-cancer
#5
REVIEW
Jill P Smith, Sandeep Nadella, Nick Osborne
Gastric cancer is the third leading cause of cancer-related mortality worldwide. Despite progress in understanding its development, challenges with treatment remain. Gastrin, a peptide hormone, is trophic for normal gastrointestinal epithelium. Gastrin also has been shown to play an important role in the stimulation of growth of several gastrointestinal cancers including gastric cancer. We sought to review the role of gastrin and its pathway in gastric cancer and its potential as a therapeutic target in the management of gastric cancer...
July 2017: Cellular and Molecular Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/28549490/whole-genome-analysis-reveals-new-insights-into-macrolide-resistance-in-mycoplasma-pneumoniae
#6
Shao Li Li, Hong Mei Sun, Bao Li Zhu, Fei Liu, Han Qing Zhao
OBJECTIVE: Mutations in 23S rRNA gene are known to be associated with macrolide resistance in Mycoplasma pneumoniae (M. pneumoniae). However, these mutations alone do not fully explain the high resistance rates in Asia. The aim of this study was to investigate other possible mutations involved in macrolide resistance in M. pneumoniae. METHODS: The whole genomes of 10 clinical isolates of M. pneumoniae with macrolide resistance were sequenced by Illumina HiSeq2000 platform...
May 2017: Biomedical and Environmental Sciences: BES
https://www.readbyqxmd.com/read/28545374/modulators-of-the-efflux-pump-cdr1p-of-candida-albicans-mechanisms-of-action-and-chemical-features
#7
Viet-Khoa Tran-Nguyen, Rajendra Prasad, Pierre Falson, Ahcène Boumendjel
The multicomponent primary active ATP-binding cassette transporter Cdr1p in the structure of the pathogenic yeast Candida albicans is among the culprits of antifungal agent resistance reported in recent decades. So far, various potential novel inhibitors/ modulators of this protein have been purified, synthesized, and biologically tested, with results showing their ability to effectively reverse CaCdr1p-mediated drug resistance phenomenon. These compounds are of diverse origins, possess non-identical structural features and adopt different mechanisms of action...
May 22, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28527154/structure-based-classification-for-bile-salt-export-pump-bsep-inhibitors-using-comparative-structural-modeling-of-human-bsep
#8
Sankalp Jain, Melanie Grandits, Lars Richter, Gerhard F Ecker
The bile salt export pump (BSEP) actively transports conjugated monovalent bile acids from the hepatocytes into the bile. This facilitates the formation of micelles and promotes digestion and absorption of dietary fat. Inhibition of BSEP leads to decreased bile flow and accumulation of cytotoxic bile salts in the liver. A number of compounds have been identified to interact with BSEP, which results in drug-induced cholestasis or liver injury. Therefore, in silico approaches for flagging compounds as potential BSEP inhibitors would be of high value in the early stage of the drug discovery pipeline...
May 19, 2017: Journal of Computer-aided Molecular Design
https://www.readbyqxmd.com/read/28516219/decreased-sensory-nerve-excitation-and-bone-pain-associated-with-mouse-lewis-lung-cancer-in-trpv1-deficient-mice
#9
Hiroki Wakabayashi, Satoshi Wakisaka, Toru Hiraga, Kenji Hata, Riko Nishimura, Makoto Tominaga, Toshiyuki Yoneda
Bone pain is one of the most common and life-limiting complications of cancer metastasis to bone. Although the mechanism of bone pain still remains poorly understood, bone pain is evoked as a consequence of sensitization and excitation of sensory nerves (SNs) innervating bone by noxious stimuli produced in the microenvironment of bone metastases. We showed that bone is innervated by calcitonin gene-related protein (CGRP)(+) SNs extending from dorsal root ganglia (DRG), the cell body of SNs, in mice. Mice intratibially injected with Lewis lung cancer (LLC) cells showed progressive bone pain evaluated by mechanical allodynia and flinching with increased CGRP(+) SNs in bone and augmented SN excitation in DRG as indicated by elevated numbers of pERK- and pCREB-immunoreactive neurons...
May 17, 2017: Journal of Bone and Mineral Metabolism
https://www.readbyqxmd.com/read/28512024/repurposing-of-proton-pump-inhibitors-as-first-identified-small-molecule-inhibitors-of-endo-%C3%AE-n-acetylglucosaminidase-engase-for-the-treatment-of-ngly1-deficiency-a-rare-genetic-disease
#10
Yiling Bi, Matthew Might, Hariprasad Vankayalapati, Balagurunathan Kuberan
N-Glycanase deficiency, or NGLY1 deficiency, is an extremely rare human genetic disease. N-Glycanase, encoded by the gene NGLY1, is an important enzyme involved in protein deglycosylation of misfolded proteins. Deglycosylation of misfolded proteins precedes the endoplasmic reticulum (ER)-associated degradation (ERAD) process. NGLY1 patients produce little or no N-glycanase (Ngly1), and the symptoms include global developmental delay, frequent seizures, complex hyperkinetic movement disorder, difficulty in swallowing/aspiration, liver dysfunction, and a lack of tears...
July 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28470523/assays-for-analyzing-the-role-of-transport-proteins-in-the-uptake-and-the-vectorial-transport-of-substances-affecting-cell-viability
#11
Emir Taghikhani, Martin F Fromm, Jörg König
Endogenous compounds, drugs, or other xenobiotics may affect cell viability. A prerequisite for intracellular cell damage is the uptake of such substances across the plasma membrane into cells. Furthermore, the subsequent transporter-mediated export out of cells may influence cell viability. Therefore, transport proteins mediating the uptake (uptake transporter) or export (export pumps) of substances in and out of cells are important determinants of cell viability. Uptake transporters mostly belong to the superfamily of solute carriers (SLC transporters), whereas export pumps are members of the ABC-transporter superfamily (ATP-binding cassette)...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28468029/effect-of-protriptyline-on-ca%C3%A2-%C3%A2-%C2%BA-i-and-viability-in-mdck-renal-tubular-cells
#12
He-Hsiung Cheng, Chiang-Ting Chou, Wei-Zhe Liang, Chun-Chi Kuo, Pochuen Shieh, Jue-Long Wang, Chung-Ren Jan
Protriptyline has been used as an antidepressant. Clinically it has been prescribed in the auxiliary treatment of cancer patients. However, its effect on Ca²⁺ signaling and related physiology is unknown in renal cells. This study examined the effect of protriptyline on cytosolic free Ca²⁺ concentrations ([Ca²⁺]i) and viability in Madin-Darby canine kidney (MDCK) tubular cells. Protriptyline induced [Ca²⁺]i rises concentration-dependently. The response was reduced by 20% by removing extracellular Ca²⁺...
April 30, 2017: Chinese Journal of Physiology
https://www.readbyqxmd.com/read/28464697/assessment-of-the-procoagulant-activity-of-microparticles-and-the-protein-z-system-in-patients-undergoing-off-pump-coronary-artery-bypass-surgery
#13
Artur Słomka, Aleksandra Piekuś, Mariusz Kowalewski, Wojciech Pawliszak, Lech Anisimowicz, Ewa Żekanowska
To understand the coagulation changes after off-pump coronary artery bypass (OPCAB) surgery, we evaluated the procoagulant activity of microparticles (MPs) and microparticles exposing tissue factor (MPs-TF), together with the levels of total tissue factor (TF), protein Z (PZ), protein Z-dependent protease inhibitor (ZPI), and factor X (FX) before (first day) and 1 week after surgery (seventh day) in plasma samples from 30 patients. Twenty healthy controls were also included. Compared to the controls, patients scheduled for surgery had significantly higher MPs-TF procoagulant activity and lower TF levels ( P = ...
January 1, 2017: Angiology
https://www.readbyqxmd.com/read/28464560/matriptase-induces-metalloproteinase-dependent-aggrecanolysis-in-vitro-and-in-vivo-multiple-mechanisms-promote-cartilage-damage-in-osteoarthritis
#14
David J Wilkinson, Angela Habgood, Heather K Lamb, Paul Thompson, Alastair R Hawkins, Antoine Désilets, Richard Leduc, Torsten Steinmetzer, Maya Hammami, Melody S Lee, Charles S Craik, Sharon Watson, Hua Lin, Jennifer M Milner, Andrew D Rowan
Objectives To assess the ability of the type II transmembrane serine proteinase matriptase to promote aggrecan loss from cartilage of osteoarthritis (OA) patients, and whether matriptase inhibition could prevent aggrecan loss and cartilage damage in experimental OA. Methods Aggrecan release was assessed from human OA cartilage explants and human stem cell-derived cartilage discs, whilst cartilage conditioned media were used for western blotting. Gene expression was analysed by real-time PCR. Murine OA was induced by surgical destabilisation of the medial meniscus, and matriptase inhibitors delivered via osmotic mini-pump or intra-articular injection...
May 2, 2017: Arthritis & Rheumatology
https://www.readbyqxmd.com/read/28428443/mechanisms-of-pinometostat-epz-5676-treatment-emergent-resistance-in-mll-rearranged-leukemia
#15
Carly T Campbell, Jessica N Haladyna, David A Drubin, Ty M Thomson, Michael J Maria, Taylor Yamauchi, Nigel J Waters, Edward J Olhava, Roy M Pollock, Jesse J Smith, Robert A Copeland, Stephen J Blakemore, Kathrin M Bernt, Scott R Daigle
DOT1L is a protein methyltransferase involved in the development and maintenance of MLL-rearranged (MLL-r) leukemia through its ectopic methylation of histones associated with well characterized leukemic genes.  Pinometostat (EPZ-5676), a selective inhibitor of DOT1L, is in clinical development in relapsed/refractory acute leukemia patients harboring rearrangements of the MLL gene. The observation of responses and subsequent relapses in the adult trial treating MLL-r patients motivated preclinical investigations into potential mechanisms of pinometostat treatment emergent resistance (TER) in cell lines confirmed to have MLL-r...
April 20, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28416809/perisomatic-changes-in-h-channels-regulate-depressive-behaviors-following-chronic-unpredictable-stress
#16
C S Kim, D H Brager, D Johnston
Chronic stress can be a precipitating factor in the onset of depression. Lentiviral-mediated knockdown of HCN1 protein expression and reduction of functional Ih produce antidepressant behavior. However, whether h-channels are altered in an animal model of depression is not known. We found that perisomatic HCN1 protein expression and Ih-sensitive physiological measurements were significantly increased in dorsal but not in ventral CA1 region/neurons following chronic unpredictable stress (CUS), a widely accepted model for major depressive disorder...
April 18, 2017: Molecular Psychiatry
https://www.readbyqxmd.com/read/28393677/in-silico-high-throughput-virtual-screening-and-molecular-dynamics-simulation-study-to-identify-inhibitor-for-adeabc-efflux-pump-of-acinetobacter-baumannii
#17
Privita Verma, Monalisa Tiwari, Vishvanath Tiwari
Emergence of multi-drug resistant strains of Acinetobacter baumannii has caused significant health problems and is responsible for high morbidity and mortality. Overexpression of AdeABC efflux system is one of the major mechanisms. In this study, we have focused on overcoming the drug resistance by identifying inhibitors that can effectively bind and inhibit integral membrane protein, AdeB of this efflux pump. We performed homology modeling to generate structure of AdeB using MODELLER v9.16 followed by model refinement using 3D-Refine tool and validated using PSVS, ProsaWeb, ERRAT, etc...
April 21, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28389804/double-tract-reconstruction-after-laparoscopic-proximal-gastrectomy-using-detachable-endo-psd
#18
Tomoki Aburatani, Kazuyuki Kojima, Sho Otsuki, Hideaki Murase, Keisuke Okuno, Kentaro Gokita, Chiharu Tomii, Toshiro Tanioka, Mikito Inokuchi
BACKGROUND: Proximal gastrectomy (PG) is widely performed in Japan as a function-preserving surgical approach. Since esophagogastrostomy (EG) was associated with increased reflux symptoms and anastomotic strictures, we have chosen double-tract reconstruction (DTR) as the standard reconstruction method since March 2013. In this study, we described a novel method of laparoscopic DTR using detachable ENDO-PSD and compared its 1-year outcome with EG performed formerly in our institution. METHODS: Patients who underwent laparoscopic PG between May 2005 and July 2014 were retrospectively divided into two groups based on the type of reconstruction and were subsequently analyzed (19 patients in the DTR group and 22 in the EG group)...
April 7, 2017: Surgical Endoscopy
https://www.readbyqxmd.com/read/28388576/proton-pump-inhibitor-ilaprazole-suppresses-cancer-growth-by-targeting-t-cell-originated-protein-kinase
#19
Mengzhu Zheng, Shanshan Luan, Suyu Gao, Li Cheng, Bin Hao, Jiacheng Li, Yao Chen, Xuemei Hou, Lixia Chen, Hua Li
T-cell-originated protein kinase (TOPK) is highly and frequently expressed in various cancer tissues and plays an indispensable role in the mitosis of cancer cells, and therefore, it is an important target for drug treatment of tumor. Ilaprazole was identified to be a potent TOPK inhibitor. The data indicated that ilaprazole inhibited TOPK activities with high affinity and selectivity. In vitro studies showed that ilaprazole inhibited TOPK activities in HCT116, ES-2, A549, SW1990 cancer cells. Moreover, knockdown of TOPK in these cells decreased their sensitivities to ilaprazole...
June 13, 2017: Oncotarget
https://www.readbyqxmd.com/read/28384516/effects-of-puerarin-on-intracellular-ca-2-and-cell-viability-of-mdck-renal-tubular-cells
#20
He-Hsiung Cheng, Chiang-Ting Chou, Wei-Zhe Liang, Chun-Chi Kuo, Pochuan Shieh, Jue-Long Wang, Chung-Ren Jan
Puerarin is a natural compound and has been used as herb medication in a number of countries, especially in Asia. The effect of puerarin on Ca(2+) signaling is unknown in renal cells. This study examined whether puerarin affected Ca(2+) physiology in MDCK renal tubular cells. Cytosolic free Ca(2+) levels ([Ca(2+)]i) were measured using the fluorescent dye fura-2. Cell viability was examined by using WST-1 assay. Puerarin induced [Ca(2+)]i rises and the response was reduced by removing extracellular Ca(2+). Puerarin-induced Ca(2+) entry was not altered by protein kinase C (PKC) activity, but was inhibited by nifedipine...
March 24, 2017: Environmental Toxicology and Pharmacology
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