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Protein pump inhibitor

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https://www.readbyqxmd.com/read/29665355/combination-therapy-with-polydeoxyribonucleotide-and-proton-pump-inhibitor-enhances-therapeutic-effectiveness-for-gastric-ulcer-in-rats
#1
Il-Gyu Ko, Sung-Eun Kim, Jun-Jang Jin, Lakkyong Hwang, Eun-Sang Ji, Chang-Ju Kim, Jin-Hee Han, In Taik Hong, Min Seop Kwak, Jin Young Yoon, Hyun Phil Shin, Jung Won Jeon
AIMS: The main action of proton pump inhibitors (PPIs) is to inhibit gastric acid secretion, and PPIs are widely used to treat gastric ulcer (GU). However, if the action of promoting gastric mucosal regeneration is added, the effectiveness of GU treatment can be enhanced. Thus, in order to improve the therapeutic effect on GU, we tried to develop combination therapy promoting regeneration in injured tissue besides suppressing gastric acid secretion. MAIN METHODS: Polydeoxyribonucleotide (PDRN) was selected to evaluate tissue regeneration, and pantoprazole was chosen as one of the PPIs...
April 14, 2018: Life Sciences
https://www.readbyqxmd.com/read/29649588/characterization-of-oxa-258-enzymes-and-axyabm-efflux-pump-from-achromobacter-ruhlandii
#2
Mariana Papalia, Germán Traglia, Melina Ruggiero, Marisa Almuzara, Carlos Vay, Gabriel Gutkind, Soledad María Ramírez, Marcela Radice
OBJECTIVES: The aim of this study was to characterize OXA-258 variants and other features that may contribute to the carbapenem resistant in Achromobacter ruhlandii. METHODS: Kinetic parameters for purified OXA-258a and OXA-258b were determined measuring the rate of hydrolysis of a representative group of antibiotics. Whole-genome shotgun sequencing was performed on A. ruhlandii 38 (producing OXA-258a) and A. ruhlandii 319 (producing OXA-258b) and in silico analysis of antimicrobial resistant determinants was conducted...
April 9, 2018: Journal of Global Antimicrobial Resistance
https://www.readbyqxmd.com/read/29605625/activation-of-soluble-guanylyl-cyclase-with-inhibition-of-multidrug-resistance-protein-inhibitor-4-mrp4-as-a-new-antiplatelet-therapy
#3
Camila B Mendes-Silverio, Caroline H Lescano, Tiago Zaminelli, Carolina Sollon, Gabriel F Anhê, Edson Antunes, Fabíola Z Mónica
The intracellular levels of cyclic GMP are controlled by its rate of formation through nitric oxide-mediated stimulation of soluble guanylate cyclase (sGC) and its degradation by phosphodiesterases. Multidrug resistance protein 4 (MRP4) expressed in human platelets pumps cyclic nucleotides out of cells. In search for new antiplatelet strategies, we tested the hypothesis that sGC activation concomitant with MRP4 inhibition confers higher antiplatelet efficacy compared with monotherapy alone. This study was undertaken to investigate the pharmacological association of the sGC activator BAY 60-2770 with the MRP4 inhibitor MK571 on human washed platelets...
March 29, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29599904/targeting-multidrug-resistant-ovarian-cancer-through-estrogen-receptor-%C3%AE-dependent-atp-depletion-caused-by-hyperactivation-of-the-unfolded-protein-response
#4
Xiaobin Zheng, Neal Andruska, Michael J Lambrecht, Sisi He, Amadeo Parissenti, Paul J Hergenrother, Erik R Nelson, David J Shapiro
Ovarian cancers often recur and tumors acquire resistance to chemotherapy due to overexpression of the ATP-dependent efflux pump, multidrug resistance protein 1 (MDR1/P-glycoprotein/ABCB1). Nontoxic small molecule inhibitors targeting MDR1 have remained largely elusive. Instead, in a novel application of our recently described estrogen receptor α (ERα) biomodulator, BHPI, we targeted MDR1's substrate, ATP. BHPI depletes intracellular ATP and nearly blocks MDR1-mediated drug efflux in ovarian cancer cells by inducing toxic hyperactivation of the endoplasmic reticulum stress sensor, the unfolded protein response (UPR)...
March 13, 2018: Oncotarget
https://www.readbyqxmd.com/read/29584668/atp-binding-cassette-transporter-vcam-from-vibrio-cholerae-is-dependent-on-the-outer-membrane-factor-family-for-its-function
#5
Wen-Jung Lu, Hsuan-Ju Lin, Thamarai K Janganan, Cheng-Yi Li, Wei-Chiang Chin, Vassiliy N Bavro, Hong-Ting Victor Lin
Vibrio cholerae ATP-binding cassette transporter VcaM ( V. cholerae ABC multidrug resistance pump) has previously been shown to confer resistance to a variety of medically important drugs. In this study, we set to analyse its properties both in vitro in detergent-solubilised state and in vivo to differentiate its dependency on auxiliary proteins for its function. We report the first detailed kinetic parameters of purified VcaM and the rate of phosphate (Pi) production. To determine the possible functional dependencies of VcaM on the tripartite efflux pumps we then utilized different E...
March 27, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29567836/histone-deacetylase-mediated-regulation-of-endolysosomal-ph
#6
Hari Prasad, Rajini Rao
The pH of the endolysosomal system is tightly regulated by a balance of proton pump and leak mechanisms that are critical for storage, recycling, turnover, and signaling functions in the cell. Dysregulation of endolysosomal pH has been linked to aging, amyloidogenesis, synaptic dysfunction, and various neurodegenerative disorders, including Alzheimer's disease. Therefore, understanding the mechanisms that regulate luminal pH may be key to identifying new targets for managing these disorders. Metaanalysis of yeast microarray databases revealed that nutrient limiting conditions inhibited the histone deacetylase (HDAC) Rpd3 and thereby upregulated transcription of the endosomal Na+ /H+ exchanger Nhx1, resulting in vacuolar alkalinization...
March 22, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29524504/pharmacological-inhibition-of-sumo-1-with-ginkgolic-acid-alleviates-cardiac-fibrosis-induced-by-myocardial-infarction-in-mice
#7
Fang Qiu, Changjiang Dong, Yanxin Liu, Xiaoqi Shao, Di Huang, Yanna Han, Bing Wang, Yanli Liu, Rong Huo, Petro Paulo, Zhiren Zhang, Dan Zhao, Wen-Feng Chu
BACKGROUND AND PURPOSE: Protein modification by small ubiquitin-like modifier (SUMO) plays a critical role in the pathogenesis of heart diseases. The present study was designed to determine whether ginkgolic acid (GA) as a SUMO-1 inhibitor exerts an inhibitory effect on cardiac fibrosis induced by myocardial infarction (MI). EXPERIMENTAL APPROACH: GA was delivered by osmotic pumps in MI mice. Masson staining, electron microscopy (EM) and echocardiography were used to assess cardiac fibrosis, ultrastructure and function...
March 7, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29522317/2-mercapto-quinazolinones-as-inhibitors-of-ndh-2-and-mycobacterium-tuberculosis-structure-activity-relationships-mechanism-of-action-and-adme-characterization
#8
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
https://www.readbyqxmd.com/read/29515774/unbiased-compound-protein-interface-mapping-and-prediction-of-chemoresistance-loci-through-forward-genetics-in-haploid-stem-cells
#9
Moritz Horn, Virginia Kroef, Kira Allmeroth, Nicole Schuller, Stephan Miethe, Martin Peifer, Josef M Penninger, Ulrich Elling, Martin S Denzel
Forward genetic screens in haploid mammalian cells have recently emerged as powerful tools for the discovery and investigation of recessive traits. Use of the haploid system provides unique genetic tractability and resolution. Upon positive selection, these screens typically employ analysis of loss-of-function (LOF) alleles and are thus limited to non-essential genes. Many relevant compounds, including anti-cancer therapeutics, however, target essential genes, precluding positive selection of LOF alleles. Here, we asked whether the use of random and saturating chemical mutagenesis might enable screens that identify essential biological targets of toxic compounds...
February 9, 2018: Oncotarget
https://www.readbyqxmd.com/read/29488678/monotherapy-with-a-novel-intervenolin-derivative-as-1934-is-an-effective-treatment-for-helicobacter-pylori-infection
#10
Tomokazu Ohishi, Tohru Masuda, Hikaru Abe, Chigusa Hayashi, Hayamitsu Adachi, Shun-Ichi Ohba, Masayuki Igarashi, Takumi Watanabe, Hitomi Mimuro, Eri Amalia, Daniel Ken Inaoka, Kota Mochizuki, Kiyoshi Kita, Masakatsu Shibasaki, Manabu Kawada
BACKGROUND: Helicobacter pylori (H. pylori) infection causes various gastrointestinal diseases including gastric cancer. Hence, eradication of this infection could prevent these diseases. The most popular first-line treatment protocol to eradicate H. pylori is termed "triple therapy" and consists of a proton pump inhibitor (PPI), clarithromycin, and amoxicillin or metronidazole. However, the antibiotics used to treat H. pylori infection are hindered by the antibiotics-resistant bacteria and by their antimicrobial activity against intestinal bacteria, leading to side effects...
February 28, 2018: Helicobacter
https://www.readbyqxmd.com/read/29485009/oral-submucous-fibrosis-as-an-overhealing-wound-implications-in-malignant-transformation
#11
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
https://www.readbyqxmd.com/read/29484528/variable-cell-line-pharmacokinetics-contribute-to-non-linear-treatment-response-in-heterogeneous-cell-populations
#12
Matthew T McKenna, Jared A Weis, Vito Quaranta, Thomas E Yankeelov
We develop a combined experimental-mathematical framework to investigate heterogeneity in the context of breast cancer treated with doxorubicin. We engineer a cell line to over-express the multi-drug resistance 1 protein (MDR1), an ATP-dependent pump that effluxes intracellular drug. Co-culture experiments mixing the MDR1-overexpressing line with its parental line are evaluated via fluorescence microscopy. To quantify the impact of population heterogeneity on therapy response, these data are analyzed with a coupled pharmacokinetics/pharmacodynamics model...
February 26, 2018: Annals of Biomedical Engineering
https://www.readbyqxmd.com/read/29471192/the-effect-of-magnolol-on-ca-2-homeostasis-and-its-related-physiology-in-human-oral-cancer-cells
#13
Shu-Feng Hsieh, Chiang-Ting Chou, Wei-Zhe Liang, Chun-Chi Kuo, Jue-Long Wang, Lyh-Jyh Hao, Chung-Ren Jan
OBJECTIVE: Magnolol, a polyphenol compound from herbal medicines, was shown to alter physiology in various cell models. However, the effect of magnolol on Ca2+ homeostasis and its related physiology in oral cancer cells is unclear. This study examined whether magnolol altered Ca2+ signaling and cell viability in OC2 human oral cancer cells. METHODS: Cytosolic Ca2+ concentrations ([Ca2+ ]i ) in suspended cells were measured by using the fluorescent Ca2+ -sensitive dye fura-2...
February 14, 2018: Archives of Oral Biology
https://www.readbyqxmd.com/read/29467212/intravital-multiphoton-microscopy-with-fluorescent-bile-salts-in-rats-as-an-in-vivo-biomarker-for-hepatobiliary-transport-inhibition
#14
Jennifer Ryan, Ryan E Morgan, Yuan Chen, Laurie Volak, Robert T Dunn, Kenneth W Dunn
The bile salt export pump (BSEP) is expressed at the canalicular domain of hepatocytes, where it mediates the elimination of monovalent bile salts into the bile. Inhibition of BSEP is considered a susceptibility factor for drug-induced liver injury (DILI) that often goes undetected during non-clinical testing. Although in vitro assays exist for screening BSEP inhibition, a reliable and specific method for confirming Bsep inhibition in vivo would be a valuable follow-up to a BSEP screening strategy, helping to put a translatable context around in vitro inhibition data, incorporating processes such as metabolism, protein binding, and other exposure properties that are lacking in most in vitro BSEP models...
February 21, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29463871/co-treatment-with-clonidine-and-a-grk2-inhibitor-prevented-rebound-hypertension-and-endothelial-dysfunction-after-withdrawal-in-diabetes
#15
Kumiko Taguchi, Nanami Bessho, Mami Hasegawa, Haruka Narimatsu, Takayuki Matsumoto, Tsuneo Kobayashi
Hypertension and diabetes are associated with a risk of cardiovascular disease. Clonidine is currently used as a fourth-line drug therapy for hypertension because of its rebound hypertensive effect and short half-life. The purpose of this study was to investigate the combined effect of an antihypertensive drug (clonidine) and a G-protein-coupled receptor kinase 2 (GRK2) inhibitor on rebound hypertension and endothelial dysfunction. The clonidine and/or GRK2 inhibitor were administered by continuous infusion for 14 days by using an osmotic pump that was implanted subcutaneously...
February 20, 2018: Hypertension Research: Official Journal of the Japanese Society of Hypertension
https://www.readbyqxmd.com/read/29463314/functional-brain-specific-microvessels-from-ipsc-derived-human-brain-microvascular-endothelial-cells-the-role-of-matrix-composition-on-monolayer-formation
#16
Moriah E Katt, Raleigh M Linville, Lakyn N Mayo, Zinnia S Xu, Peter C Searson
BACKGROUND: Transwell-based models of the blood-brain barrier (BBB) incorporating monolayers of human brain microvascular endothelial cells (dhBMECs) derived from induced pluripotent stem cells show many of the key features of the BBB, including expression of transporters and efflux pumps, expression of tight junction proteins, and physiological values of transendothelial electrical resistance. The fabrication of 3D BBB models using dhBMECs has so far been unsuccessful due to the poor adhesion and survival of these cells on matrix materials commonly used in tissue engineering...
February 20, 2018: Fluids and Barriers of the CNS
https://www.readbyqxmd.com/read/29462315/overexpression-of-stenotrophomonas-maltophilia-major-facilitator-superfamily-protein-mfsa-increases-resistance-to-fluoroquinolone-antibiotics
#17
Paiboon Vattanaviboon, Punyawee Dulyayangkul, Skorn Mongkolsuk, Nisanart Charoenlap
Background: Stenotrophomonas maltophilia is an opportunistic human pathogen causing nosocomial infections worldwide. S. maltophilia infection is of particular concern due to its inherent resistance to currently used antibiotics. Proton motive force-driven transporters of the major facilitator superfamily frequently contribute to the efflux of substances, including antibiotics, across cell membranes. Methods: An mfsA expression plasmid (pMfsA) was constructed and transferred into bacterial strains by electroporation...
February 14, 2018: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29453043/understanding-of-human-atp-binding-cassette-superfamily-and-novel-multidrug-resistance-modulators-to-overcome-mdr
#18
REVIEW
Imran Shair Mohammad, Wei He, Lifang Yin
Indeed, multi-drug resistance (MDR) is a significant obstacle to effective chemotherapy. The overexpression of ATP-binding cassette (ABC) membrane transporters is a principal cause of enhanced cytotoxic drug efflux and treatment failure in various types of cancers. At cellular level, the pumps of ABC family regulate the transportation of numerous substances including drugs in and out of the cells. In past, the overexpression of ABC pumps suggested a well-known mechanism of drug resistance in cancers as well as infectious diseases...
February 13, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29452094/evolving-mechanisms-of-vascular-smooth-muscle-contraction-highlight-key-targets-in-vascular-disease
#19
REVIEW
Zhongwei Liu, Raouf A Khalil
Vascular smooth muscle (VSM) plays an important role in the regulation of vascular function. Identifying the mechanisms of VSM contraction has been a major research goal in order to determine the causes of vascular dysfunction and exaggerated vasoconstriction in vascular disease. Major discoveries over several decades have helped to better understand the mechanisms of VSM contraction. Ca 2+ has been established as a major regulator of VSM contraction, and its sources, cytosolic levels, homeostatic mechanisms and subcellular distribution have been defined...
February 13, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29428471/efficacy-of-constant-long-term-delivery-of-ym-58483-for-the-treatment-of-rheumatoid-arthritis
#20
Maya Miyoshi, Shuang Liu, Asuka Morizane, Erika Takemasa, Yashuyuki Suzuki, Takeshi Kiyoi, Kazutaka Maeyama, Masaki Mogi
The aim of this study was to investigate the efficacy and safety of YM-58483, a small molecular antagonist of Ca2+ release-activated Ca2+ (CRAC) channels, for the treatment of rheumatoid arthritis (RA), in vivo and ex vivo. YM-58483 was continuously injected subcutaneously in a collagen-induced arthritis (CIA) mouS.E.M.odel using an implanted osmotic pump. The severity of CIA was evaluated using the following parameters: body weight, hind paw volume, clinical score, histological analysis, cytokine levels, Ca2+ influx, and specific IgG production...
February 8, 2018: European Journal of Pharmacology
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