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https://www.readbyqxmd.com/read/28636355/semisynthetic-flavone-derived-antimicrobials-with-therapeutic-potential-against-methicillin-resistant-staphylococcus-aureus-mrsa
#1
Shuimu Lin, Jun-Jie Koh, Thet Tun Aung, Wan Ling Wendy Sin, Fanghui Lim, Lin Wang, Rajamani Lakshminarayanan, Lei Zhou, Donald T H Tan, Derong Cao, Roger W Beuerman, Li Ren, Shouping Liu
A new series of semisynthetic flavone-based small molecules mimicking antimicrobial peptides has been designed from natural icaritin to combat drug-resistant Gram-positive bacterial infections. Compound 6 containing two arginine residues exhibited excellent antibacterial activity against Gram-positive bacteria, including MRSA, and very low toxicity to mammalian cells, resulting in a high selectivity of more than 511, comparable to that of several membrane-active antibiotics in clinical trials. Our data show for the first time that icaritin derivatives effectively kill bacteria...
June 21, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28634393/a-small-molecule-ds44170716-inhibits-ca-2-induced-mitochondrial-permeability-transition
#2
Naohiro Kon, Atsushi Satoh, Naoki Miyoshi
Mitochondria are involved in a variety of physiological and pathological processes. Ca(2+) uptake is one of the important functions of the organelle for maintenance of cellular Ca(2+) homeostasis. In pathological conditions such as ischemia reperfusion injury, Ca(2+) overload into mitochondria induces mitochondrial permeability transition (MPT), a critical step for cell death. Because inhibition of MPT is a promising approach to protecting cells and organs, it is important for drug discovery to identify novel chemicals or mechanisms to inhibit MPT...
June 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28632878/identification-of-novel-g-protein-coupled-receptor-143-ligands-as-pharmacologic-tools-for-investigating-x-linked-ocular-albinism
#3
Elisabetta De Filippo, Prashiela Manga, Anke C Schiedel
Purpose: GPR143 regulates melanosome biogenesis and organelle size in pigment cells. The mechanisms underlying receptor function remain unclear. G protein-coupled receptors (GPCRs) are excellent pharmacologic targets; thus, we developed and applied a screening approach to identify potential GPR143 ligands and chemical modulators. Methods: GPR143 interacts with β-arrestin; we therefore established a β-arrestin recruitment assay to screen for compounds that modulate activity...
June 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/28630638/cichorium-intybus-l-promotes-intestinal-uric-acid-excretion-by-modulating-abcg2-in-experimental-hyperuricemia
#4
Yu Wang, Zhijian Lin, Bing Zhang, Anzheng Nie, Meng Bian
BACKGROUND: Excessive production and/or reduced excretion of uric acid could lead to hyperuricemia, which could be a major cause of disability. Hyperuricemia has received increasing attention in the last few decades due to its global prevalence. Cichorium intybus L., commonly known as chicory, is a perennial herb of the asteraceae family. It was previously shown to exert potent hypouricemic effects linked with decreasing uric acid formation in the liver by down-regulating the activity of xanthine oxidase, and increasing uric acid excretion by up-regulating the renal OAT3 mRNA expression...
2017: Nutrition & Metabolism
https://www.readbyqxmd.com/read/28630155/haemolytic-actinoporins-interact-with-carbohydrates-using-their-lipid-binding-module
#5
Koji Tanaka, Jose M M Caaveiro, Koldo Morante, Kouhei Tsumoto
Pore-forming toxins (PFTs) are proteins endowed with metamorphic properties that enable them to stably fold in water solutions as well as in cellular membranes. PFTs produce lytic pores on the plasma membranes of target cells conducive to lesions, playing key roles in the defensive and offensive molecular systems of living organisms. Actinoporins are a family of potent haemolytic toxins produced by sea anemones vigorously studied as a paradigm of α-helical PFTs, in the context of lipid-protein interactions, and in connection with nanopore technologies...
August 5, 2017: Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences
https://www.readbyqxmd.com/read/28629128/interactions-between-a-heparin-trisaccharide-library-and-fgf-1-analyzed-by-nmr-methods
#6
María José García-Jiménez, Sergio Gil-Caballero, Ángeles Canales, Jesús Jiménez-Barbero, José L de Paz, Pedro M Nieto
FGF-1 is a potent mitogen that, by interacting simultaneously with Heparan Sulfate Glycosaminoglycan HSGAG and the extracellular domains of its membrane receptor (FGFR), generates an intracellular signal that finally leads to cell division. The overall structure of the ternary complex Heparin:FGF-1:FGFR has been finally elucidated after some controversy and the interactions within the ternary complex have been deeply described. However, since the structure of the ternary complex was described, not much attention has been given to the molecular basis of the interaction between FGF-1 and the HSGAG...
June 17, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28627652/eriodictyol-7%C3%A2-o%C3%A2-%C3%AE-%C3%A2-d-glucopyranoside-from-coreopsis%C3%A2-tinctoria-nutt-ameliorates-lipid-disorders-via-protecting-mitochondrial-function-and-suppressing-lipogenesis
#7
Yuyan Liang, Hai Niu, Limei Ma, Dan Du, Li Wen, Qing Xia, Wen Huang
Coreopsis tinctoria (snow chrysanthemum) has been reported to exert antihyperlipidemic effects. The present study aimed to identify the active compounds of Coreopsis tinctoria and to investigate the molecular mechanisms underlying its effects on lipid dysregulation by measuring lipid levels, reactive oxygen species, lipid peroxidation and fatty acid synthesis. The present results demonstrated that snow chrysanthemum aqueous extracts significantly reduced serum lipid levels and oxidative stress in vivo. The main compounds that were isolated were identified as flavanomarein (compound 1) and eriodictyol 7‑O‑β‑D glucopyranoside (compound 2)...
June 9, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28626428/molecular-surgery-concept-from-bench-to-bedside-a-focus-on-trpv1-pain-sensing-neurons
#8
REVIEW
László Pecze, Béla Viskolcz, Zoltán Oláh
"Molecular neurosurgery" is emerging as a new medical concept, and is the combination of two partners: (i) a molecular neurosurgery agent, and (ii) the cognate receptor whose activation results in the selective elimination of a specific subset of neurons in which this receptor is endogenously expressed. In general, a molecular surgery agent is a selective and potent ligand, and the target is a specific cell type whose elimination is desired through the molecular surgery procedure. These target cells have the highest innate sensitivity to the molecular surgery agent usually due to the highest receptor density being in their plasma membrane...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28625734/synthesis-and-cardiomyocyte-protection-activity-of-crocetin-diamide-derivatives
#9
Jin Gao, Ming Chen, Xue-Cong Ren, Xiao-Bo Zhou, Qiang Shang, Wen-Qi Lu, Pei Luo, Zhi-Hong Jiang
A series of novel diamide derivatives (2-8) of crocetin (1) were synthesized and evaluated for their cardioprotective activity in vitro. Using well-established model of hypoxia-induced injury in H9c2 cells, we investigated the effects of 9 compounds and positive drug nicorandil on cellular cytotoxicity by MTT assay, mitochondrial viable staining, LDH activity and mitochondrial membrane potential (MMP). Among the new derivatives, compounds 3 and 4 with good liposolubility showed significantly potent activity than crocetin (1) against hypoxia-induced cytotoxicity...
June 15, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28623355/epigenetic-and-antitumor-effects-of-platinum-iv-octanoato-conjugates
#10
Vojtech Novohradsky, Ilaria Zanellato, Cristina Marzano, Jitka Pracharova, Jana Kasparkova, Dan Gibson, Valentina Gandin, Domenico Osella, Viktor Brabec
We present the anticancer properties of cis, cis, trans-[Pt(IV)(NH3)2Cl2(OA)2] [Pt(IV)diOA] (OA = octanoato), Pt(IV) derivative of cisplatin containing two OA units appended to the axial positions of a six-coordinate Pt(IV) center. Our results demonstrate that Pt(IV)diOA is a potent cytotoxic agent against many cancer cell lines (the IC50 values are approximately two orders of magnitude lower than those of clinically used cisplatin or Pt(IV) derivatives with biologically inactive axial ligands). Importantly, Pt(IV)diOA overcomes resistance to cisplatin, is significantly more potent than its branched Pt(IV) valproato isomer and exhibits promising in vivo antitumor activity...
June 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28623332/interaction-of-the-antimicrobial-peptide-aurein-1-2-and-charged-lipid-bilayer
#11
Durgesh K Rai, Shuo Qian
Aurein 1.2 is a potent antimicrobial peptide secreted by frog Litoria aurea. As a short membrane-active peptide with only 13 amino acids in sequence, it has been found to be residing on the surface of lipid bilayer and permeabilizing bacterial membranes at high concentration. However, the detail at the molecular level is largely unknown. In this study, we investigated the action of Aurein 1.2 in charged lipid bilayers composed of DMPC/DMPG. Oriented Circular Dichroism results showed that the peptide was on the surface of lipid bilayer regardless of the charged lipid ratio...
June 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28621538/discovery-of-highly-potent-and-selective-small-molecule-reversible-factor-d-inhibitors-demonstrating-alternative-complement-pathway-inhibition-in-vivo
#12
Edwige Lorthiois, Karen Anderson, Anna Vulpetti, Olivier Rogel, Frederic Cumin, Nils Ostermann, Stefan Steinbacher, Aengus Mac Sweeney, Omar Delgado, Sha-Mei Liao, Stefan Randl, Simon Rüdisser, Solene Dussauge, Kamal Fettis, Laurence Kieffer, Andrea de Ekernez, Louis Yang, Constanze Hartwieg, Upendra A Argikar, Laura R LaBonte, Ronald Newton, Viral Kansara, Stefanie Flohr, Ulrich Hommel, Bruce Jaffee, Jürgen Maibaum
The highly specific S1 serine protease Factor D (FD) plays a central role in the amplification of the complement alternative pathway (AP) of the innate immune system. Genetic associations in humans have implicated AP activation in age-related macular degeneration (AMD), and AP dysfunction predisposes individuals to disorders such as paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS). The combination of structure-based hit identification and subsequent optimization of the center (S)-proline-based lead 7 has led to the discovery of non-covalent reversible and selective human Factor D (FD) inhibitors with drug-like properties...
June 16, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28620137/biological-specificity-of-cdk4-6-inhibitors-dose-response-relationship-in-vivo-signaling-and-composite-response-signature
#13
Erik S Knudsen, Jack Hutcheson, Paris Vail, Agnieszka K Witkiewicz
Recently developed potent and selective CDK4/6 inhibitors fall into two classes based on structure and toxicity profiles in clinical studies. One class, exemplified by palbociclib and ribociclib, exhibits neutropenia as a dose-limiting toxicity and requires discontinuous dosing. In contrast, the structurally distinct CDK4/6 inhibitor abemaciclib is dosed continuously, and has diarrhea and fatigue as dose-limiting toxicities. In preclinical models, palbociclib has been extensively studied and induces cell cycle inhibition in an RB-dependent manner...
June 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/28617852/dicumarol-inhibits-pdk1-and-targets-multiple-malignant-behaviors-of-ovarian-cancer-cells
#14
Wenjia Zhang, Jing Su, Huadan Xu, Shanshan Yu, Yanan Liu, Yong Zhang, Liankun Sun, Ying Yue, Xiaoli Zhou
Pyruvate dehydrogenase kinase 1 (PDK1) is overexpressed in ovarian cancer and thus is a promising anticancer therapeutic target. Our previous work suggests that coumarin compounds are potential inhibitors of PDKs. In this study, we used the ovarian cancer cell line SKOV3 as the model system and examined whether dicumarol (DIC), a coumarin compound, could inhibit ovarian cancer through targeting PDK1. We showed that DIC potently inhibited the kinase activity of PDK1, shifted the glucose metabolism from aerobic glycolysis to oxidative phosphorylation, generated a higher level of reactive oxygen species (ROS), attenuated the mitochondrial membrane potential (MMP), induced apoptosis, and reduced cell viability in vitro...
2017: PloS One
https://www.readbyqxmd.com/read/28615203/phosphorylation-of-serine-225-in-hepatitis-c-virus-ns5a-regulates-protein-protein-interactions
#15
Niluka Goonawardane, Anna Gebhardt, Christopher Bartlett, Andreas Pichlmair, Mark Harris
Hepatitis C virus (HCV) non-structural protein 5A (NS5A) is a phosphoprotein that plays key, yet poorly defined, roles in both virus genome replication and virion assembly/release. It has been proposed that differential phosphorylation could act as a switch to regulate the various functions of NS5A, however the mechanistic details of the role of this post-translational modification in the virus life cycle remains obscure. We previously reported (Ross-Thriepland et al, 2015) a role for phosphorylation at serine 225 (S225) of NS5A in the regulation of JFH-1 (genotype 2a) genome replication...
June 14, 2017: Journal of Virology
https://www.readbyqxmd.com/read/28612503/distinctive-in-vitro-signal-transduction-profile-of-nlx-112-a-potent-and-efficacious-serotonin-5-ht1a-receptor-agonist
#16
Adrian Newman-Tancredi, Jean-Claude Martel, Cristina Cosi, Peter Heusler, Fabrice Lestienne, Mark A Varney, Didier Cussac
OBJECTIVES: NLX-112 (befiradol, F13640) is a selective serotonin 5-HT1A receptor agonist. Although it has been tested in vivo, little has been reported on its in vitro signal transduction profile. METHODS: NLX-112 was tested on G-protein activation, inhibition of adenylyl cyclase, ERK1/2 phosphorylation (pERK) and receptor internalization in recombinant cell lines. NLX-112 was also tested on G-protein activation in rat hippocampal membranes. Gα subunit mRNA expression in cell lines and rat brain tissue was quantified by quantitative PCR...
June 14, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28611436/antibacterial-and-detoxifying-activity-of-nz17074-analogues-with-multi-layers-of-selective-antimicrobial-actions-against-escherichia-coli-and-salmonella-enteritidis
#17
Na Yang, Xuehui Liu, Da Teng, Zhanzhan Li, Xiumin Wang, Ruoyu Mao, Xiao Wang, Ya Hao, Jianhua Wang
NZ17074 (N1), an arenicin-3 derivative isolated from the lugworm, has potent antibacterial activity and is cytotoxic. To reduce its cytotoxicity, seven N1 analogues with different structures were designed by changing their disulfide bonds, hydrophobicity, or charge. The "rocket" analogue-N2 and the "kite" analogue-N6 have potent activity and showed lower cytotoxicity in RAW264.7 cells than N1. The NMR spectra revealed that N1, N2, and N6 adopt β-sheet structures stabilized by one or two disulfide bonds. N2 and N6 permeabilized the outer/inner membranes of E...
June 13, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28607172/tweety-homologue-1-drives-brain-colonization-of-gliomas
#18
Erik Jung, Matthias Osswald, Jonas Blaes, Benedikt Wiestler, Felix Sahm, Torsten Schmenger, Gergely Solecki, Katrin Deumelandt, Felix T Kurz, Ruifan Xie, Sophie Weil, Oliver Heil, Carina Thomé, Miriam Gömmel, Mustafa Syed, Peter Häring, Peter E Huber, Sabine Heiland, Michael Platten, Andreas von Deimling, Wolfgang Wick, Frank Winkler
Early and progressive colonization of the healthy brain is one hallmark of diffuse gliomas, including glioblastomas. Recently we have discovered ultra-long (> ten to hundreds of microns) membrane protrusions (tumor microtubes, TMs) that are extended by glioma cells. TMs were associated with the capacity of glioma cells to effectively invade the brain, and proliferate. Moreover, TMs were also used by some tumor cells to interconnect to one large, resistant multicellular network. Here, we performed a correlative gene expression microarray and in vivo imaging analysis, and identified novel molecular candidates for TM formation and function...
June 8, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28606819/cytotoxicity-of-cerastes-cerastes-snake-venom-involvement-of-imbalanced-redox-status
#19
Hayet Kebir-Chelghoum, Fatima Laraba-Djebari
Envenomation caused by Cerastes cerastes snake venom is characterized by a local and a systemic tissue damage due to myonecrosis, hemorrhage, edema and acute muscle damage. The present study aimed to evaluate the relationship between the pro/anti-oxidants status and the cytotoxicity of C. cerastes snake venom. The in vivo cytotoxicity analysis was undertaken by the injection of C. cerastes venom (48μg/20g body weight) by i.p. route, mice were then sacrificed at 3, 24 and 48h post injection, organs were collected for further analysis...
June 9, 2017: Acta Tropica
https://www.readbyqxmd.com/read/28606812/novel-ctl-epitopes-identified-through-a-y-pestis-proteome-wide-analysis-in-the-search-for-vaccine-candidates-against-plague
#20
Anat Zvi, Shahar Rotem, Ayelet Zauberman, Uri Elia, Moshe Aftalion, Erez Bar-Haim, Emanuelle Mamroud, Ofer Cohen
The causative agent of Plague, Yersinia pestis, is a highly virulent pathogen and a potential bioweapon. Depending on the route of infection, two prevalent occurrences of the disease are known, bubonic and pneumonic. The latter has a high fatality rate. In the absence of a licensed vaccine, intense efforts to develop a safe and efficacious vaccine have been conducted, and humoral-driven subunit vaccines containing the F1 and LcrV antigens are currently under clinical trials. It is well known that a cellular immune response might have an essential additive value to immunity and protection against Y...
June 9, 2017: Vaccine
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