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Protein pump inhibitor

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https://www.readbyqxmd.com/read/29453043/understanding-of-human-atp-binding-cassette-superfamily-and-novel-multidrug-resistance-modulators-to-overcome-mdr
#1
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
#2
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
#3
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
https://www.readbyqxmd.com/read/29424299/medicinal-chemistry-updates-on-bacterial-efflux-pump-modulators
#4
Fernando Andre Pereira Marques Duraes, Madalena Maria Magalhaes Pinto, Maria Emilia Silva Pereira de Sousa
Antibiotic resistance is one of the most pressing health issues of our days. It can arise due to a multiplicity of factors, such as target modification, decrease in the drug uptake, changes in the metabolic pathways and activation of efflux pumps. The overexpression of efflux pumps is responsible for the extrusion of drugs, making antibiotic therapy fail, as the quantity of intracellular antibiotic is not enough to provide the desired therapeutic effect. Efflux pumps can be included in five families according to their composition, nature of substrates, energy source, and number of transmembrane spanning regions...
February 9, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29412345/characterisation-of-an-abc-transporter-of-a-resistant-candida-glabrata-clinical-isolate
#5
Debora Afonso Silva Rocha, Leandro Figueira Reis de Sa, Ana Carolina Cartagenes Pinto, Maria de Lourdes Junqueira, Emiliana Mandarano da Silva, Ronaldo Mohana Borges, Antonio Ferreira-Pereira
BACKGROUND: Candida glabrata ranks second in epidemiological surveillance studies, and is considered one of the main human yeast pathogens. Treatment of Candida infections represents a contemporary public health problem due to the limited availability of an antifungal arsenal, toxicity effects and increasing cases of resistance. C. glabrata presents intrinsic fluconazole resistance and is a significant concern in clinical practice and in hospital environments. OBJECTIVE: The aim of this study was to characterise the azole resistance mechanism presented by a C...
February 5, 2018: Memórias do Instituto Oswaldo Cruz
https://www.readbyqxmd.com/read/29409796/the-anti-diabetic-drug-dapagliflozin-induces-vasodilation-via-activation-of-pkg-and-kv-channels
#6
Hongliang Li, Sung Eun Shin, Mi Seon Seo, Jin Ryeol An, Il-Whan Choi, Won-Kyo Jung, Amy L Firth, Dae-Sung Lee, Mi-Jin Yim, Grace Choi, Jeong Min Lee, Sung Hun Na, Won Sun Park
AIM: Considering the clinical efficacy of dapagliflozin in patients with type 2 DM and the pathophysiological relevance of Kv channels for vascular reactivity. We investigate the vasodilatory effect of dapagliflozin and related mechanisms using phenylephrine (Phe)-induced contracted aortic rings. MATERIAL AND METHODS: Arterial tone measurement was performed in aortic smooth muscle. KEY FINDINGS: Application of dapagliflozin induced vasodilation in a concentration-dependent manner...
January 31, 2018: Life Sciences
https://www.readbyqxmd.com/read/29406029/lc-ms-ms-bioassay-of-four-proton-pump-inhibitors
#7
Ehab F Elkady, Marwa A Fouad, Bushra M Jaadan
A new validated bio-analytical LC-MS/MS method was developed for the simultaneous extraction and determination of four proton pump inhibitors: esomeprazole, lansoprazole, pantoprazole and rabeprazole in human plasma using escitalopram as an internal standard. The proteins in plasma samples were precipitated using acetonitrile for the extraction of analytes which is a simple economic method. The separation was accomplished using a mobile phase composed of 10 mM ammonium formate: acetonitrile: methanol (20:40:40% v/v) at a flow rate of 0...
February 15, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29404492/concomitant-proton-pump-inhibitor-use-does-not-reduce-the-efficacy-of-elbasvir-grazoprevir-a-pooled-analysis-of-1-322-patients-with-hepatitis-c-infection
#8
Nancy Reau, Michael N Robertson, Hwa-Ping Feng, Luzelena Caro, Wendy W Yeh, Bach-Yen T Nguyen, Janice Wahl, Eliav Barr, Peggy Hwang, Stephanie O Klopfer
Concomitant proton pump inhibitor (PPI) use reduces plasma concentrations of certain nonstructural protein 5A inhibitors, which are key components of modern hepatitis C infection (HCV) treatments. These reduced concentrations may decrease efficacy, leading to challenging treatment failures due to the development of resistance-associated substitutions. This post-hoc analysis assessed 12-week sustained viral response (SVR12) and pharmacokinetics of fixed-dose combination elbasvir/grazoprevir (EBR/GZR) in patients with HCV infection and self-reported PPI use...
October 2017: Hepatology Communications
https://www.readbyqxmd.com/read/29399561/salicylic-acid-reduces-ompf-expression-rendering-salmonella-enterica-serovar-typhimurium-more-resistant-to-cephalosporin-antibiotics
#9
Kyung Min Choi, Mi Hyun Kim, Hua Cai, Yong Jin Lee, Yeongjin Hong, Phil Youl Ryu
Salmonella enterica serovar Typhimurium is one of the most important bacterial pathogens causing diarrhea. The resistance of S. typhimurium to antimicrobial agents, which has recently been isolated from patients, is causing serious problems. We investigated the effects of salicylic acid (Sal) and acetyl salicylate (AcSal) on the susceptibility of S. typhimurium to cephalosporin antibiotics, which are known to increase resistance to cephalosporin and quinolone antibiotics. The MIC of cephalosporin antibiotics was higher than that of the media without Sal...
January 2018: Chonnam Medical Journal
https://www.readbyqxmd.com/read/29377455/lysotracker-and-mitotracker-red-are-transport-substrates-of-p-glycoprotein-implications-for-anticancer-drug-design-evading-multidrug-resistance
#10
Benny Zhitomirsky, Hodaya Farber, Yehuda G Assaraf
LysoTracker and MitoTracker Red are fluorescent probes widely used for viable cell staining of lysosomes and mitochondria, respectively. They are utilized to study organelle localization and their resident proteins, assess organelle functionality and quantification of organelle numbers. The ATP-driven efflux transporter P-glycoprotein (P-gp) is expressed in normal and malignant tissues and extrudes structurally distinct endogenous and exogenous cytotoxic compounds. Thus, once aromatic hydrophobic compounds such as the above-mentioned fluorescent probes are recognized as transport substrates, efflux pumps including P-gp may abolish their ability to reach their cellular target organelles...
January 26, 2018: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/29377374/identification-of-small-molecular-inhibitors-for-efflux-protein-rv2688c-of-mycobacterium-tuberculosis
#11
Rajender Vadija, Kiran Kumar Mustyala, Vasavi Malkhed, Ramasree Dulapalli, Hymavathi Veeravarapu, Ramesh Malikanti, Uma Vuruputuri
Mycobacterium tuberculosis (Mtb) is the pathogen, which causes Tuberculosis (TB). Development of Multidrug resistant (MDR) and extensively drug resistant (XDR) strains in Mtb is due to an efflux mechanism of antibiotics in the bacteria. The efflux pump proteins in the bacteria are implicated in the active efflux of antibiotics. The efflux pump protein, 'Fluoroquinolones export ATP-binding protein Rv2688c' (FEAB), is considered as a potential therapeutic target to prevent Tuberculosis. In the present work, in silico protocols are applied to identify inhibitors for the FEAB protein to arrest the efflux mechanism...
January 29, 2018: Biotechnology and Applied Biochemistry
https://www.readbyqxmd.com/read/29376492/is-the-use-of-proton-pump-inhibitors-a-risk-factor-for-alzheimer-s-disease-molecular-mechanisms-and-clinical-implications
#12
Kazuki Ide, Norihiro Matsuoka, Koji Kawakami
Proton-pump inhibitors (PPIs), such as omeprazole, lansoprazole, and rabeprazole, are used for the treatment of gastroesophageal reflux disease and peptic ulcer disease. The use of PPIs has increased, especially in older individuals, and a pharmacoepidemiological study indicated that the use of PPIs peaks in people aged 80 years or older. In this population, Alzheimer's disease (AD) is a common neurological disorder and type of dementia, occurring with a frequency of approximately 10%. Currently, over 45 million people are estimated to have dementia worldwide, and it is a major cause of death in the elderly...
January 28, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29339082/water-mediated-interactions-enable-smooth-substrate-transport-in-a-bacterial-efflux-pump
#13
Attilio Vittorio Vargiu, Venkata Krishnan Ramaswamy, Ivana Malvacio, Giuliano Malloci, Ulrich Kleinekathöfer, Paolo Ruggerone
BACKGROUND: Efflux pumps of the Resistance-Nodulation-cell Division superfamily confer multi-drug resistance to Gram-negative bacteria. The most-studied polyspecific transporter belonging to this class is the inner-membrane trimeric antiporter AcrB of Escherichia coli. In previous studies, a functional rotation mechanism was proposed for its functioning, according to which the three monomers undergo concerted conformational changes facilitating the extrusion of substrates. However, the molecular determinants and the energetics of this mechanism still remain unknown, so its feasibility must be proven mechanistically...
January 12, 2018: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29321388/suppression-of-abdominal-aortic-aneurysm-formation-in-mice-by-teneligliptin-a-dipeptidyl-peptidase-4-inhibitor
#14
Yusuke Takahara, Tomotake Tokunou, Toshihiro Ichiki
AIM: Dipeptidyl peptidase-4 (DPP-4) inhibitors lower blood glucose levels through inhibition of incretin degradation, which stimulates insulin secretion. Recent studies reported that DPP-4 inhibitors suppressed atherogenesis in apolipoprotein E-knockout (ApoEKO) mice. In this study, we investigated whether teneligliptin, a DPP-4 inhibitor, affects the development of abdominal aortic aneurysms (AAA) in ApoEKO mice. METHODS: ApoEKO mice were fed a high-fat diet (HFD) and infused with angiotensin (Ang) II by osmotic mini pumps for 4 weeks to induce AAA with (DPP-4i group) or without (control group) teneligliptin administered orally from 1 week before HFD and Ang II infusion to the end of the experiment...
January 10, 2018: Journal of Atherosclerosis and Thrombosis
https://www.readbyqxmd.com/read/29318780/the-synergistic-role-of-atp-dependent-drug-efflux-pump-and-focal-adhesion-signaling-pathways-in-vinorelbine-resistance-in-lung-cancer
#15
Takao Nakanishi, Toshi Menju, Shigeto Nishikawa, Koji Takahashi, Ryo Miyata, Kei Shikuma, Terumasa Sowa, Naoto Imamura, Masatsugu Hamaji, Hideki Motoyama, Kyoko Hijiya, Akihiro Aoyama, Toshihiko Sato, Toyofumi F Chen-Yoshikawa, Makoto Sonobe, Hiroshi Date
The vinorelbine (VRB) plus cisplatin regimen is widely used to treat non-small cell lung cancer (NSCLC), but its cure rate is poor. Drug resistance is the primary driver of chemotherapeutic failure, and the causes of resistance remain unclear. By focusing on the focal adhesion (FA) pathway, we have highlighted a signaling pathway that promotes VRB resistance in lung cancer cells. First, we established VRB-resistant (VR) lung cancer cells (NCI-H1299 and A549) and examined its transcriptional changes, protein expressions, and activations...
January 10, 2018: Cancer Medicine
https://www.readbyqxmd.com/read/29316665/towards-comprehension-of-the-abcb1-p-glycoprotein-role-in-chronic-myeloid-leukemia
#16
REVIEW
Raquel C Maia, Flavia C Vasconcelos, Paloma S Souza, Vivian M Rumjanek
Abstract: The introduction of imatinib (IM), a BCR-ABL1 tyrosine kinase inhibitor (TKI), has represented a significant advance in the first-line treatment of chronic myeloid leukemia (CML). However, approximately 30% of patients need to discontinue IM due to resistance or intolerance to this drug. Both resistance and intolerance have also been observed in treatment with the second-generation TKIs-dasatinib, nilotinib, and bosutinib-and the third-generation TKI-ponatinib. The mechanisms of resistance to TKIs may be BCR-ABL1-dependent and/or BCR-ABL1-independent...
January 7, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29304406/multixenobiotic-resistance-in-mytilus-edulis-molecular-and-functional-characterization-of-an-abcg2-type-transporter-in-hemocytes-and-gills
#17
Yosra Ben Cheikh, Benoit Xuereb, Céline Boulangé-Lecomte, Frank Le Foll
Among the cellular protection arsenal, ABC transporters play an important role in xenobiotic efflux in marine organisms. Two pumps belonging to B and C subfamily has been identified in Mytilus edulis. In this study, we investigated the presence of the third major subtype ABCG2/BCRP protein in mussel tissues. Transcript was expressed in hemocytes and with higher level in gills. Molecular characterization revealed that mussel ABCG2 transporter shares the sequence and organizational structure with mammalian and molluscan orthologs...
December 28, 2017: Aquatic Toxicology
https://www.readbyqxmd.com/read/29302209/histone-deacetylase-inhibition-attenuates-hepatic-steatosis-in-rats-with-experimental-cushing-s-syndrome
#18
Mina Kim, Hae-Ahm Lee, Hyun-Min Cho, Seol-Hee Kang, Eunjo Lee, In Kyeom Kim
Cushing's syndrome (CS) is a collection of symptoms caused by prolonged exposure to excess cortisol. Chronically elevated glucocorticoid (GC) levels contribute to hepatic steatosis. We hypothesized that histone deacetylase inhibitors (HDACi) could attenuate hepatic steatosis through glucocorticoid receptor (GR) acetylation in experimental CS. To induce CS, we administered adrenocorticotropic hormone (ACTH; 40 ng/kg/day) to Sprague-Dawley rats by subcutaneous infusion with osmotic mini-pumps. We administered the HDACi, sodium valproate (VPA; 0...
January 2018: Korean Journal of Physiology & Pharmacology
https://www.readbyqxmd.com/read/29286119/perioperative-oral-supplementation-with-fish-oil-promotes-liver-regeneration-following-partial-hepatectomy-in-mice-via-ampk-activation
#19
Hui Yao, Xiao Fu, Xuejian Zi, Wenjun Jia, Yudong Qiu
The present study aimed to observe the effects of perioperative oral supplementation with fish oil (FO) on liver regeneration in mice and examine the potential mechanism. A total of 120 male ICR mice were randomly divided into 5 groups: Sham, Control, fish oil (FO), Compound C [the AMP‑activated protein kinase (AMPK) inhibitor dorsomorphin], and Compound C + FO. Changes in liver function, alterations in hepatocyte proliferation and in the expression of polarization markers, and activation of AMPK signaling were examined following partial hepatectomy (PH)...
December 27, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29275225/the-efflux-pump-inhibitor-phenylalanine-arginine-beta-naphthylamide-pa%C3%AE-n-increases-the-resistance-to-carbapenems-in-chilean-clinical-isolates-of-kpc-producing-k-pneumoniae
#20
Alejandra Vera-Leiva, Sergio Carrasco-Anabalón, Celia A Lima, Nicolás Villagra, Mariana Domínguez, Helia Bello-Toledo, Gerardo González-Rocha
OBJECTIVES: KPC-producing strains present a wide range of MICs of carbapenems; this variation may be due to different gene expression levels of the blaKPC and porin genes, associated with efflux-pumps and the production of ESBLs and/or AmpC β-lactamase. The aim of this study was to determine the role of efflux-pumps inhibited by PAβN in the resistance to carbapenems in Chilean clinical isolates of K. pneumoniae harbouring the gene blaKPC. METHODS: Minimum Inhibitory Concentration (MIC) was determined by the agar dilution method for imipenem, meropenem, ertapenem and ciprofloxacin in the presence and absence of PAβN (25mg/L)...
December 21, 2017: Journal of Global Antimicrobial Resistance
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