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Proton pump inhibition

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https://www.readbyqxmd.com/read/29139202/lego-inspired-drug-design-unveiling-of-the-novel-class-of-benzo-d-thiazole-containing-a-3-4-dihydroxyphenyl-moiety-as-plasma-membrane-h-atpase-inhibitors
#1
Truong Thanh Tung, Dao Trong Tuan, Marta Grifell Junyent, Michael Palmgren, Thomas Günther-Pomorski, Anja Thoe Fuglsang, Søren Brøgger Christensen, John Nielsen
The fungal plasma membrane H+-ATPase (Pma1p) is a potential target for the discovery of new antifungal agents. Surprisingly, no structure-activity relationship studies for small molecules targeting Pma1p have been reported. Herein, we disclose a LEGO-inspired fragment assembly strategy for design, synthesis and discovery of benzo[d]thiazoles containing a 3,4-dihydroxyphenyl moiety as potential Pma1p inhibitors. A series of 2-(benzo[d]thiazol-2-ylthio)-1-(3,4-dihydroxyphenyl)ethanones was found to inhibit Pma1p with the most potent IC50 of 8 µM in an in vitro plasma membrane H+-ATPase assay...
November 15, 2017: ChemMedChem
https://www.readbyqxmd.com/read/29105152/proton-pump-inhibitor-alters-oral-microbiome-in-gastrointestinal-tract-of-healthy-volunteers
#2
Tsuyoshi Mishiro, Kentaro Oka, Yasutoshi Kuroki, Motomichi Takahashi, Kasumi Tatsumi, Tsukasa Saitoh, Hiroshi Tobita, Norihisa Ishimura, Shuichi Sato, Shunji Ishihara, Joji Sekine, Koichiro Wada, Yoshikazu Kinoshita
BACKGROUND AND AIM: Acid suppressive agents including proton pump inhibitors (PPIs) are used as first-line treatment for various acid-related gastrointestinal disorders. Although known to profoundly reduce gastric acid production, their influence on inhibition of acid secretion as part of the function of the gastrointestinal tract microbiome remains to be elucidated. The aim of the present study was to examine the effects of PPI usage on oral and gut microbiota in healthy volunteers. METHODS: Ten healthy adult volunteers receiving no medications were enrolled...
November 4, 2017: Journal of Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/29070456/-characterization-of-chromate-resistance-in-genetically-engineered-escherichia-coli-expressing-chromate-ion-transporter-chra
#3
Si-Min Zhou, Lan-Lan Dong, Yuan He, Hong Xiao
OBJECTIVE: To construct a genetically engineered Escherichia coli expressing chromate (Cr) ion transporter ChrA and test its Cr resistance capacity. METHODS: ChrA gene was cloned by PCR from the DNA template of Serratia sp. S2 and linked with the prokaryotic vector pET-28a (+). The recombinant vector was transformed into E.coli BL21 (DE3) cells for expression of ChrA protein. Cr (VI) risistance and Cr (VI) uptake and efflux of the engineered bacteria were tested, and the effects of Cr loading time, oxyanions (ulfate, molybdate, vanadate, tungstate), and respiratory inhibitors (valinomycin, CN(-), oligomycin, and NADH) on Cr (VI) efflux were examined to analyze the pathway of Cr (VI) transport by ChrA protein...
October 20, 2017: Nan Fang Yi Ke da Xue Xue Bao, Journal of Southern Medical University
https://www.readbyqxmd.com/read/29060457/a-pharmacokinetic-model-of-drug-drug-interaction-between-clopidogrel-and-omeprazole-at-cyp2c19-in-humans
#4
Wimonchat Tangamornsuksan, Pongpak Thiansupornpong, Thirawut Morasuk, Ornrat Lohitnavy, Manupat Lohitnavy
BACKGROUND: Clopidogrel is a thienopryridine antiplatelet agent commonly used in the management of cardiovascular diseases. Clopidogrel is metabolized by hepatic CYP2C19 and CYP2B6, therefore, co-administration of clopidogrel and CYP2C19 inhibitors can alter pharmacokinetics of clopidogrel. Omeprazole is a proton pump inhibitor used for decreasing gastric acid production. Omeprazole is known to be a potent inhibitor of CYP2C19. Thus when the drugs are simultaneously administered, clopidogrel plasma concentration levels can be increased...
July 2017: Conference Proceedings: Annual International Conference of the IEEE Engineering in Medicine and Biology Society
https://www.readbyqxmd.com/read/29055186/designed-inhibitors-with-hetero-linkers-for-gastric-proton-pump-h-k-atpase-steered-molecular-dynamics-and-metadynamics-studies
#5
Kalyanashis Jana, Tusar Bandyopadhyay, Bishwajit Ganguly
Acid suppressant SCH28080 and its derivatives reversibly reduce acid secretion activity of the H(+),K(+)-ATPase in a K(+) competitive manner. The results on homologation of the SCH28080 by varying the linker chain length suggested the improvement in efficacy. However, the pharmacokinetic studies reveal that the hydrophobic nature of the CH2 linker units may not help it to function as a better acid suppressant. We have exploited the role of linker unit to enhance the efficacy of such reversible acid suppressant drug molecules using hetero linker, i...
October 12, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/29043071/recent-advances-in-the-management-of-peptic-ulcer-bleeding
#6
REVIEW
Ian Beales
Acute upper gastrointestinal haemorrhage due to peptic ulcer bleeding remains an important cause of emergency presentation and hospital admission. Despite advances in many aspects of management, peptic ulcer bleeding is still associated with significant morbidity, mortality, and healthcare costs. Comprehensive international guidelines have been published, but advances as well as controversies continue to evolve. Important recent advances include the evidence supporting a more restrictive transfusion strategy aiming for a target haemoglobin of 70-90 g/l...
2017: F1000Research
https://www.readbyqxmd.com/read/29038303/f-actin-reorganization-by-v-atpase-inhibition-in-prostate-cancer
#7
Yamhilette Licon-Munoz, Vera Michel, Colleen A Fordyce, Karlett J Parra
The vacuolar ATPase (V-ATPase) proton pump sustains cellular pH homeostasis, and its inhibition triggers numerous stress responses. However, the cellular mechanisms involved remain largely elusive in cancer cells. We studied V-ATPase in the prostate cancer (PCa) cell line PC-3, which has characteristics of highly metastatic PCa. V-ATPase inhibitors impaired endo-lysosomal pH, vesicle trafficking, migration, and invasion. V-ATPase accrual in the Golgi and recycling endosomes suggests that traffic of internalized membrane vesicles back to the plasma membrane was particularly impaired...
November 15, 2017: Biology Open
https://www.readbyqxmd.com/read/29018343/impact-of-gastric-h-k-atpase-rs2733743-on-the-intragastric-ph-values-of-dexlansoprazole-injection-in-chinese-subjects
#8
Lu-Ning Sun, Yang Cao, Yue-Qi Li, Yun-Qian Fang, Hong-Wen Zhang, Mei-Feng Wang, Li-Jun Xie, Juan Chen, Zhi-Cheng Yang, Ming-Liang Bian, Hao Li, Pei-Pei Zhang, Ji-Fu Wei, Ling Meng, Xue-Hui Zhang, Ping Zhao, Yong-Qing Wang
Background: Not all patients with acid-related disorders receiving proton pump inhibitor (PP) treatment get adequate gastric pH control. The genetic variation of receptors, metabolic enzymes, and transporters are known to cause failures of therapies. We have conducted a study to evaluate the influence of gastric H(+)/K(+)-ATPase, CYP2C19, and ABCB1 polymorphisms on the pharmacokinetic and pharmacodynamic profiles of dexlansoprazole injection in healthy Chinese subjects. Methods: A total of 51 subjects were enrolled for pharmacokinetic and pharmacodynamic study after a single intravenous administration of 20 or 30 mg dexlansoprazole...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28979813/tumor-microenvironment-interruption-a-novel-anti-cancer-mechanism-of-proton-pump-inhibitor-in-gastric-cancer-by-suppressing-the-release-of-microrna-carrying-exosomes
#9
Xu-Wen Guan, Fang Zhao, Jing-Ya Wang, Hai-Yan Wang, Shao-Hua Ge, Xia Wang, Le Zhang, Rui Liu, Yi Ba, Hong-Li Li, Ting Deng, Li-Kun Zhou, Ming Bai, Tao Ning, Hai-Yang Zhang, Ding-Zhi Huang
Poor prognosis of gastric cancer is related to not only malignancy of gastric cancer cells, but also the tumor microenvironment. Thus drugs, which can inhibit both of them, are urgently needed to be explored. Studies on effect of Proton-pump inhibitors (PPIs) in anti-neoplasms are increasing, but is rare in gastric in gastric cancer. Here we investigated how the gastric cancer microenvironment is regulated by PPIs. The objective response rate of gastric cancer patients in our hospital treated by PPIs is investigated...
2017: American Journal of Cancer Research
https://www.readbyqxmd.com/read/28978047/restoring-microenvironmental-redox-and-ph-homeostasis-inhibits-neoplastic-cell-growth-and-migration-therapeutic-efficacy-of-esomeprazole-plus-sulfasalazine-on-3-mca-induced-sarcoma
#10
Enrica Balza, Patrizia Castellani, Paola Sanchez Moreno, Patrizia Piccioli, Iria Medraño-Fernandez, Claudia Semino, Anna Rubartelli
Neoplastic cells live in a stressful context and survive thanks to their ability to overcome stress. Thus, tumor cell responses to stress are potential therapeutic targets. We selected two such responses in melanoma and sarcoma cells: the xc- antioxidant system, that opposes oxidative stress, and surface v-ATPases that counteract the low pHi by extruding protons, and targeted them with the xc- blocker sulfasalazine and the proton pump inhibitor esomeprazole. Sulfasalazine inhibited the cystine/cysteine redox cycle and esomeprazole decreased pHi while increasing pHe in tumor cell lines...
September 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28968600/the-h-k-atpase-inhibitor-sch-28080-inhibits-insulin-secretion-and-induces-cell-death-in-ins-1e-rat-insulinoma-cells
#11
Martin Jakab, Nina Ketterl, Johannes Fürst, Marlena Beyreis, Michael Kittl, Tobias Kiesslich, Cornelia Hauser-Kronberger, Martin Gaisberger, Markus Ritter
BACKGROUND/AIMS: Glucose-stimulated insulin secretion (GSIS) of pancreatic β-cells involves glucose uptake and metabolism, closure of KATP channels and depolarization of the cell membrane potential (Vmem), activation of voltage-activated Ca2+ currents (ICav) and influx of Ca2+, which eventually triggers hormone exocytosis. Beside this classical pathway, KATP-independent mechanisms such as changes in intracellular pH (pHi) or cell volume, which also affect β-cell viability, can elicit or modify insulin release...
October 2, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28938598/proton-pump-inhibitors-increase-the-chemosensitivity-of-patients-with-advanced-colorectal-cancer
#12
Xiaoyu Wang, Chun Liu, Jiaqi Wang, Yue Fan, Zhenghua Wang, Yuanyuan Wang
Changes in pH can alter the uptake of chemotherapy drugs. Proton pump inhibitors (PPIs) may therefore increase the chemosensitivity of cancer cells and cytotoxicity of chemotherapeutic drugs by increasing their uptake. We investigated the chemosensitizing potential of PPIs in colorectal cancer (CRC). Our in vitro data show that the PPI pantoprazole increases the chemosensitivity of CRC HT29 and RKO cells to fluorouracil (5-FU). Our in vivo data demonstrate that pantoprazole also increases the ability of 5-FU to inhibit CRC tumor growth in mice...
August 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/28937021/optimized-high-dose-amoxicillin-proton-pump-inhibitor-dual-therapies-fail-to-achieve-high-cure-rates-in-china
#13
Jia-Li Hu, Jun Yang, Yin-Bin Zhou, Ping Li, Ran Han, Dian-Chun Fang
Background\Aim: Quadruple daily administration of proton-pump inhibitor (PPI) therapy achieves potent acid inhibition, and combined with amoxicillin, with its pharmacodynamic and pharmacokinetic characteristics, may be efficient for Helicobacter pylori eradication. We compared the efficacy of two optimized high-dose dual therapies with a bismuth-containing quadruple regimen for treating H. pylori infection. Rabeprazole dosages for H. pylori eradication were also evaluated. PATIENTS AND METHODS: Treatment-naive and H...
September 2017: Saudi Journal of Gastroenterology: Official Journal of the Saudi Gastroenterology Association
https://www.readbyqxmd.com/read/28926955/identification-of-novel-bisbenzimidazole-derivatives-as-anticancer-vacuolar-h%C3%A2-%C2%BA-atpase-inhibitors
#14
Renukadevi Patil, Arpita Kulshrestha, Anjali Tikoo, Sara Fleetwood, Gajendra Katara, Bala Kolli, William Seibel, Alice Gilman-Sachs, Shivaputra A Patil, Kenneth D Beaman
The vacuolar (H⁺)-ATPases (V-ATPases) are a family of ATP-driven proton pumps and they have been associated with cancer invasion, metastasis, and drug resistance. Despite the clear involvement of V-ATPases in cancer, the therapeutic use of V-ATPase-targeting small molecules has not reached human clinical trials to date. Thus, V-ATPases are emerging as important targets for the identification of potential novel therapeutic agents. We identified a bisbenzimidazole derivative (V) as an initial hit from a similarity search using four known V-ATPase inhibitors (I-IV)...
September 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28911053/co-ordination-of-ndh-and-cup-proteins-in-co2-uptake-in-cyanobacterium-synechocystis-sp-pcc-6803
#15
Xunling Han, Nan Sun, Min Xu, Hualing Mi
High and low affinity CO2-uptake systems containing CupA (NDH-1MS) and CupB (NDH-1MS'), respectively, have been identified in Synechocystis sp. PCC 6803, but it is yet unknown how the complexes function in CO2 uptake. In this work, we found that deletion of cupB significantly lowered the growth of cells, and deletion of both cupA and cupB seriously suppressed the growth below pH 7.0 even under 3% CO2. The rate of photosynthetic oxygen evolution was decreased slightly by deletion of cupA but significantly by deletion of cupB and more severely by deletion of both cupA and cupB, especially in response to changed pH conditions under 3% CO2...
June 1, 2017: Journal of Experimental Botany
https://www.readbyqxmd.com/read/28902909/the-cytoprotective-protein-clusterin-is-overexpressed-in-hypergastrinemic-rodent-models-of-oxyntic-preneoplasia-and-promotes-gastric-cancer-cell-survival
#16
Pål Vange, Torunn Bruland, Berit Doseth, Reidar Fossmark, Mirta M L Sousa, Vidar Beisvag, Øystein Sørdal, Gunnar Qvigstad, Helge L Waldum, Arne K Sandvik, Ingunn Bakke
The cytoprotective protein clusterin is often dysregulated during tumorigenesis, and in the stomach, upregulation of clusterin marks emergence of the oxyntic atrophy (loss of acid-producing parietal cells)-associated spasmolytic polypeptide-expressing metaplasia (SPEM). The hormone gastrin is important for normal function and maturation of the gastric oxyntic mucosa and hypergastrinemia might be involved in gastric carcinogenesis. Gastrin induces expression of clusterin in adenocarcinoma cells. In the present study, we examined the expression patterns and gastrin-mediated regulation of clusterin in gastric tissue from: humans; rats treated with proton pump (H+/K+-ATPase) inhibitors and/or a gastrin receptor (CCK2R) antagonist; H+/K+-ATPase β-subunit knockout (H/K-β KO) mice; and Mongolian gerbils infected with Helicobacter pylori and given a CCK2R antagonist...
2017: PloS One
https://www.readbyqxmd.com/read/28894571/vonoprazan-10-mg-daily-is-effective-for-the-treatment-of-patients-with-proton-pump-inhibitor-resistant-gastroesophageal-reflux-disease
#17
Satoshi Shinozaki, Hiroyuki Osawa, Yoshikazu Hayashi, Hirotsugu Sakamoto, Yasutoshi Kobayashi, Alan Kawarai Lefor, Hironori Yamamoto
Gastroesophageal reflux disease (GERD) is commonly treated by primary care physicians. Although proton pump inhibitors (PPI) have been the mainstay of GERD treatment for two decades, in some patients GERD is refractory to standard dose PPI for more than eight weeks and is referred to as PPI-resistant GERD. Vonoprazan, a novel competitive acid blocker, became available in Japan for the treatment of patients with GERD, and has greater acid inhibition than existing PPIs. The aim of the present study was to determine the effect of vonoprazan 10 mg daily on PPI-resistant GERD...
September 2017: Biomedical Reports
https://www.readbyqxmd.com/read/28880991/a-comparison-of-alkaline-water-and-mediterranean-diet-vs-proton-pump-inhibition-for-treatment-of-laryngopharyngeal-reflux
#18
COMPARATIVE STUDY
Craig H Zalvan, Shirley Hu, Barbara Greenberg, Jan Geliebter
Importance: Laryngopharyngeal reflux (LPR) is a common disorder with protean manifestations in the head and neck. In this retrospective study, we report the efficacy of a wholly dietary approach using alkaline water, a plant-based, Mediterranean-style diet, and standard reflux precautions compared with that of the traditional treatment approach of proton pump inhibition (PPI) and standard reflux precautions. Objective: To determine whether treatment with a diet-based approach with standard reflux precautions alone can improve symptoms of LPR compared with treatment with PPI and standard reflux precautions...
October 1, 2017: JAMA Otolaryngology—Head & Neck Surgery
https://www.readbyqxmd.com/read/28866861/effects-of-the-proton-pump-inhibitors-omeprazole-and-pantoprazole-on-the-cytochrome-p450-mediated-metabolism-of-venlafaxine
#19
Maxim Kuzin, Georgios Schoretsanitis, Ekkehard Haen, Benedikt Stegmann, Christoph Hiemke, Gerhard Gründer, Michael Paulzen
BACKGROUND AND OBJECTIVE: An increasing trend in prescribing proton pump inhibitors (PPIs) inevitably increases the risk of unwanted drug-drug interactions (DDIs). The aim of this study was to uncover pharmacokinetic interactions between two PPIs-omeprazole and pantoprazole-and venlafaxine. METHODS: A therapeutic drug monitoring database contained plasma concentrations of venlafaxine and its active metabolite O-desmethylvenlafaxine. We considered three groups: a group of patients who received venlafaxine without confounding medications (non-PPI group, n = 906); a group of patients who were comedicated with omeprazole (n = 40); and a group of patients comedicated with pantoprazole (n = 40)...
September 2, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28861639/repositioning-of-proton-pump-inhibitors-in-cancer-therapy
#20
REVIEW
Zhen-Ning Lu, Bing Tian, Xiu-Li Guo
Drug repositioning, as a smart way to exploit new molecular targets of a known drug, has been gaining increasing attention in the discovery of anti-cancer drugs. Proton pump inhibitors (PPIs) as benzimidazole derivatives, which are essentially H(+)-K(+)-ATPases inhibitors, are commonly used in the treatment of acid-related diseases such as gastric ulcer. In recent years, exploring the new application of PPIs in anti-cancer field has become a hot research topic. Interestingly, cancer cells display an alkaline intracellular pH and an acidic extracellular pH...
August 31, 2017: Cancer Chemotherapy and Pharmacology
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