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https://www.readbyqxmd.com/read/28329765/structural-insights-into-adiponectin-receptors-suggest-ceramidase-activity
#1
Ieva Vasiliauskaité-Brooks, Remy Sounier, Pascal Rochaix, Gaëtan Bellot, Mathieu Fortier, François Hoh, Luigi De Colibus, Chérine Bechara, Essa M Saied, Christoph Arenz, Cédric Leyrat, Sébastien Granier
Adiponectin receptors (ADIPORs) are integral membrane proteins that control glucose and lipid metabolism by mediating, at least in part, a cellular ceramidase activity that catalyses the hydrolysis of ceramide to produce sphingosine and a free fatty acid (FFA). The crystal structures of the two receptor subtypes, ADIPOR1 and ADIPOR2, show a similar overall seven-transmembrane-domain architecture with large unoccupied cavities and a zinc binding site within the seven transmembrane domain. However, the molecular mechanisms by which ADIPORs function are not known...
March 22, 2017: Nature
https://www.readbyqxmd.com/read/28327306/design-synthesis-antibacterial-activity-and-docking-study-of-some-new-trimethoprim-derivatives
#2
Umer Rashid, Waqas Ahmad, Syed Fahad Hassan, Naveeda Akhtar Qureshi, Basit Niaz, Bakhtiar Muhammad, Sameera Imdad, Muhammad Sajid
In present study, nineteen novel trimethoprim (TMP) derivatives were designed, synthesized and evaluated for their antibacterial potential. Hydroxy trimethoprim 2 (HTMP) was synthesized by following the demethylation of 4-methoxy group at trimethoxy benzyl ring of TMP. Structure-activity relationship (SAR) studies were explored on HTMP by incorporating various substituents leading to the identification of some new compounds with improved antibacterial activities. The results revealed that the introduction of benzyloxy (4a-e) and phenyl ethanone (5a-e) group at 4-position of dimethoxy benzyl ring leads to overall increase in the antibacterial activity...
December 1, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28323106/implications-of-epigallocatechin-3-gallate-in-cultured-human-sertoli-cells-glycolytic-and-oxidative-profile
#3
Tânia R Dias, Marco G Alves, Joaquina Silva, Alberto Barros, Mário Sousa, Susana Casal, Branca M Silva, Pedro F Oliveira
Sertoli cells are crucial for the success of spermatogenesis, which is the biological process that ensures male fertility. These cells present high metabolic rates, being often subjected to high oxidative stress levels that, if uncontrolled, may compromise male fertility. Since the most abundant tea catechin, epigallocatechin-3-gallate (EGCG), has demonstrated a potent preventive activity against oxidative stress, we have evaluated its effect at concentrations of 5 and 50μM, on the metabolism, mitochondrial functionality and oxidative profile of human Sertoli cells (hSCs)...
March 17, 2017: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/28323051/anticancer-and-anti-angiogenic-activities-of-extract-from-actinidia-eriantha-benth-root
#4
Jian-Guo Wu, Li Ma, Shui-Hua Lin, Yan-Bin Wu, Jun Yi, Bin-Jun Yang, Jin-Zhong Wu, Ka-Hing Wong
ETHNOPHARMACOLOGICAL RELEVANCE: The roots of Actinidia eriantha Benth (AER) are commonly used traditional folk medicine for the treatment of gastric carcinoma, nasopharyngeal carcinoma, and breast carcinoma. Besides, the anti-proliferative and immunomodulatory effects of AER polysaccharides on tumor-bearing mice have been reported previously. AIM OF THE STUDY: This work was carried out to investigate the anticancer and anti-angiogenic activities of AER. MATERIALS AND METHODS: The growth inhibitory effects of ethanol extracts from the leaves (EEL), stems (EES) and roots (EER) of A...
March 17, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28322271/mechanistic-and-structural-basis-of-bioengineered-bovine-cathelicidin-5-with-optimized-therapeutic-activity
#5
Bikash R Sahoo, Kenta Maruyama, Jyotheeswara R Edula, Takahiro Tougan, Yuxi Lin, Young-Ho Lee, Toshihiro Horii, Toshimichi Fujiwara
Peptide-drug discovery using host-defense peptides becomes promising against antibiotic-resistant pathogens and cancer cells. Here, we customized the therapeutic activity of bovine cathelicidin-5 targeting to bacteria, protozoa, and tumor cells. The membrane dependent conformational adaptability and plasticity of cathelicidin-5 is revealed by biophysical analysis and atomistic simulations over 200 μs in thymocytes, leukemia, and E. coli cell-membranes. Our understanding of energy-dependent cathelicidin-5 intrusion in heterogeneous membranes aided in designing novel loss/gain-of-function analogues...
March 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28320998/design-synthesis-and-biological-evaluation-of-potent-human-glyoxalase-i-inhibitors
#6
Tian Jin, Jing Zhai, Xiao Liu, Yan Yue, Maolin Huang, Zonghe Li, Caixia Ni, Qishan Deng, Yankui Sang, Zhongwei Yao, Hong Zhang, Xiaopeng Hu, Zhe-Bin Zheng
Several glutathione derivatives bearing the S-(N-aryl-N-hydroxycarbamoyl) or S-(C-aryl-N-hydroxycarbamoyl) moieties [10, 10' and 13-15] were synthesized, characterized, and their human glyoxalase I (hGLO1) inhibitory activity was evaluated. Compound 10 was proved to be the effective hGLO1 inhibitor with a Ki value of 1 nM and the inhibition effect of compound 10 on hGLO1 was nearly ten-fold higher than that of the strongest inhibitor 2 (Ki = 10 nM) which has been reported in the field of glutathione-type hGLO1 inhibitors...
March 17, 2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28320857/regulation-of-very-long-acyl-chain-ceramide-synthesis-by-acyl-coa-binding-protein
#7
Natalia Santos Ferreira, Hanne Engelsby, Ditte Neess, Samuel L Kelly, Giora Volpert, Alfred H Merrill, Anthony H Futerman, Nils J Faergeman
Ceramide and more complex sphingolipids constitute a diverse group of lipids, which serve important roles as structural entities of biological membranes and as regulators of cellular growth, differentiation, and development. Thus, ceramides are vital players in numerous diseases including metabolic and cardiovascular diseases as well as neurological disorders. Here we show that acyl coenzyme A binding protein (ACBP) potently facilitates very-long acyl chain ceramide synthesis. ACBP increases the activity of ceramide synthase 2 (CerS2) by more than 2-fold and CerS3 activity by 7-fold...
March 19, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28319176/insight-into-the-mechanism-of-action-of-temporin-sha-a-new-broad-spectrum-antiparasitic-and-antibacterial-agent
#8
Zahid Raja, Sonia André, Feten Abbassi, Vincent Humblot, Olivier Lequin, Tahar Bouceba, Isabelle Correia, Sandra Casale, Thierry Foulon, Denis Sereno, Bruno Oury, Ali Ladram
Antimicrobial peptides (AMPs) are promising drugs to kill resistant pathogens. In contrast to bacteria, protozoan parasites, such as Leishmania, were little studied. Therefore, the antiparasitic mechanism of AMPs is still unclear. In this study, we sought to get further insight into this mechanism by focusing our attention on temporin-SHa (SHa), a small broad-spectrum AMP previously shown to be active against Leishmania infantum. To improve activity, we designed analogs of SHa and compared the antibacterial and antiparasitic mechanisms...
2017: PloS One
https://www.readbyqxmd.com/read/28317440/potent-immune-responses-induced-by-a-salmonella-ghost-delivery-system-that-expresses-the-recombinant-stx2eb-fedf-and-feda-proteins-of-the-escherichia-coli-producing-f18-and-shiga-toxin-in-a-murine-model-and-evaluation-of-its-protective-effect-as-a-porcine-vaccine
#9
Gayeon Won, John Hwa Lee
BACKGROUND: In the pathogenicity of porcine edema disease, which is caused by the Escherichia coli-producing F18 and Shiga toxin, F18(+) fimbrial adhesins and Shiga toxin 2e (Stx2e) play pivotal roles in the colonization and enterotoxicity of this pathogen. OBJECTIVE: To develop a vaccine candidate against edema disease by combining three selected antigens of F18(+) Shiga toxin-producing Escherichia coli (STEC). METHODS: Genetically engineered Salmonella Typhimurium (ST) ghosts that express Stx2eB, FedF, and FedA were individually inserted in a ghost plasmid cassette (pJHL184), and the resultant plasmids were transformed into a Δasd Δlon ΔcpxR ST (JOL912)...
March 20, 2017: Veterinary Quarterly
https://www.readbyqxmd.com/read/28315687/-10-gingerol-a-major-phenolic-constituent-of-ginger-root-induces-cell-cycle-arrest-and-apoptosis-in-triple-negative-breast-cancer-cells
#10
Megan M Bernard, Jason R McConnery, David W Hoskin
The ginger rhizome is rich in bioactive compounds, including [6]-gingerol, [8]-gingerol, and [10]-gingerol; however, to date, most research on the anti-cancer activities of gingerols have focused on [6]-gingerol. In this study, we compared [10]-gingerol with [8]-gingerol and [6]-gingerol in terms of their ability to inhibit the growth of human and mouse mammary carcinoma cells. A colorimetric assay based on the enzymatic reduction of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide revealed that [10]-gingerol was more potent than [6]-gingerol and at least as potent as [8]-gingerol for the inhibition of triple-negative human (MDA-MB-231, MDA-MB-468) and mouse (4T1, E0771) mammary carcinoma cell growth...
March 16, 2017: Experimental and Molecular Pathology
https://www.readbyqxmd.com/read/28315462/implications-of-cerebrovascular-atp-binding-cassette-transporter-g1-abcg1-and-apolipoprotein-m-in-cholesterol-transport-at-the-blood-brain-barrier
#11
Alexandra Carmen Kober, Anil Paul Chirackal Manavalan, Carmen Tam-Amersdorfer, Andreas Holmér, Ahmed Saeed, Elham Fanaee Danesh, Martina Zandl, Nicole Maria Albrecher, Ingemar Björkhem, Gerhard M Kostner, Björn Dahlbäck, Ute Panzenboeck
Impaired cholesterol/lipoprotein metabolism is linked to neurodegenerative diseases such as Alzheimer's disease (AD). Cerebral cholesterol homeostasis is maintained by the highly efficient blood-brain barrier (BBB) and flux of the oxysterols 24(S)-hydroxycholesterol and 27-hydroxycholesterol, potent liver-X-receptor (LXR) activators. HDL and their apolipoproteins are crucial for cerebral lipid transfer, and loss of ATP binding cassette transporters (ABC)G1 and G4 results in toxic accumulation of oxysterols in the brain...
March 14, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28314993/comparative-analysis-of-internalisation-haemolytic-cytotoxic-and-antibacterial-effect-of-membrane-active-cationic-peptides-aspects-of-experimental-setup
#12
Kata Horváti, Bernadett Bacsa, Tamás Mlinkó, Nóra Szabó, Ferenc Hudecz, Ferenc Zsila, Szilvia Bősze
Cationic peptides proved fundamental importance as pharmaceutical agents and/or drug carrier moieties functioning in cellular processes. The comparison of the in vitro activity of these peptides is an experimental challenge and a combination of different methods, such as cytotoxicity, internalisation rate, haemolytic and antibacterial effect, is necessary. At the same time, several issues need to be addressed as the assay conditions have a great influence on the measured biological effects and the experimental setup needs to be optimised...
March 17, 2017: Amino Acids
https://www.readbyqxmd.com/read/28303012/tryptophan-end-tagging-for-promoted-lipopolysaccharide-interactions-and-anti-inflammatory-effects
#13
Shalini Singh, Aritreyee Datta, Artur Schmidtchen, Anirban Bhunia, Martin Malmsten
The objective of the present study is the investigation of possibilities for boosting peptide anti-inflammatory effects by tryptophan end-tagging, including identification of underlying mechanisms for this. In doing so, effects of tryptophan end-tagging of KYE21 (KYEITTIHNLFRKLTHRLFRR), a peptide derived from heparin co-factor II, on membrane and lipopolysaccharide (LPS) interactions were investigated by ellipsometry, NMR, fluorescence spectroscopy, and circular dichroism measurements. Through its N-terminal W stretch, WWWKYE21 displays higher membrane binding, liposome rupture, and bacterial killing than unmodified KYE21...
March 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28300835/geranylgeranyl-diphosphate-synthase-inhibition-induces-apoptosis-that-is-dependent-upon-ggpp-depletion-erk-phosphorylation-and-caspase-activation
#14
Sherry S Agabiti, Jin Li, Andrew J Wiemer
Bisphosphonates are diphosphate analogs that inhibit the intermediate enzymes of the mevalonate pathway. Here, we compared the effects of a farnesyl diphosphate synthase inhibitor, zoledronate, and a geranylgeranyl diphosphate synthase (GGDPS) inhibitor, digeranyl bisphosphonate (DGBP), on lymphocytic leukemia cell proliferation and apoptosis. Both zoledronate and DGBP inhibited proliferation with DGBP doing so more potently. DGBP was markedly less toxic than zoledronate toward the viability of healthy human peripheral blood mononuclear cells...
March 16, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28299853/the-effect-of-a-beta-lactamase-inhibitor-peptide-on-bacterial-membrane-structure-and-integrity-a-comparative-study
#15
Begum Alaybeyoglu, Bilge Gedik Uluocak, Berna Sariyar Akbulut, Elif Ozkirimli
Co-administration of beta-lactam antibiotics and beta-lactamase inhibitors has been a favored treatment strategy against beta-lactamase-mediated bacterial antibiotic resistance, but the emergence of beta-lactamases resistant to current inhibitors necessitates the discovery of novel non-beta-lactam inhibitors. Peptides derived from the Ala46-Tyr51 region of the beta-lactamase inhibitor protein are considered as potent inhibitors of beta-lactamase; unfortunately, peptide delivery into the cell limits their potential...
March 16, 2017: Journal of Peptide Science: An Official Publication of the European Peptide Society
https://www.readbyqxmd.com/read/28298149/methotrexate-induced-mitochondrial-injury-and-cytochrome-c-release-in-rat-liver-hepatocytes
#16
Abdullah Al Maruf, Peter J O'Brien, Parvaneh Naserzadeh, Rozhina Fathian, Ahmad Salimi, Jalal Pourahmad
Methotrexate (MTX) is a folic acid antagonist that is widely used to treat a variety of diseases. One of the most serious side effects of MTX therapy is hepatotoxicity. The potential molecular cytotoxic mechanisms of MTX toward isolated rat hepatocytes were investigated using Accelerated Cytotoxicity Mechanism Screening (ACMS) techniques. A concentration and time dependent increase in cytotoxicity and reactive oxygen species (ROS) formation and a decrease in mitochondrial membrane potential (MMP) were observed with MTX...
March 16, 2017: Drug and Chemical Toxicology
https://www.readbyqxmd.com/read/28296541/pharmacological-modulators-of-autophagy-activate-a-parallel-noncanonical-pathway-driving-unconventional-lc3-lipidation
#17
Elise Jacquin, Stéphanie Leclerc-Mercier, Celine Judon, Emmanuelle Blanchard, Sylvie Fraitag, Oliver Florey
The modulation of canonical macroautophagy/autophagy for therapeutic benefit is an emerging strategy of medical and pharmaceutical interest. Many drugs act to inhibit autophagic flux by targeting lysosome function, while others were developed to activate the pathway. Here, we report the surprising finding that many therapeutically relevant autophagy modulators with lysosomotropic and ionophore properties, classified as inhibitors of canonical autophagy, are also capable of activating a parallel noncanonical autophagy pathway that drives MAP1LC3/LC3 lipidation on endolysosomal membranes...
February 15, 2017: Autophagy
https://www.readbyqxmd.com/read/28288817/animal-venoms-as-a-source-of-natural-antimicrobials-an-overview
#18
REVIEW
Ramar Perumal Samy, Bradley G Stiles, Octavio L Franco, Gautam Sethi, Lina Hk Lim
Hospitals are breeding grounds for many life-threatening bacteria worldwide. Clinically associated gram-positive bacteria such as Staphylococcus aureus/methicillin-resistant S. aureus and many others increase the risk of severe mortality and morbidity. The failure of antibiotics to kill various pathogens due to bacterial resistance highlights the urgent need to develop novel, potent, and less toxic agents from natural sources against various infectious agents. Currently, several promising classes of natural molecules from snake (terrestrial and sea), scorpion, spider, honey bee and wasp venoms hold promise as rich sources of chemotherapeutics against infectious pathogens...
March 10, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28287172/killing-of-staphylococcus-aureus-and-salmonella-enteritidis-and-neutralization-of-lipopolysaccharide-by-17-residue-bovine-lactoferricins-improved-activity-of-trp-ala-containing-molecules
#19
Ya Hao, Na Yang, Xiumin Wang, Da Teng, Ruoyu Mao, Xiao Wang, Zhanzhan Li, Jianhua Wang
Bovine lactoferricin (LfcinB) has potent antibacterial, antifungal and antiparasitic activities but is also hemolytic. Our objective was to identify LfcinB17-31 derivatives with reduced hemolysis and improved antimicrobial activity via substituting Cys3, Arg4, Gln7, Met10, and Gly14 with more hydrophobic residues. Two peptides, Lfcin4 and Lfcin5, showed higher activity against Staphylococcus aureus and Salmonella enteritidis and lower hemolytic activity than the parent peptide LfcinB17-31. These peptides permeabilized the outer and inner membranes of S...
March 13, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28284981/exosomes-from-m1-polarized-macrophages-potentiate-the-cancer-vaccine-by-creating-a-pro-inflammatory-microenvironment-in-the-lymph-node
#20
Lifang Cheng, Yuhua Wang, Leaf Huang
Exosomes are small membrane-bound vesicular particles generated by most cells for intercellular communication and regulation. During biogenesis, specific lipids, RNAs, proteins, and carbohydrates are enriched and packaged into the vesicles so that the exosomal contents reflect not only the source but also the physiological conditions of the parental cells. These exosomes transport materials or signals to the target cells for diverse physiological purposes. Our study focused on the exosomes derived from M1-polarized, proinflammatory macrophages for the possibility of using M1 exosomes as an immunopotentiator for a cancer vaccine...
March 8, 2017: Molecular Therapy: the Journal of the American Society of Gene Therapy
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