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efflux pump inhibition

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https://www.readbyqxmd.com/read/28435070/siderophores-in-clinical-isolates-of-klebsiella-pneumoniae-promote-ciprofloxacin-resistance-by-inhibiting-the-oxidative-stress
#1
Wenli Zhang, Ying Zhang, Xinxin Wang, Fengshu Ding, Yingmei Fu, Jizi Zhao, Wuqi Song, Ogutu James Opiyo, Fengmin Zhang, Xiaobei Chen
To explore the relevance of and understand the potential mechanisms behind the production of siderophores by clinical isolates of K. pneumoniae and ciprofloxacin (CIP) resistance, we divided the K. pneumoniae isolates into two groups based on bacterial siderophores productin: high siderophore-yielding group (39 strains) and low siderophore-yielding group (38 strains). The rate of CIP resistance in K. pneumoniae (27/39 = 69.23%) from the high siderophore-yielding group was significantly higher than that (16/38 = 42...
April 20, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28432381/modulation-of-the-multidrug-efflux-pump-emrd-3-from-vibrio-cholerae-by-allium-sativum-extract-and-the-bioactive-agent-allyl-sulfide-plus-synergistic-enhancement-of-antimicrobial-susceptibility-by-a-sativum-extract
#2
Merissa M Bruns, Prathusha Kakarla, Jared T Floyd, Mun Mun Mukherjee, Robert C Ponce, John A Garcia, Indrika Ranaweera, Leslie M Sanford, Alberto J Hernandez, T Mark Willmon, Grace L Tolson, Manuel F Varela
The causative agent of cholera, Vibrio cholerae, is a public health concern. Multidrug-resistant V. cholerae variants may reduce chemotherapeutic efficacies of severe cholera. We previously reported that the multidrug efflux pump EmrD-3 from V. cholerae confers resistance to multiple structurally distinct antimicrobials. Medicinal plant compounds are potential candidates for EmrD-3 efflux pump modulation. The antibacterial activities of garlic Allium sativum, although poorly understood, predicts that a main bioactive component, allyl sulfide, modulates EmrD-3 efflux...
April 21, 2017: Archives of Microbiology
https://www.readbyqxmd.com/read/28427190/pygopus2-inhibits-the-efficacy-of-paclitaxel-induced-apoptosis-and-induces-multidrug-resistance-in-human-glioma-cells
#3
Cefan Zhou, Hongxia Cheng, Wenying Qin, Yi Zhang, Hui Xiong, Jing Yang, Huang Huang, Yefu Wang, Xing-Zhen Chen, Jingfeng Tang
Anti-microtubule drugs, such as paclitaxel (PTX), are extensively used for the treatment of numerous cancers. However, growing evidence has shown that PTX resistance, either intrinsic or acquired, frequently occurs in patients and results in the failure of treatment, contributing to the high cancer mortality rate. Therefore, it is necessary to identify the genes or pathways involved in anti-microtubule drug resistance for future successful treatment of cancers. Pygopus2 (Pygo2), which contains a Zn-coordinated plant homeodomain (PHD) finger domain, is critical for β-catenin-dependent transcriptional switches in normal and malignant tissues and is over-expressed in various cancers, including human brain glioma...
March 2, 2017: Oncotarget
https://www.readbyqxmd.com/read/28411377/mir-495-sensitizes-mdr-cancer-cells-to-the-combination-of-doxorubicin-and-taxol-by-inhibiting-mdr1-expression
#4
Zhenyou Zou, Ruyi Zou, Dan Zong, Yonghong Shi, Jinyao Chen, Jie Huang, Jiahui Zhu, Liguan Chen, Xiaoyan Bao, Yuan Liu, Weihao Liu, Wenhui Huang, Jingsang Hu, Zhi Chen, Xiaojie Lao, Chaoqun Chen, Xiaoli Huang, Yao Lu, Xueyin Ni, Daoquan Fang, Dengqiang Wu, Shuangshuang Lu, Mingzhu Jiang, Chenyang Qiu, Yuya Wu, Qisha Qiu, Yanyuan Dong, Yangyang Su, Chenmin Zhao, Zhihe Zhong, Jing Cai, Yong Liang
MDR1 is highly expressed in MDR A2780DX5 ovarian cancer cells, MDR SGC7901R gastric cancer cells and recurrent tumours. It pumps cytoplasmic agents out of cells, leading to decreased drug accumulation in cells and making cancer cells susceptible to multidrug resistance. Here, we identified that miR-495 was predicted to target ABCB1, which encodes protein MDR1. To reduce the drug efflux and reverse MDR in cancer cells, we overexpressed a miR-495 mimic in SGC7901R and A2780DX cells and in transplanted MDR ovarian tumours in vivo...
April 14, 2017: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/28408143/tetrandrine-potentiates-the-glucocorticoid-pharmacodynamics-via-inhibiting-p-glycoprotein-and-mitogen-activated-protein-kinase-in-mitogen-activated-human-peripheral-blood-mononuclear-cells
#5
Wencheng Xu, Kehan Meng, Yuanchao Tu, Sachiko Tanaka, Kenji Onda, Kentaro Sugiyama, Toshihiko Hirano, Haruki Yamada
Glucocorticoids play significant roles in treatments of inflammatory and autoimmune diseases. Some patients show a poor or absent response even to high doses of glucocorticoids. The purpose of this study was to explore whether tetrandrine combined with glucocorticoids could be a new treatment strategy to resolve glucocorticoids resistance. Information on glucocorticoids sensitivity was usually obtained through mitogen-activated human peripheral blood mononuclear cells in cell culture procedures. Thus, human peripheral blood mononuclear cells was chosen as a model to study the immunosuppressive effect of methylprednisolone combined with tetrandrine, including the possible action mechanisms...
April 10, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28394295/antimicrobial-resistance-and-the-alternative-resources-with-special-emphasis-on-plant-based-antimicrobials-a-review
#6
REVIEW
Harish Chandra, Parul Bishnoi, Archana Yadav, Babita Patni, Abhay Prakash Mishra, Anant Ram Nautiyal
Indiscriminate and irrational use of antibiotics has created an unprecedented challenge for human civilization due to microbe's development of antimicrobial resistance. It is difficult to treat bacterial infection due to bacteria's ability to develop resistance against antimicrobial agents. Antimicrobial agents are categorized according to their mechanism of action, i.e., interference with cell wall synthesis, DNA and RNA synthesis, lysis of the bacterial membrane, inhibition of protein synthesis, inhibition of metabolic pathways, etc...
April 10, 2017: Plants (Basel, Switzerland)
https://www.readbyqxmd.com/read/28393677/in-silico-high-throughput-virtual-screening-and-molecular-dynamics-simulation-study-to-identify-inhibitor-for-adeabc-efflux-pump-of-acinetobacter-baumannii
#7
Privita Verma, Monalisa Tiwari, Vishvanath Tiwari
Emergence of multi-drug resistant strains of Acinetobacter baumannii has caused significant health problems and is responsible for high morbidity and mortality. Overexpression of AdeABC efflux system is one of the major mechanisms. In this study, we have focused on overcoming the drug resistance by identifying inhibitors that can effectively bind and inhibit integral membrane protein, AdeB of this efflux pump. We performed homology modeling to generate structure of AdeB using MODELLER v9.16 followed by model refinement using 3D-Refine tool and validated using PSVS, ProsaWeb, ERRAT etc...
April 10, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28385542/model-systems-for-studying-the-role-of-canalicular-efflux-transporters-in-drug-induced-cholestatic-liver-disease
#8
REVIEW
Bruno Stieger, Zainab M Mahdi
Bile formation is a key function of the liver. Disturbance of bile flow may lead to liver disease and is called cholestasis. Cholestasis may be inherited such as for example in progressive familial intrahepatic cholestasis or acquired, such as for example by drug-mediated inhibition of bile salt export from hepatocytes into the canaliculi. The key transport system for exporting bile salts into the canaliculi is the bile salt export pump. Inhibition of the bile salt export pump by drugs is a well-established cause of drug-induced cholestasis...
April 3, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28385250/in-vitro-evaluation-of-glycol-chitosan-based-formulations-as-oral-delivery-systems-for-efflux-pump-inhibition
#9
Delia Mandracchia, Adriana Trapani, Giuseppe Tripodo, Maria Grazia Perrone, Gaetano Giammona, Giuseppe Trapani, Nicola Antonio Colabufo
Recently, we have reported that glycol chitosan (GCS) was able to reverse the P- glycoprotein (P-gp) efflux pump. The objective of the present study was to evaluate the potential of two GCS-based dosage forms (aqueous solution or nanoparticle suspension) for oral administration of the P-gp substrate Rho-123. A further aim of the present study was to assess the effect of the glycol chitosan-4-thiobutylamidine thiomer (GCS-TBA) on P-gp activity considering that the corresponding thiomer of chitosan series is a well-known P-gp inhibitor...
June 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28381709/structural-analysis-and-new-drug-development-against-multidrug-efflux-pumps
#10
Seiji Yamasaki, Ryosuke Nakashima, Keisuke Sakurai, Akihito Yamaguchi, Kunihiko Nishino
 Multidrug efflux pumps are important in the multidrug resistance of Gram-negative pathogens. However, despite efforts to develop efflux inhibitors, clinically useful inhibitors are not available at present. ABI-PP (a pryridopyrimidine derivative) is a MexB-specific inhibitor that does not inhibit MexY; MexB and MexY are principal pumps in Pseudomonas aeruginosa. We previously found that drugs were exported through tandem proximal and distal multisite drug-binding pockets. Here we describe the first inhibitor-bound structures of pumps...
2017: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
https://www.readbyqxmd.com/read/28369588/in-vitro-drug-induced-liver-injury-prediction-criteria-optimization-of-efflux-transporter-ic50-and-physicochemical-properties
#11
Robert W Yucha, Kan He, Qin Shi, Lining Cai, Yukie Nakashita, Cindy Q Xia, Mingxiang Liao
Drug-induced liver injury (DILI) is a severe drug adverse response, which cannot always be reliably predicted in preclinical or clinical studies. Lack of observation of DILI during preclinical and clinical drug development has led to DILI being a leading cause of drug withdrawal from the market. As DILI is potentially fatal, pharmaceutical companies have been developing in vitro tools to screen for potential liver injury. Screens for physicochemical properties, mitochondrial function, and transport protein inhibition have all been employed to varying degrees of success...
March 27, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/28359232/identification-and-characterization-of-a-chemical-compound-that-inhibits-methionyl-trna-synthetase-from-pseudomonas-aeruginosa
#12
Sara Robles, Yanmei Hu, Tahyra Resto, Frank Dean, James M Bullard
Pseudomonas aeruginosa is an opportunistic pathogen problematic in causing nosocomial infections and is highly susceptible to development of resistance to multiple antibiotics. The gene encoding methionyl-tRNA synthetase (MetRS) from P. aeruginosa was cloned and the resulting protein characterized. MetRS was kinetically evaluated and the KM for its three substrates, methionine, ATP and tRNAMet were determined to be 35, 515, and 29 μM, respectively. P. aeruginosa MetRS was used to screen two chemical compound libraries (1690) and a natural product compound was identified that inhibited the aminoacylation function...
March 30, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28357121/uricosuric-targets-of-tranilast
#13
Asim K Mandal, Adriana Mercado, Andria Foster, Kambiz Zandi-Nejad, David B Mount
Uric acid, generated from the metabolism of purines, has both proven and emerging roles in human disease. Serum uric acid in humans is determined by production and by the net balance of reabsorption and secretion in kidney and intestine. In the human kidney, epithelial reabsorption dominates over secretion, such that in normal subjects there is at least 90% net reabsorption of filtered urate resulting in a fractional excretion of <10%. Tranilast, an anti-inflammatory drug with pleiotropic effects, has a marked hypouricemic, uricosuric effect in humans...
April 2017: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/28355970/clinical-impact-and-management-of-fluconazole-discontinuation-on-sirolimus-levels-in-bone-marrow-transplant-patients
#14
Edith Nwaroh, Jennifer Jupp, Esther Jadusingh, Gregory Guilcher
Sirolimus, an immunosuppressant, is indicated post-allogeneic stem cell transplant to reduce the risk of graft-versus-host-disease. Sirolimus is metabolized by cytochrome P450 3A4 and is a substrate of the P-glycoprotein (P-gp) drug efflux pump. Interactions with known inhibitors of the CYP3A4 enzyme and P-glycoprotein, such as fluconazole, are anticipated. Co-administration of fluconazole leads to an increase in sirolimus blood concentrations due to an inhibition of metabolism. The discontinuation of fluconazole will likely result in a decline in sirolimus blood concentrations, leaving patients at risk of graft-versus-host-disease...
January 1, 2017: Journal of Oncology Pharmacy Practice
https://www.readbyqxmd.com/read/28348056/analysis-of-shigella-flexneri-resistance-biofilm-formation-and-transcriptional-profile-in-response-to-bile-salts
#15
Kourtney P Nickerson, Rachael B Chanin, Jeticia R Sistrunk, David A Rasko, Peter J Fink, Eileen M Barry, James P Nataro, Christina S Faherty
The Shigella species cause millions of cases of watery or bloody diarrhea each year, mostly in children in developing countries. While many aspects of Shigella colonic cell invasion are known, crucial gaps in knowledge remain regarding how the bacteria survive, transit, and regulate gene expression prior to infection. In this study, we define mechanisms of bile salts resistance and build on previous research highlighting induced virulence in S. flexneri strain 2457T following bile salts exposure. Typical growth patterns were observed within the physiological range of bile salts; however, growth was inhibited at higher concentrations...
March 27, 2017: Infection and Immunity
https://www.readbyqxmd.com/read/28337665/effect-of-efflux-transporter-inhibition-on-the-distribution-of-fluconazole-in-the-rat-brain
#16
Wei Wang, Na Zheng, Jiatang Zhang, Xusheng Huang, Shengyuan Yu
Multidrug resistance-associated proteins (MRPs) and organic anion transporters (OATs) are expressed on the blood-brain barrier (BBB) and blood-cerebrospinal fluid barrier (BCSFB), preventing the entry of or the pumping out of numerous molecules. Fluconazole is widely used to treat fungal meningoencephalitis. The effect of these transporters on the distribution of fluconazole in the brain is unclear. We used microdialysis to compare the distribution of fluconazole in the rat brain with and without co-administration of probenecid, a MRP and OAT inhibitor...
March 24, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28337331/light-regulated-no-release-as-a-novel-strategy-to-overcome-doxorubicin-multidrug-resistance
#17
Konstantin Chegaev, Aurore Fraix, Elena Gazzano, Gamal Eldein F Abd-Ellatef, Marco Blangetti, Barbara Rolando, Sabrina Conoci, Chiara Riganti, Roberta Fruttero, Alberto Gasco, Salvatore Sortino
Nitric oxide (NO) release from a suitable NO photodonor (NOP) can be fine-tuned by visible light stimuli at doses that are not toxic to cells but that inhibit several efflux pumps; these are mainly responsible for the multidrug resistance of the anticancer agent doxorubicin (DOX). The strategy may thus increase DOX toxicity against resistant cancer cells. Moreover, a novel molecular hybrid covalently joining DOX and NOP showed similar increased toxicity toward resistant cancer cells and, in addition, lower cardiotoxicity than DOX...
March 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28319068/iron-addiction-a-novel-therapeutic-target-in-ovarian-cancer
#18
D Basuli, L Tesfay, Z Deng, B Paul, Y Yamamoto, G Ning, W Xian, F McKeon, M Lynch, C P Crum, P Hegde, M Brewer, X Wang, L D Miller, N Dyment, F M Torti, S V Torti
Ovarian cancer is a lethal malignancy that has not seen a major therapeutic advance in over 30 years. We demonstrate that ovarian cancer exhibits a targetable alteration in iron metabolism. Ferroportin (FPN), the iron efflux pump, is decreased, and transferrin receptor (TFR1), the iron importer, is increased in tumor tissue from patients with high grade but not low grade serous ovarian cancer. A similar profile of decreased FPN and increased TFR1 is observed in a genetic model of ovarian cancer tumor-initiating cells (TICs)...
March 20, 2017: Oncogene
https://www.readbyqxmd.com/read/28314281/chemosensitizing-properties-of-%C3%AE-caryophyllene-and-%C3%AE-caryophyllene-oxide-in-combination-with-doxorubicin-in-human-cancer-cells
#19
Silvia DI Giacomo, Antonella DI Sotto, Gabriela Mazzanti, Michael Wink
BACKGROUND/AIM: The natural sesquiterpenes β-caryophyllene (CRY) and β-caryophyllene oxide (CRYO) were evaluated for their potential chemosensitizing properties. MATERIALS AND METHODS: CRY and CRYO cytotoxicity was tested against the Caco-2, CCRF/CEM and CEM/ADR5000 human cancer cell lines. Furthermore, combination experiments were carried out in order to study the ability of the sesquiterpenes to increase doxorubicin cytotoxicity. The possible interference of CRY and CRYO with functionality of ATP-binding cassette (ABC)-transporters was also investigated by Rhodamine123 efflux assay...
March 2017: Anticancer Research
https://www.readbyqxmd.com/read/28294992/new-roads-leading-to-old-destinations-efflux-pumps-as-targets-to-reverse-multidrug-resistance-in-bacteria
#20
REVIEW
Gabriella Spengler, Annamária Kincses, Márió Gajdács, Leonard Amaral
Multidrug resistance (MDR) has appeared in response to selective pressures resulting from the incorrect use of antibiotics and other antimicrobials. This inappropriate application and mismanagement of antibiotics have led to serious problems in the therapy of infectious diseases. Bacteria can develop resistance by various mechanisms and one of the most important factors resulting in MDR is efflux pump-mediated resistance. Because of the importance of the efflux-related multidrug resistance the development of new therapeutic approaches aiming to inhibit bacterial efflux pumps is a promising way to combat bacteria having over-expressed MDR efflux systems...
March 15, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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