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Proton pump inhibition

Mizuki Sekiya, Yu Shimoyama, Taichi Ishikawa, Minoru Sasaki, Masamitsu Futai, Mayumi Nakanishi-Matsui
Porphyromonas gingivalis is a well-known Gram-negative bacterium that causes periodontal disease. The bacterium metabolizes amino acids and peptides to obtain energy. An ion gradient across its plasma membrane is thought to be essential for nutrient import. However, it is unclear whether an ion-pumping ATPase responsible for the gradient is required for bacterial growth. Here, we report the inhibitory effect of protonophores and inhibitors of a proton-pumping ATPase on the growth of P. gingivalis. Among the compounds examined, curcumin and citreoviridin appreciably reduced the bacterial growth...
March 9, 2018: Biochemical and Biophysical Research Communications
Dinakaran Murugesan, Peter C Ray, Tracy Bayliss, Gareth A Prosser, Justin R Harrison, Kirsteen Green, Candice Soares de Melo, Tzu-Shean Feng, Leslie J Street, Kelly Chibale, Digby F Warner, Valerie Mizrahi, Ola Epemolu, Paul Scullion, Lucy Ellis, Jennifer Riley, Yoko Shishikura, Liam Ferguson, Maria Osuna-Cabello, Kevin D Read, Simon R Green, Dirk A Lamprecht, Peter M Finin, Adrie J C Steyn, Thomas R Ioerger, Jim Sacchettini, Kyu Y Rhee, Kriti Arora, Clifton E Barry Iii, Paul G Wyatt, Helena Ingrid M Boshoff
Mycobacterium tuberculosis (MTb) possesses two non-proton pumping type II NADH dehydrogenase (NDH-2) enzymes which are predicted to be jointly essential for respiratory metabolism.. Furthermore, the structure of a closely related bacterial NDH-2 has been reported recently, allowing for the structure-based design of small-molecule inhibitors. Herein, we disclose MTb whole-cell structure-activity relationships (SAR) for a series of 2-mercapto-quinazolinones which target the ndh encoded NDH-2 with nanomolar potencies...
March 9, 2018: ACS Infectious Diseases
Mohit Sharma, Smitha Sammith Shetty, Raghu Radhakrishnan
BACKGROUND: Oral submucous fibrosis is an oral potentially malignant disorder with high incidence of malignant transformation and rising global prevalence. However, the genesis of oral submucous fibrosis is still unclear despite superfluity of literature. In the background of ineffective treatment, it is necessary to decode its onset and progression before designing customized treatment regimens. OBJECTIVE: The objective of this article is to decipher the pathogenesis of oral submucous fibrosis in order to identify novel drug targets...
February 26, 2018: Recent Patents on Anti-cancer Drug Discovery
Nele Brusselaers, Lars Engstrand, Jesper Lagergren
BACKGROUND: The association of long-term use of proton pump inhibitors (PPIs) with oesophageal adenocarcinoma has been poorly defined. Our aim was to assess the risk of oesophageal cancer assessing confounding by indication. METHODS: This population-based cohort study included all 796,492 adults exposed to maintenance therapy with PPIs in Sweden in 2005-2012. Standardised incidence ratios (SIRs) and 95% confidence intervals (CIs) were calculated to assess the risk of oesophageal adenocarcinoma (and squamous cell carcinoma as a comparison) among long-term PPI users relative to the corresponding background population...
February 21, 2018: Cancer Epidemiology
Sabine Ottilie, Gregory M Goldgof, Andrea L Cheung, Jennifer L Walker, Edgar Vigil, Kenneth E Allen, Yevgeniya Antonova-Koch, Carolyn W Slayman, Yo Suzuki, Jacob D Durrant
Given that many antifungal medications are susceptible to evolved resistance, there is a need for novel drugs with unique mechanisms of action. Inhibiting the essential proton pump Pma1p, a P-type ATPase, is a potentially effective therapeutic approach that is orthogonal to existing treatments. We identify NSC11668 and hitachimycin as structurally distinct antifungals that inhibit yeast ScPma1p. These compounds provide new opportunities for drug discovery aimed at this important target.
February 20, 2018: Journal of Cheminformatics
Yu-Di Hsu, Yu-Fen Huang, Yih-Jiuan Pan, Li-Kun Huang, Ya-Yun Liao, Wei-Hua Lin, Tzu-Yin Liu, Ching-Hung Lee, Rong-Long Pan
Plant vacuolar H + -transporting inorganic pyrophosphatase (V-PPase; EC is a crucial enzyme that exists on the tonoplast to maintain pH homeostasis across the vacuolar membrane. This enzyme generates proton gradient between cytosol and vacuolar lumen by hydrolysis of a metabolic byproduct, pyrophosphate (PP i ). The regulation of V-PPase at protein level has drawn attentions of many workers for decades, but its mechanism is still unclear. In this work, we show that AVP1, the V-PPase from Arabidopsis thaliana, is a target protein for regulatory 14-3-3 proteins at the vacuolar membrane, and all twelve 14-3-3 isoforms were analyzed for their association with AVP1...
February 16, 2018: Journal of Membrane Biology
Eugene R Przespolewski, Erica S Westphal, Michelle Rainka, Nicholas M Smith, Vernice Bates, Fran M Gengo
BACKGROUND AND GOAL: Cytochrome P450 (CYP) enzymes are responsible for the conversion of clopidogrel into its active metabolite and the metabolism of proton pump inhibitors (PPIs), which may also inhibit CYP enzymes. A current Food and Drug Administration advisory suggests avoiding esomeprazole and omeprazole while taking clopidogrel because of concerns that PPIs may compromise clopidogrel's antiplatelet effects. The objective of the present study was to examine the robustness of this interaction using a well-controlled study design in a population of participants free of confounders...
February 12, 2018: Journal of Stroke and Cerebrovascular Diseases: the Official Journal of National Stroke Association
Foong Way David Tai, Mark E McAlindon
PURPOSE OF REVIEW: The review describes the effects of NSAID gastrointestinal toxicity on the small bowel, wherein injury is as prevalent as in the gastroduodenum. This is well documented by capsule endoscopy, which also provides an endoscopic endpoint for novel treatment strategies. RECENT FINDINGS: Appreciation of the prevalence of NSAID enteropathy has grown with capsule endoscopy and the use of composite end points that include obscure haemoglobin decreases in clinical studies...
February 12, 2018: Current Opinion in Gastroenterology
Naomi Uemura, Yoshikazu Kinoshita, Ken Haruma, Takashi Yao, Ryoji Kushima, Tatsuhiro Kanoo
Erosive esophagitis (EE) occurs when the epithelial mucosa is damaged due to gastric acid reflux, and the incidence of this disease is increasing in Japan due to changes in diet and lifestyle. The condition can be treated using proton pump inhibitors (PPIs) that act by irreversibly blocking the H+ ,K+ -ATPase responsible for acid secretion. Vonoprazan is a K+ competitive channel inhibitor, which reversibly and potently inhibits gastric acid secretion. However, long-term data on vonoprazan use are limited. The aim of the VISION trial is to investigate the long-term efficacy and safety of vonoprazan in comparison with the PPI lansoprazole...
2018: Clinical and Experimental Gastroenterology
Danielle Armas, Robert J Holt, Nils F Confer, Gregg C Checani, Mohammad Obaidi, Yuli Xie, Meg Brannagan
INTRODUCTION: Cystinosis is a rare, metabolic, autosomal recessive, genetic lysosomal storage disorder characterized by an accumulation of cystine in various organs and tissues. Cysteamine bitartrate (CB) is a cystine-depleting aminothiol agent approved in the United States and Europe in immediate-release and delayed-release (DR) formulations for the treatment of nephropathic cystinosis in children and adults. It is recommended that CBDR be administered with fruit juice (except grapefruit juice) for maximum absorption...
February 6, 2018: Advances in Therapy
Avinash K Nehra, Jeffrey A Alexander, Conor G Loftus, Vandana Nehra
First introduced in 1989, proton pump inhibitors (PPIs) are among the most widely utilized medications worldwide, both in the ambulatory and inpatient clinical settings. The PPIs are currently approved by the US Food and Drug Administration for the management of a variety of gastrointestinal disorders including symptomatic peptic ulcer disease, gastroesophageal reflux disease, and nonulcer dyspepsia as well as for prevention of gastrointestinal bleeding in patients receiving antiplatelet therapy. PPIs inhibit gastric acid secretion, and the most commonly associated adverse effects include abdominal pain, diarrhea, and headache...
February 2018: Mayo Clinic Proceedings
Xiao-Qing Wei, Lei Song, Xue-Song Zhang, Kui-Yang Wang, Jie Wu
RATIONALE: Aortogastric fistula (AGF) is a rare but devastating clinical complication after esophagectomy. In a recent report, nearly all AGF patients died of massive hemorrhage or aspiration of massive hematemesis. Therefore, timely appropriate treatment of AGF remains a challenge.Herein, we report a case of AGF that resulted from peptic ulceration after esophagectomy and was successfully treated with endovascular stent graft placement. PATIENT CONCERNS: A 59-year-old man had undergone video-assisted thoracoscopic esophagectomy for squamous cell carcinoma and esophageal reconstruction using a gastric tube 14 months previously...
December 2017: Medicine (Baltimore)
Yugo Hamada, Kenji Ikemura, Takuya Iwamoto, Masahiro Okuda
Lansoprazole, a proton pump inhibitor, potently inhibits human organic anion transporter, hOAT3 (SLC22A8). Lansoprazole has an asymmetric atom in its structure and is clinically administered as a racemic mixture of (R)-and (S)-enantiomers. However, little is known about the stereoselective inhibitory potencies of lansoprazole against hOAT3 and its homolog, hOAT1. In the present study, the stereoselective inhibitory effect of lansoprazole was evaluated using hOAT1-and hOAT3-expressing cultured cells. hOAT1 and hOAT3 transported [14C]p-aminohippurate and [3H]estrone-3-sulfate (ES) with Michaelis-Menten constants of 29...
January 19, 2018: Pharmacology
Kazuki Sato, Keita Miyata, Sota Ozawa, Koichi Hasegawa
The vacuolar (H+ )-ATPases (V-ATPases) are ATP-driven proton pumps with multiple functions in many organisms. In this study, we performed structural and functional analysis of vha55 gene that encodes V-ATPase subunit B in the smokybrown cockroach Periplaneta fuliginosa (Blattodea). We observed a high homology score of the deduced amino acid sequences between 10 species in seven orders. RNAi of the vha55 gene in P. fuliginosa caused nymphal/nymphal molting defects with incomplete shedding of old cuticles, growth inhibition, as well as bent and wrinkled cuticles of thoraxes and abdominal segments...
December 29, 2017: Insect Science
Megumi Takahashi, Shin Takagi
Feeding, a vital behavior in animals, is modulated depending on internal and external factors. In the nematode Caenorhabditis elegans, the feeding organ called the pharynx ingests food by pumping driven by the pharyngeal muscles. Here we report that optical silencing of the body wall muscles, which drive the locomotory movement of worms, affects pumping. In worms expressing the Arch proton pump or the ACR2 anion channel in the body wall muscle cells, the pumping rate decreases after activation of Arch or ACR2 with light illumination, and recovers gradually after terminating illumination...
December 27, 2017: PLoS Genetics
Marketa Absolonova, Mary J Beilby, Aniela Sommer, Marion C Hoepflinger, Ilse Foissner
To understand salt stress, the full impact of salinity on plant cell physiology has to be resolved. Electrical measurements suggest that salinity inhibits the proton pump and opens putative H+/OH- channels all over the cell surface of salt sensitive Chara australis (Beilby and Al Khazaaly 2009; Al Khazaaly and Beilby 2012). The channels open transiently at first, causing a characteristic noise in membrane potential difference (PD), and after longer exposure remain open with a typical current-voltage (I/V) profile, both abolished by the addition of 1 mM ZnCl2, the main known blocker of animal H+ channels...
December 15, 2017: Protoplasma
Pei Zhu, Zhan Gao, Xiao-Fang Tang, Jing-Jing Xu, Yin Zhang, Li-Jian Gao, Jue Chen, Shu-Bin Qiao, Yue-Jin Yang, Run-Lin Gao, Bo Xu, Jin-Qing Yuan
BACKGROUND: Prior studies have reported controversial conclusions regarding the risk of adverse cardiovascular events in patients using proton-pump inhibitors (PPIs) combined with clopidogrel therapy, causing much uncertainty in clinical practice. We sought to evaluate the safety of PPIs use among high-risk cardiovascular patients who underwent percutaneous coronary intervention (PCI) in a long-term follow-up study. METHODS: A total of 7868 consecutive patients who had undergone PCI and received dual antiplatelet therapy (DAPT) at a single center from January 2013 to December 2013 were enrolled...
December 20, 2017: Chinese Medical Journal
R Ruiter, H F Wunderink, R A Veenendaal, L G Visser, M G J de Boer
Helicobacter pylori infection is clinically associated with dyspepsia, gastric and duodenal ulcers, and gastric cancer. Increasing antimicrobial resistance in H. pylori is a worldwide problem and failure of eradication with standard triple therapy (high-dose proton pump inhibition, amoxicillin and clarithromycin) is directly related to the presence of a resistant strain. Other treatment combinations have been investigated, but with inconsistent results. Based on a review of the recent literature in conjunction with an analysis of the regional resistance data, we address the increasing complexity of H...
November 2017: Netherlands Journal of Medicine
Ewa Żesławska, Wojciech Nitek, Jadwiga Handzlik
The 2-amine derivatives of 5-arylidene-3H-imidazol-4(5H)-one are a new class of bacterial efflux pump inhibitors, the chemical compounds that are able to restore antibiotic efficacy against multidrug resistant bacteria. 5-Arylidene-3H-imidazol-4(5H)-ones with a piperazine ring at position 2 reverse the mechanisms of multidrug resistance (MDR) of the particularly dangerous Gram-negative bacteria E. coli by inhibition of the efflux pump AcrA/AcrB/TolC (a main multidrug resistance mechanism in Gram-negative bacteria, consisting of a membrane fusion protein, AcrA, a Resistant-Nodulation-Division protein, AcrB, and an outer membrane factor, TolC)...
December 1, 2017: Acta Crystallographica. Section C, Structural Chemistry
Vijay K Samineni, Aaron D Mickle, Jangyeol Yoon, Jose G Grajales-Reyes, Melanie Y Pullen, Kaitlyn E Crawford, Kyung Nim Noh, Graydon B Gereau, Sherri K Vogt, H Henry Lai, John A Rogers, Robert W Gereau
Patients with interstitial cystitis/bladder pain syndrome (IC/BPS) suffer from chronic pain that severely affects quality of life. Although the underlying pathophysiology is not well understood, inhibition of bladder sensory afferents temporarily relieves pain. Here, we explored the possibility that optogenetic inhibition of nociceptive sensory afferents could be used to modulate bladder pain. The light-activated inhibitory proton pump Archaerhodopsin (Arch) was expressed under control of the sensory neuron-specific sodium channel (sns) gene to selectively silence these neurons...
November 20, 2017: Scientific Reports
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