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Protein pump inhibitor

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https://www.readbyqxmd.com/read/28720734/lack-of-acrb-efflux-function-confers-loss-of-virulence-on-salmonella-enterica-serovar-typhimurium
#1
Xuan Wang-Kan, Jessica M A Blair, Barbara Chirullo, Jonathan Betts, Roberto M La Ragione, Alasdair Ivens, Vito Ricci, Timothy J Opperman, Laura J V Piddock
AcrAB-TolC is the paradigm resistance-nodulation-division (RND) multidrug resistance efflux system in Gram-negative bacteria, with AcrB being the pump protein in this complex. We constructed a nonfunctional AcrB mutant by replacing D408, a highly conserved residue essential for proton translocation. Western blotting confirmed that the AcrB D408A mutant had the same native level of expression of AcrB as the parental strain. The mutant had no growth deficiencies in rich or minimal medium. However, compared with wild-type SL1344, the mutant had increased accumulation of Hoechst 33342 dye and decreased efflux of ethidium bromide and was multidrug hypersusceptible...
July 18, 2017: MBio
https://www.readbyqxmd.com/read/28713161/functional-expression-of-the-ca-2-signaling-machinery-in-human-embryonic-stem-cells
#2
Ji-Jun Huang, Yi-Jie Wang, Min Zhang, Peng Zhang, He Liang, Hua-Jun Bai, Xiu-Jian Yu, Huang-Tian Yang
Emerging evidence suggests that Ca(2+) signals are important for the self-renewal and differentiation of human embryonic stem cells (hESCs). However, little is known about the physiological and pharmacological properties of the Ca(2+)-handling machinery in hESCs. In this study we used RT-PCR and Western blotting to analyze the expression profiles of genes encoding Ca(2+)-handling proteins; we also used confocal Ca(2+) imaging and pharmacological approaches to determine the contribution of the Ca(2+)-handling machinery to the regulation of Ca(2+) signaling in hESCs...
July 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28700656/unexpected-effects-of-azole-transporter-inhibitors-on-antifungal-susceptibility-in-candida-glabrata-and-other-pathogenic-candida-species
#3
Yohsuke Nagayoshi, Taiga Miyazaki, Shintaro Shimamura, Hironobu Nakayama, Asuka Minematsu, Shunsuke Yamauchi, Takahiro Takazono, Shigeki Nakamura, Katsunori Yanagihara, Shigeru Kohno, Hiroshi Mukae, Koichi Izumikawa
The pathogenic fungus Candida glabrata is often resistant to azole antifungal agents. Drug efflux through azole transporters, such as Cdr1 and Cdr2, is a key mechanism of azole resistance and these genes are under the control of the transcription factor Pdr1. Recently, the monoamine oxidase A (MAO-A) inhibitor clorgyline was shown to inhibit the azole efflux pumps, leading to increased azole susceptibility in C. glabrata. In the present study, we have evaluated the effects of clorgyline on susceptibility of C...
2017: PloS One
https://www.readbyqxmd.com/read/28700113/na-k-atpase-coupled-to-endothelin-receptor-type-b-stimulates-peripheral-nerve-regeneration-via-lactate-signaling
#4
Nguyen H Tu, Tayo Katano, Shinji Matsumura, Nobuo Funatsu, Vuong Minh Pham, Jun-Ichi Fujisawa, Seiji Ito
We have recently demonstrated that endothelin (ET) is functionally coupled to Nax , a Na(+) concentration-sensitive Na(+) channel for lactate release via ET receptor type B (ETB R) and is involved in peripheral nerve regeneration in a sciatic nerve transection-regeneration mouse model. Nax is known to interact directly with Na(+) /K(+) -ATPase, leading to lactate production in the brain. To investigate the role of Na(+) /K(+) -ATPase in peripheral nerve regeneration, in the present study we applied ouabain, a Na(+) /K(+) -ATPase inhibitor, to the cut site for 4 weeks with an osmotic pump...
July 12, 2017: European Journal of Neuroscience
https://www.readbyqxmd.com/read/28682903/acute-abrin-poisoning-treated-with-continuous-renal-replacement-therapy-and-hemoperfusion-successfully-a-case-report
#5
Jiliang Huang, Wenbin Zhang, Xin Li, Shufen Feng, Gang Ye, Hongcheng Wei, Xiaobing Gong
RATIONALE: Abrin is a highly toxic protein obtained from the seeds of Abrus precatorius, but poisoning due to ingestion of A precatorius is extremely rare in China. PATIENT CONCERNS: A 16-year-old girl, perfectly healthy before, was admitted to the department of gastroenterology owing to intentional ingestion of 10 crushed A precatorius seeds, with multiple episodes of somnolent and anxious mental status, vomiting, abdominal pain, diarrhea, hematochezia, and hematuria...
July 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28671633/l1210-cells-overexpressing-abcb1-drug-transporters-are-resistant-to-inhibitors-of-the-n-and-o-glycosylation-of-proteins
#6
Lucia Pavlikova, Mario Seres, Milan Hano, Viera Bohacova, Ivana Sevcikova, Tomas Kyca, Albert Breier, Zdena Sulova
Overexpression of P-glycoprotein (P-gp, drug transporter) in neoplastic cells is the most frequently observed molecular cause of multidrug resistance. Here, we show that the overexpression of P-gp in L1210 cells leads to resistance to tunicamycin and benzyl 2-acetamido-2-deoxy-α-d-galactopyranoside (GalNAc-α-O-benzyl). Tunicamycin induces both glycosylation depression and ubiquitination improvement of P-gp. However, the latter is not associated with large increases in molecular mass as evidence for polyubiquitination...
July 3, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28669723/the-jak2-inhibitors-cep-33779-and-nvp-bsk805-have-high-p-gp-inhibitory-activity-and-sensitize-drug-resistant-cancer-cells-to-vincristine
#7
J I Hyun Cheon, Kyeong Seok Kim, Mihyun Kim, Hyung Sik Kim, Sungpil Yoon
P-glycoprotein (P-gp) is overexpressed in cancer cells in order to pump out chemotherapeutic drugs, and is one of the major mechanisms responsible for multidrug resistance (MDR). It is important to identify P-gp inhibitors with low toxicity to normal cells in order to increase the efficacy of anti-cancer drugs. Previously, a JAK2 inhibitor CEP-33779 demonstrated inhibitory actions against P-gp and an ability to sensitize drug-resistant cancer cells to treatment. In the present study, we tested another JAK2 inhibitor NVP-BSK805 for P-gp inhibitory activity...
June 29, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28658523/effect-of-tetramethylpyrazine-tmp-on-ca-2-signal-transduction-and-cell-viability-in-a-model-of-renal-tubular-cells
#8
Yi-Chien Fang, Chiang-Ting Chou, Wei-Zhe Liang, Chun-Chi Kuo, Shu-Shong Hsu, Jue-Long Wang, Chung-Ren Jan
Tetramethylpyrazine (TMP) is a compound purified from herb. Its effect on Ca(2+) concentrations ([Ca(2+) ]i ) in renal cells is unclear. This study examined whether TMP altered Ca(2+) signaling in Madin-Darby canine kidney (MDCK) cells. TMP at 100-800 μM induced [Ca(2+) ]i rises, which were reduced by Ca(2+) removal. TMP induced Mn(2+) influx implicating Ca(2+) entry. TMP-induced Ca(2+) entry was inhibited by 30% by modulators of protein kinase C (PKC) and store-operated Ca(2+) channels. Treatment with the endoplasmic reticulum Ca(2+) pump inhibitor 2,5-di-tert-butylhydroquinone (BHQ) inhibited 93% of TMP-evoked [Ca(2+) ]i rises...
June 28, 2017: Journal of Biochemical and Molecular Toxicology
https://www.readbyqxmd.com/read/28655984/bacterial-load-and-cytokine-profile-in-patients-with-cirrhosis-following-therapy-with-proton-pump-inhibitors-a-prospective-cohort-study
#9
Christos Triantos, Maria Kalafateli, Panagiota I Spantidea, Dimitrios Goukos, Efstratios Koutroumpakis, Christos Konstantakis, Stelios F Assimakopoulos, Charalambos Gogos, Athanasia Mouzaki, Georgios Daikos, Konstantinos Thomopoulos
BACKGROUND: The aim of this study was to explore the presence of bacterial products and the cytokine profile in outpatients with cirrhosis before and after short-term (4-8 weeks) administration of proton pump inhibitors (PPIs). METHODS: Seventeen patients with cirrhosis-male/female: 12/5; age: median 59.2 years (49-65); etiology: HBV±HDV 23.5%, HCV 17.7%, alcohol 41.2%, other 17.6%; Child-Pugh score: median 7.5 (5-12); Model for End-stage Liver Disease: 10.5 (7-21); ascites (%): 3 (17...
2017: Annals of Gastroenterology: Quarterly Publication of the Hellenic Society of Gastroenterology
https://www.readbyqxmd.com/read/28650638/identification-and-structure-activity-relationships-of-novel-compounds-that-potentiate-the-activities-of-antibiotics-in-escherichia-coli
#10
Keith M Haynes, Narges Abdali, Varsha Jhawar, Helen I Zgurskaya, Jerry M Parks, Adam T Green, Jerome Yves Baudry, Valentin V Rybenkov, Jeremy C Smith, John K Walker
In Gram-negative bacteria, efflux pumps are able to prevent effective cellular concentrations from being achieved for a number of antibiotics. Small molecule adjuvants that act as efflux pump inhibitors (EPIs) have the potential to reinvigorate existing antibiotics that are currently ineffective due to efflux mechanisms. Through a combination of rigorous experimental screening and in silico virtual screening we recently identified novel classes of EPIs that interact with the membrane fusion protein AcrA, a critical component of the AcrAB-TolC efflux pump in E...
June 26, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28645727/inhibition-of-non-canonical-hiv-1-tat-secretion-through-the-cellular-na-k-atpase-blocks-hiv-1-infection
#11
Silvia Agostini, Hashim Ali, Chiara Vardabasso, Antonio Fittipaldi, Ennio Tasciotti, Anna Cereseto, Antonella Bugatti, Marco Rusnati, Marina Lusic, Mauro Giacca
Besides its essential role in the activation of HIV-1 gene expression, the viral Tat protein has the unusual property of trafficking in and out of cells. In contrast to Tat internalization, the mechanism involved in extracellular Tat release has so far remained elusive. Here we show that Tat secretion occurs through a Golgi-independent pathway requiring binding of Tat with three short, non-consecutive intracytoplasmic loops at the C-terminus of the cellular Na(+),K(+)-ATPase pump alpha subunit. Ouabain, a pump inhibitor, blocked this interaction and prevented Tat secretion; virions produced in the presence of this drug were less infectious, consistent the capacity of virion-associated Tat to increase HIV-1 infectivity...
June 13, 2017: EBioMedicine
https://www.readbyqxmd.com/read/28616949/monitoring-atpase-induced-ph-changes-in-single-proteoliposomes-with-the-lipid-coupled-fluorophore-oregon-green-488
#12
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...
July 10, 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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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...
June 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
#20
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
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