keyword
https://read.qxmd.com/read/38546099/cardiac-glycosides-inhibit-early-and-late-vaccinia-virus-protein-expression
#1
JOURNAL ARTICLE
Jerzy Samolej, Ian J White, Blair L Strang, Jason Mercer
Cardiac glycosides (CGs) are natural steroid glycosides, which act as inhibitors of the cellular sodium-potassium ATPase pump. Although traditionally considered toxic to human cells, CGs are widely used as drugs for the treatment of cardiovascular-related medical conditions. More recently, CGs have been explored as potential anti-viral drugs and inhibit replication of a range of RNA and DNA viruses. Previously, a compound screen identified CGs that inhibited vaccinia virus (VACV) infection. However, no further investigation of the inhibitory potential of these compounds was performed, nor was there investigation of the stage(s) of the poxvirus lifecycle they impacted...
March 2024: Journal of General Virology
https://read.qxmd.com/read/38543080/a-drug-safety-briefing-ii-in-transplantation-from-real-world-individual-pharmacotherapy-management-to-prevent-patient-and-graft-from-polypharmacy-risks-at-the-very-earliest-stage
#2
REVIEW
Ursula Wolf
For early and long-term patient and graft survival, drug therapy in solid organ and hematopoietic stem cell transplantation inevitably involves polypharmacy in patients with widely varying and even abruptly changing conditions. In this second part, relevant medication briefing is provided, in addition to the scores defined in the previously published first part on the design of the Individual Pharmacotherapy Management (IPM). The focus is on the growing spectrum of contemporary polypharmacy in transplant patients, including early and long-term follow-up medications...
February 25, 2024: Pharmaceuticals
https://read.qxmd.com/read/38521473/discovery-of-novel-dihydronaphthalene-imidazole-ligands-as-potential-inhibitors-of-staphylococcus-aureus-multidrug-resistant-nora-efflux-pump-a-combination-of-experimental-and-in-silico-molecular-docking-studies
#3
JOURNAL ARTICLE
Asif A Malik, Nisar A Dangroo, Parminder Kaur, Shobit Attery, Manzoor A Rather, Abrar Khan, Tabassum Ara, Hemraj Nandanwar
Overexpression of the efflux pump is a predominant mechanism by which bacteria show antimicrobial resistance (AMR) and leads to the global emergence of multidrug resistance (MDR). In this work, the inhibitory potential of library of dihydronapthyl scaffold-based imidazole derivatives having structural resemblances with some known efflux pump inhibitors (EPI) were designed, synthesized and evaluated against efflux pump inhibitor against overexpressing bacterial strains to study the synergistic effect of compounds and antibiotics...
March 21, 2024: Microbial Pathogenesis
https://read.qxmd.com/read/38503568/antimicrobial-and-antibiofilm-activity-of-highly-soluble-polypyrrole-against-methicillin-resistant-staphylococcus-aureus
#4
JOURNAL ARTICLE
Danillo Sales Rosa, Samily Aquino de Sá Oliveira, Renata de Faria Silva Souza, Chirles Araujo de França, Isabelle Caroline Pires, Márcio Rennan Santos Tavares, Helinando Pequeno de Oliveira, Fernando Antônio Gomes da Silva Júnior, Maria Aparecida Scatamburlo Moreira, Mariana de Barros, Gustavo Batista de Menezes, Maísa Mota Antunes, Vasco Ariston de Carvalho Azevedo, Carine Rosa Naue, Mateus Matiuzzi da Costa
INTRODUCTION: As a new promising therapeutic option, the activity of highly soluble polypyrrole (Hs-PPy), a specific formulation of a conducting polymer (polypyrrole - PPy) is evaluated against bacteria of clinical importance. AIMS: The purpose was to evaluate the antimicrobial activity of Hs-PPy, alone or combined with oxacillin, as well as its antibiofilm potential against methicillin-resistant Staphylococcus aureus strains. Furthermore, the in silico inhibitory mechanism in efflux pumps was also investigated...
March 19, 2024: Journal of Applied Microbiology
https://read.qxmd.com/read/38503396/unlocking-bacterial-defense-exploring-the-potent-inhibition-of-nora-efflux-pump-by-coumarin-derivatives-in-staphylococcus-aureus
#5
JOURNAL ARTICLE
Ana Luíza A R Martin, Raimundo Luiz Silva Pereira, Janaína Esmeraldo Rocha, Pablo A M Farias, Thiago S Freitas, Francisco Rodrigo de Lemos Caldas, Fernando G Figueredo, Nadghia Figueiredo Leite Sampaio, Cícera Datiane de Morais Oliveira-Tintino, Saulo Relison Tintino, Gabriel Costa A da Hora, Maria Carolina Pacheco Lima, Irwin Rose A de Menezes, Diogo T Carvalho, Henrique D M Coutinho, Marta M F Fonteles
The occurrence of bacterial resistance has been increasing, compromising the treatment of various infections. The high virulence of Staphylococcus aureus allows for the maintenance of the infectious process, causing many deaths and hospitalizations. The MepA and NorA efflux pumps are transporter proteins responsible for expelling antimicrobial agents such as fluoroquinolones from the bacterial cell. Coumarins are phenolic compounds that have been studied for their diverse biological actions, including against bacteria...
March 20, 2024: Microbial Pathogenesis
https://read.qxmd.com/read/38501654/cell-envelope-structural-and-functional-contributions-to-antibiotic-resistance-in-burkholderia-cenocepacia
#6
JOURNAL ARTICLE
Andrew M Hogan, Anna Motnenko, A S M Zisanur Rahman, Silvia T Cardona
Antibiotic activity is limited by the physical construction of the Gram-negative cell envelope. Species of the Burkholderia cepacia complex (Bcc) are known as intrinsically multidrug-resistant opportunistic pathogens with low permeability cell envelopes. Here, we re-examined a previously performed chemical-genetic screen of barcoded transposon mutants in B. cenocepacia K56-2, focusing on cell envelope structural and functional processes. We identified structures mechanistically important for resistance to singular and multiple antibiotic classes...
March 19, 2024: Journal of Bacteriology
https://read.qxmd.com/read/38497784/unraveling-the-ligand-specificity-and-promiscuity-of-the-staphylococcus-aureus-nora-efflux-pump-a-computational-study
#7
JOURNAL ARTICLE
Esra Büşra Işık, Onur Serçinoğlu
Staphylococcus aureus , a gram-positive bacterial pathogen, develops antibiotic resistance partly through enhanced activity of transmembrane multi-drug efflux pump proteins like NorA. Being a prominent member of the Major Facilitator Superfamily (MFS), NorA transports various small molecules including hydrophilic fluoroquinolone antibiotics across the cell membrane. Intriguingly, NorA is inhibited by a structurally diverse set of small molecule inhibitors as well, indicating a highly promiscuous ligand/inhibitor recognition...
March 18, 2024: Journal of Biomolecular Structure & Dynamics
https://read.qxmd.com/read/38467328/fasn-negatively-regulates-p65-expression-by-reducing-its-stability-via-thr-254-phosphorylation-and-isomerization-by-pin1
#8
JOURNAL ARTICLE
Lincoln Barlow, Sophia Josephraj, Boqing Gu, Zizheng Dong, Jian-Ting Zhang
Fatty acid synthase (FASN), the sole cytosolic enzyme responsible for de novo palmitate synthesis in mammalian cells, has been associated with poor prognosis in cancer and shown to cause drug and radiation resistance by upregulating DNA-damage repair via suppression of p65 expression. Targeting FASN by repurposing proton pump inhibitors has generated impressive outcomes in triple negative breast cancer patients. While p65 regulation of DNA damage repair was thought to be due to its suppression of PARP1 gene transcription, the mechanism of FASN regulation of p65 expression was unknown...
March 9, 2024: Journal of Lipid Research
https://read.qxmd.com/read/38451783/activity-of-the-ubiquitin-activating-enzyme-inhibitor-tak-243-in-adrenocortical-carcinoma-acc-cell-lines-patient-derived-organoids-pdos-and-murine-xenografts
#9
JOURNAL ARTICLE
Yashuhiro Arakawa, Ukhyun Jo, Suresh Kumar, Nai-Yun Sun, Fathi Elloumi, Anish Thomas, Nitin Roper, Diana Grace Varghese, Naoko Takebe, Xiaohu Zhang, Michele Ceribelli, David O Holland, Erin Beck, Zina Itkin, Crystal McKnight, Kelli M Wilson, Jameson Travers, Carleen Klumpp-Thomas, Craig J Thomas, Chuong D Hoang, Jonathan M Hernandez, Jaydira Del Rivero, Yves Pommier
Current treatment options for metastatic adrenocortical carcinoma (ACC) have limited efficacy, despite the common use of mitotane and cytotoxic agents. This study aimed to identify novel therapeutic options for ACC. An extensive drug screen was conducted to identify compounds with potential activity against ACC cell lines. We further investigated the mechanism of action of the identified compound, TAK-243, its synergistic effects with current ACC therapeutics, and its efficacy in ACC models including patient-derived organoids and mouse xenografts...
March 7, 2024: Cancer Res Commun
https://read.qxmd.com/read/38447474/deleterious-association-between-proton-pump-inhibitor-and-protein-kinase-inhibitor-exposure-and-survival-for-patients-with-lung-cancer-a-nationwide-cohort-study
#10
JOURNAL ARTICLE
Constance Bordet, Mahmoud Zureik, Yoann Zelmat, Margaux Lafaurie, Maryse Lapeyre-Mestre, Agnès Sommet, Julien Mazieres, Fabien Despas
INTRODUCTION: Previous studies have identified an interaction between protein kinase inhibitors (PKIs) and proton pump inhibitors (PPIs) in patients with lung cancer. This type of interaction may reduce the efficacy of PKIs. However, the effect of PKI-PPI interaction on patient mortality remains controversial. This study set out to determine the impact of PKI-PPI interaction on overall survival for lung cancer patients. MATERIALS AND METHODS: This study was conducted using data from the French National Health Care Database from January 1, 2011 to December 31, 2021...
February 29, 2024: Cancer Treatment and Research Communications
https://read.qxmd.com/read/38439656/control-iq-technology-use-in-individuals-with-high-insulin-requirements-results-from-the-multicenter-higher-iq-trial
#11
JOURNAL ARTICLE
Anders L Carlson, Timothy E Graham, Halis K Akturk, David R Liljenquist, Richard M Bergenstal, Becky Sulik, Viral N Shah, Mark Sulik, Peter Zhao, Peter Briggs, Ravid Sassan-Katchalski, Jordan E Pinsker
BACKGROUND: Control-IQ technology version 1.5 allows for a wider range of weight and total daily insulin (TDI) entry, in addition to other changes to enhance performance for users with high basal rates. This study evaluated the safety and performance of the updated Control-IQ system for users with basal rates >3 units/h and high TDI in a multicenter, single arm, prospective study. METHODS: Adults with type 1 diabetes (T1D) using continuous subcutaneous insulin infusion (CSII) and at least one basal rate over 3 units/h (N = 34, mean age = 39...
March 5, 2024: Journal of Diabetes Science and Technology
https://read.qxmd.com/read/38422177/glycolysis-mediated-activation-of-v-atpase-by-nicotinamide-mononucleotide-ameliorates-lipid-induced-cardiomyopathy-by-repressing-the-cd36-tlr4-axis
#12
JOURNAL ARTICLE
Shujin Wang, Yinying Han, Ruimin Liu, Mengqian Hou, Dietbert Neumann, Jun Zhang, Fang Wang, Yumeng Li, Xueya Zhao, Francesco Schianchi, Chao Dai, Lizhong Liu, Miranda Nabben, Jan F C Glatz, Xin Wu, Xifeng Lu, Xi Li, Joost J F P Luiken
BACKGROUND: Chronic overconsumption of lipids followed by their excessive accumulation in the heart leads to cardiomyopathy. The cause of lipid-induced cardiomyopathy involves a pivotal role for the proton-pump vacuolar-type H+ -ATPase (v-ATPase), which acidifies endosomes, and for lipid-transporter CD36, which is stored in acidified endosomes. During lipid overexposure, an increased influx of lipids into cardiomyocytes is sensed by v-ATPase, which then disassembles, causing endosomal de-acidification and expulsion of stored CD36 from the endosomes toward the sarcolemma...
March 2024: Circulation Research
https://read.qxmd.com/read/38399772/overview-of-ecology-and-aspects-of-antibiotic-resistance-in-campylobacter-spp-isolated-from-free-grazing-chicken-tissues-in-rural-households
#13
JOURNAL ARTICLE
Argyrios Dermatas, Georgios Rozos, Konstantinos Zaralis, Aikaterini Dadamogia, Konstantina Fotou, Eugenia Bezirtzoglou, Konstantoula Akrida-Demertzi, Panagiotis Demertzis, Chrysoula Chrysa Voidarou
Rural households all over the world rear backyard chicken mainly for their own consumption and, to a lesser extent, for barter trade. These chickens represent a staple dish with numerous culinary variations and a cheap source of protein. Although some Campylobacter species, and particularly Campylobacter jejuni and Campylobacter coli , have been associated with industrial poultry carcasses, studies concerning the ecology of this genus in rural households do not exist. To assess the prevalence of Campylobacter species in the tissues of backyard chickens, samples were collected from birds Gallus domesticus bred in households in the rural area of Epirus (Greece), and Campylobacter strains were isolated by quantitative methods at 37 °C and 42 °C...
February 10, 2024: Microorganisms
https://read.qxmd.com/read/38399423/structure-based-in-silico-approaches-reveal-iressa-as-a-multitargeted-breast-cancer-regulatory-signalling-and-receptor-protein-inhibitor
#14
JOURNAL ARTICLE
Hassan Hussain Almasoudi, Mutaib M Mashraqi, Saleh A Alshamrani, Afaf Awwadh Alharthi, Ohud Alsalmi, Mohammed H Nahari, Fares Saeed H Al-Mansour, Abdulfattah Yahya M Alhazmi
Breast cancer begins in the breast cells, mainly impacting women. It starts in the cells that line the milk ducts or lobules responsible for producing milk and can spread to nearby tissues and other body parts. In 2020, around 2.3 million women across the globe received a diagnosis, with an estimated 685,000 deaths. Additionally, 7.8 million women were living with breast cancer, making it the fifth leading cause of cancer-related deaths among women. The mutational changes, overexpression of drug efflux pumps, activation of alternative signalling pathways, tumour microenvironment, and cancer stem cells are causing higher levels of drug resistance, and one of the major solutions is to identify multitargeted drugs...
February 6, 2024: Pharmaceuticals
https://read.qxmd.com/read/38371642/eosinophilic-oesophagitis-in-a-nigerian-adolescent-a-case-report
#15
Ikobah Joanah Moses, Ikwuagwu Elekwachi, Ita Ukpabio, Theophilus Ugbem, Omeodu Chimankpan Okechukwu, Emmanuel Ekanem
Eosinophilic oesophagitis (EoE) is a chronic immune and antigen-mediated disease characterized by symptoms related to oesophageal dysfunction, and histologically, is marked by eosinophilic infiltrate in the oesophageal mucosa. It is prevalent in developed countries and considered rare in developing countries. There is an interplay of allergic and genetic factors in the aetiology of EoE. This is a report of EoE in a 15-year-old female adolescent in Nigeria who presented to the University of Calabar Teaching Hospital with recurrent vomiting, abdominal pain, weight loss, and dysphagia...
2024: Pan African Medical Journal
https://read.qxmd.com/read/38341568/the-anti-staphylococcal-fusidic-acid-as-an-efflux-pump-inhibitor-combined-with-fluconazole-against-vaginal-candidiasis-in-mouse-model
#16
JOURNAL ARTICLE
Salwa E Gomaa, Hisham A Abbas, Fatma A Mohamed, Mohamed A M Ali, Tarek M Ibrahim, Alyaa S Abdel Halim, Mashael A Alghamdi, Basem Mansour, Anis Ahmad Chaudhary, Amr Elkelish, Fehmi Boufahja, Wael A H Hegazy, Fatma Al-Zahraa A Yehia
BACKGROUND: Candida albicans is the most common fungus that causes vaginal candidiasis in immunocompetent women and catastrophic infections in immunocompromised patients. The treatment of such infections is hindered due to the increasing emergence of resistance to azoles in C. albicans. New treatment approaches are needed to combat candidiasis especially in the dwindled supply of new effective and safe antifungals. The resistance to azoles is mainly attributed to export of azoles outside the cells by means of the efflux pump that confers cross resistance to all azoles including fluconazole (FLC)...
February 10, 2024: BMC Microbiology
https://read.qxmd.com/read/38339095/the-mechanism-of-tigecycline-resistance-in-acinetobacter-baumannii-under-sub-minimal-inhibitory-concentrations-of-tigecycline
#17
JOURNAL ARTICLE
Cunwei Liu, Jia Liu, Qinghui Lu, Ping Wang, Qinghua Zou
The presence of sub-minimal inhibitory concentration (sub-MIC) antibiotics in our environment is widespread, and their ability to induce antibiotic resistance is inevitable. Acinetobacter baumannii , a pathogen known for its strong ability to acquire antibiotic resistance, has recently shown clinical resistance to the last-line antibiotic tigecycline. To unravel the complex mechanism of A. baumannii drug resistance, we subjected tigecycline-susceptible, -intermediate, and -mildly-resistant strains to successive increases in sub-MIC tigecycline and ultimately obtained tigecycline-resistant strains...
February 2, 2024: International Journal of Molecular Sciences
https://read.qxmd.com/read/38283226/development-of-pharmacophore-models-for-acrb-protein-and-the-identification-of-potential-adjuvant-candidates-for-overcoming-efflux-mediated-colistin-resistance
#18
JOURNAL ARTICLE
Dibyajyoti Uttameswar Behera, Mahendra Gaur, Maheswata Sahoo, Enketeswara Subudhi, Bharat Bhusan Subudhi
Growing multi-drug resistance (MDR) among ESKAPE pathogens is a huge challenge. Increased resistance to last-resort antibiotics, like colistin, has further aggravated this. Efflux is identified as a major route of colistin resistance. So, finding an FDA-approved efflux inhibitor for potential application as an adjuvant to colistin was the primary objective of this study. E. coli -AcrB pump inhibitors and substrates were used to develop and validate the pharmacophoric model. Drugs confirming this pharmacophore were subjected to molecular docking to identify hits for the AcrB binding pocket...
January 25, 2024: RSC medicinal chemistry
https://read.qxmd.com/read/38283082/the-cell-envelope-integrity-protein-homologue-d0y85_rs06240-of-stenotrophomonas-confers-multiantibiotic-resistance
#19
JOURNAL ARTICLE
Chuanqing Zhong, Xiaoqiang Deng, Aihua Jiang, Yayu Liu, Yuanyuan Liu, Jiafang Fu, Guangxiang Cao
BACKGROUND: The potential role of cell envelope integrity proteins in mediating antibiotic resistance is not well understood. In this study, we investigated whether the cell envelope integrity protein D0Y85_RS06240 from the multiantibiotic resistant strain Stenotrophomonas sp. G4 mediates antibiotic resistance. METHODS: Bioinformatics analysis was conducted to identify proteins related to the D0Y85_RS06240 protein. The D0Y85_RS06240 gene was heterologously expressed in Escherichia coli , both antibiotic MICs and the effect of efflux pump inhibitors on antibiotic MICs were determined by the broth microdilution method...
2024: Canadian Journal of Infectious Diseases & Medical Microbiology
https://read.qxmd.com/read/38269224/chronic-use-of-proton-pump-inhibitors-a-potential-link-to-amino-acid-deficiency-and-the-development-of-depression
#20
Jeevan J Murthy, Sarah Hughes, Colin Travis, Ankit Chalia, Samira Khan, Michael Ang-Rabanes, Raja Mogallapu
In recent years, the gut-brain axis (GBA) has been implicated in several vital physiological processes, including digestion, immunity, inflammation, and mood regulation. Disruption of this network is tied to the development of several pathological conditions, including mood disorders, inflammatory bowel diseases, and dementia. Proton pump inhibitors (PPI) are among the most utilized and easily accessible medications worldwide. Although they are effective at treating conditions, including gastroesophageal reflux disorder (GERD), peptic ulcer disease, Zollinger-Ellison syndrome, and erosive esophagitis, PPIs have several mechanisms that may precipitate protein and, thus, amino acid malnutrition...
December 2023: Curēus
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