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Matthew V Helliwell, Yihong Zhang, Aziza El Harchi, Chunyun Du, Jules C Hancox, Christopher E Dempsey
Cardiac potassium channels encoded by human Ether-à-go-go Related Gene (hERG) are major targets for structurally diverse drugs associated with acquired long QT syndrome. This study characterized hERG channel inhibition by a minimally structured high affinity hERG inhibitor, Cavalli-2, composed of three phenyl groups linked by polymethylene spacers around a central amino group, chosen to probe the spatial arrangement of side chain groups in the high-affinity drug binding site of the hERG pore. hERG current (IhERG ) recorded at physiological temperature from HEK 293 cells was inhibited with an IC50 of 35...
March 15, 2018: Journal of Biological Chemistry
Sheng Huang, Jie Gao, Jiangfeng You, Yanan Liang, Kexing Guan, Siqi Yan, Meiqi Zhan, Zhenming Yang
Aluminum (Al) toxicity in acidic soils affects crop production worldwide. C2 H2 -type zinc finger transcription factor STOP1/ART1-mediated expression of Al tolerance genes has been shown to be important for Al resistance in Arabidopsis , rice and other crop plants. Here, we identified and characterized four STOP1-like proteins (SbSTOP1a, SbSTOP1b, SbSTOP1c, and SbSTOP1d) in sweet sorghum, a variant of grain sorghum ( Sorghum bicolor L.). Al induced the transcription of the four SbSTOP1 genes in both time- and Al concentration-dependent manners...
2018: Frontiers in Plant Science
Silvia Revoltella, Giorgia Baraldo, Birgit Waltenberger, Stefan Schwaiger, Philipp Kofler, Julia Moesslacher, Astrid Huber-Seidel, Konrad Pagitz, Roland Kohl, Pidder Jansen-Duerr, Hermann Stuppner
NADPH oxidase 4 (Nox4) has recently been implicated as driving force in cellular senescence. Thus, there is growing interest to develop Nox4 inhibitors, which might be valuable agents for cosmeceutical applications. Alpine plants represent a valuable source for the identification of novel bioactive natural products with anti-ageing effects, especially substances that protect plants against UV radiation, which is also known to contribute to the ageing of human skin. Therefore, the aim of this study was to identify novel Nox4 inhibitors from alpine plants...
March 14, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Sylwia Bloch, Bożena Nejman-Faleńczyk, Karolina Pierzynowska, Ewa Piotrowska, Alicja Węgrzyn, Christelle Marminon, Zouhair Bouaziz, Pascal Nebois, Joachim Jose, Marc Le Borgne, Luciano Saso, Grzegorz Węgrzyn
Oxidative stress may be the major cause of induction of Shiga toxin-converting (Stx) prophages from chromosomes of Shiga toxin-producing Escherichia coli (STEC) in human intestine. Thus, we aimed to test a series of novel antioxidant compounds for their activities against prophage induction, thus, preventing pathogenicity of STEC. Forty-six compounds (derivatives of carbazole, indazole, triazole, quinolone, ninhydrine, and indenoindole) were tested. Fifteen of them gave promising results and were further characterized...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
Linda E Flinterman, Karin Hek, Joke C Korevaar, Liset van Dijk
Governments have several options to reduce the increasing costs of health care, including restrictions for the reimbursement of medicines. Next to the intended effect of reduced costs for medicines, reimbursement restriction can have unintended effects such as patients refraining from their treatment which may lead to health problems and increased use of health care. An example of a reimbursement restriction is the one for proton pump inhibitors (PPIs) that became effective in the Netherlands in January 2012...
2018: Frontiers in Public Health
Shaoyi Cai, Gengzheng Zhu, Xiaohong Cen, Jingjie Bi, Jingru Zhang, Xiaoshan Tang, Kun Chen, Kui Cheng
Toll-like receptor 2 (TLR2) can recognize pathogen-associated molecular patterns to defense against invading organisms and has been represents an attractive therapeutic target. Until today, none TLR2 small molecule antagonist have been developed in clinical trial. Herein, we designed and synthesized 50 N-benzylideneaniline compounds with the help of CADD. And subsequent in vitro studies leading to the optimized compound SMU-A0B13 with most potent inhibitory activity to TLR2 (IC50 =18.21 ± 0.87 μM)...
March 10, 2018: Bioorganic & Medicinal Chemistry
Abidullah Khan, Bai Hongliang, Enqi Liu, Chen Mingxia, Yu Chunshui, Rai Wang, Khan Amin, Bai Zhuanli
Studies have shown that skin exposure to ultraviolet radiation (UVR) results in the formation of reactive oxygen species (ROS), thus altering the cellular function. The human epidermal skin layer is mainly composed of keratinocytes, which is damaged by UV-B radiation induced intracellular oxidative stress. Neferine is an alkaloid extract from lotus seed embryos, and its photoprotective action against UV-B produced oxidative damage in human epidermal keratinocytes (HEKs) has never been proposed. Neferine inhibited UV-B mediated increase in ROS and malondialdehyde (MDA) levels in pretreated keratinocytes...
March 13, 2018: Journal of Dermatological Treatment
Kelley M Heffner, Qiong Wang, Deniz Baycin Hizal, Özge Can, Michael J Betenbaugh
Mammalian expression systems such as Chinese hamster ovary (CHO), mouse myeloma (NS0), and human embryonic kidney (HEK) cells serve a critical role in the biotechnology industry as the production host of choice for recombinant protein therapeutics. Most of the recombinant biologics are glycoproteins that contain complex oligosaccharide or glycan attachments representing a principal component of product quality. Both N-glycans and O-glycans are present in these mammalian cells, but the engineering of N-linked glycosylation is of critical interest in industry and many efforts have been directed to improve this pathway...
March 13, 2018: Advances in Biochemical Engineering/biotechnology
Kuo-Hsuan Chang, Guan-Chiun Lee, Chin-Chang Huang, Hung-Chou Kuo, Chiung-Mei Chen, Ya-Chin Hsiao, Hsuan-Chu Hsu, Ke-Jen Hsu, Chih-Hsin Lin, Chia Wen Chang, Guey-Jen Lee-Chen, Yih-Ru Wu
BACKGROUND: Mutations in the GRN (granulin precursor) are a frequent cause of frontotemporal dementia (FTD) and other atypical parkinsonian disorders. However, the frequency of GRN mutations in Asian patients with atypical parkinsonian disorders is still uncertain. METHODS: We screened GRN mutations by sequencing cDNA from 98 patients with FTD or atypical parkinsonian disorders. The functional properties of the identified mutation were evaluated by overexpression in human embryonic kidney (HEK)-293 cells...
February 28, 2018: Parkinsonism & related Disorders
Peng Yu, Lili Hu, Jinyan Xie, Sisi Chen, Lin Huang, Zixuan Xu, Xiao Liu, Qiongqiong Zhou, Ping Yuan, Xia Yan, Jiejin Jin, Yang Shen, Wengen Zhu, Linghua Fu, Qi Chen, Jianhua Yu, Jianxin Hu, Qing Cao, Rong Wan, Kui Hong
BACKGROUND: Cardiovascular complications are major causes of mortality and morbidity in diabetic patients. The mechanisms underlying the progression of diabetic heart (DH) to ventricular arrhythmias are unclear. O-linked GlcNAcylation (O-GlcNAc) is a reversible post-translational modification for the regulation of diverse cellular processes. The purpose of this study was to assess whether the cardiac voltage-gated sodium channel (Nav1.5) is subjected to O-linked GlcNAcylation (O-GlcNAc), which plays an essential role in DH-induced arrhythmias...
February 27, 2018: International Journal of Cardiology
Zafer Sahin, Merve Ertas, Barkın Berk, Sevde Nur Biltekin, Leyla Yurttas, Seref Demirayak
Steroidal and non-steroidal aromatase inhibitors target the suppression of estrogen biosynthesis in the treatment of breast cancer. Researchers have increasingly focused on developing non-steroidal derivatives for their potential clinical use avoiding steroidal side-effects. Non-steroidal derivatives generally have planar aromatic structures attached to the azole ring system. One part of this ring system comprises functional groups that inhibit aromatization through the coordination of the haem group of the aromatase enzyme...
February 27, 2018: Bioorganic & Medicinal Chemistry
Jeremy Streuli, Alan G Harris, Cecilia Cottiny, Florent Allagnat, Adrian F Daly, Eric Grouzmann, Karim Abid
BACKGROUND: Somatostatin analogs (SSAs) are first-line medical therapy for the treatment of acromegaly and neuroendocrine tumors that express somatostatin receptors (SSTR). Somatostatin suppresses secretion of a large number of hormones through the stimulation of the five SSTR. However, unbalanced inhibition of secretion as observed with the highly potent SSAs pasireotide causes hyperglycaemia mainly by inhibiting insulin secretion. In contrast, AP102 a new SSAs has neutral effect on blood glucose while suppressing GH secretion...
March 2, 2018: Neuropeptides
Shailja Kumar, Virendra Kumar Meena, Puja Panwar Hazari, Surinder Kumar Sharma, Rakesh Kumar Sharma
We report here, reverse micelle mediated synthesis of multifunctional dextran (dex) coated Gd2 O3 nanoparticles (NPs) carrying rose bengal (RB) dye for magnetic resonance and optical imaging. The diameter of these RB attached dex coated Gd2 O3 NPs (Gd-dex-RB NPs) was found to be ~17 nm as measured by TEM. NMR line broadening effect on the surrounding water protons affirmed the paramagnetic nature of these NPs. Optical properties of Gd-dex-RB NPs were validated by UV-Vis and fluorescence spectroscopy. Time dependent release profile of RB from NPs at two different pH of 7...
March 6, 2018: European Journal of Pharmaceutical Sciences
Merve Ertas, Zafer Sahin, Barkin Berk, Leyla Yurttas, Sevde N Biltekin, Seref Demirayak
Drugs used in breast cancer treatments target the suppression of estrogen biosynthesis. During this suppression, the main goal is to inhibit the aromatase enzyme that is responsible for the cyclization and structuring of estrogens either with steroid or non-steroidal-type inhibitors. Non-steroidal derivatives generally have a planar aromatic structure attached to the triazole ring system in their structures, which inhibits hydroxylation reactions during aromatization by coordinating the heme group. Bioisosteric replacement of the triazole ring system and development of aromatic/cyclic structures of the side chain can increase the selectivity for aromatase enzyme inhibition...
March 9, 2018: Archiv der Pharmazie
Yasin Tülüce, Bewar Ali Ahmed, İsmail Koyuncu, Mustafa Durgun
Colorectal cancer (CRC) is the third most common tumor, malignant and has developed one of the main reasons of cancer mortality. According to studies conducted recently; carbonic anhydrase 9 (CAIX) is an especially attractive target for cancer therapy, in part since it is limited way expressed in normal tissues on the other hand in a wide variety of solid neoplasia are overexpressed. The aim of this study was to appreciate the effects of CAIX inhibitor, namely novel synthesized sulfonamide derivative (H-4i) with high affinity for CAIX, in CAIX-positive human colorectal cancer cell (HT-29) and CAIX-negative human normal embryonic kidney cell line (HEK-293)...
March 9, 2018: Journal of Bioenergetics and Biomembranes
Rabia Kouser, Arti Vashist, Md Zafaryab, Moshahid A Rizvi, Sharif Ahmad
The synergistic contributions of nanofillers and polymer matrix induce remarkable properties in nanocomposite hydrogels. Present article reports the facile synthesis of biocompatible nanocomposite hydrogels using microporous multi wall carbon nanotubes (MWCNTs) dispersed chitosan (CH)-Acrylonitrile (AN), N,N'-methylenebisacrylamide (MBAAm) and linseed polyol through solution blending method. Polyol and N,N'-methylenebisacrylamide (MBAAm) was used as the crosslinking agent. The structural characterization and formation of highly crosslinked network with dendrimer morphology was confirmed by FT-IR and scanning electron microscope (SEM) analysis...
March 1, 2018: Materials Science & Engineering. C, Materials for Biological Applications
Anna Koziorowska, Maria Romerowicz-Misielak, Przemysław Sołek, Marek Koziorowski
The exposure to extremely low frequency electromagnetic field (ELF-EMF) may result in various changes at the cellular level. To identify the effect of ELF-EMF exposure on viability of cells, cancer cells (U87-MG; 143B) and noncancerous cells (BJ; HEK) in exponential growth phase were exposed or sham-exposed to different values of frequency (2, 20, 30, 50 and 60 Hz), different shapes (sinusoidal, square and triangular) and time of exposure (0.5, 1, 2, 3 h) to electromagnetic field. After exposure, viability of cells was detected by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT)...
March 7, 2018: Electromagnetic Biology and Medicine
Nan Xie, Nicholas Matigian, Tharindu D Vithanage, Kye Gregory, Zeyad D Nassar, Peter J Cabot, Paul Nicholas Shaw, Carl Mj Kirkpatrick, Kim-Anh Lê Cao, David Sturgess, Marie-Odile Parat
PURPOSE: To investigate the potential interplay between opioid analgesia and tumour metastasis through modulation of μ opioid receptor (MOR), Toll-like receptor 4 (TLR4) activation, and matrix degradation potential. EXPERIMENTAL DESIGN: Plasma samples were collected from 60 patients undergoing elective lower limb joint replacement pre-operatively and at 3, 6 and 24 h after surgery; pain scores were documented at the same time points. Opioid administration was recorded and converted into morphine IV equivalents...
March 6, 2018: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
Tarunkumar Hemraj Madne, Mark Edward Carl Dockrell
The interactions of the extracellular matrix (ECM) proteins with cells strongly regulate cell behaviour. The glomerular basement membrane (GBM) is a dynamic structure made up of protein secreted by endothelial cells and podocyte. These proteins could regulate the behaviour of these cells in health and diseases. Extra Domain A + Fn (EDA+Fn) is an alternatively spliced form of Fibronectin (Fn) recently identified in GBM and a recognised marker of various pathologies. In this study for the first time, we have investigated the responses of human podocytes cultured on different composition of GBM proteins which are cellular Fn (EDA+), plasma Fn (EDA-) and collagen IV...
February 28, 2018: Cellular and Molecular Biology
Ismail Koyuncu
In the treatment of cancer, which remains a fatal disease, increasingly successful treatment rates of alternative therapies using the power of plants have directed the scientific world towards natural plant resources. This study aimed to examine the anti-cancer and antioxidant properties and identify the phenolic content of the methanolic extract obtained from Artemisia absinthium L. (AR) species, which is used as folk-medicine. The antioxidant activity of the extract was investigated using total phenolics, flavonoids, ABTS and CUPRAC methods...
February 28, 2018: Cellular and Molecular Biology
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