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https://www.readbyqxmd.com/read/29677485/octapeptins-lipopeptide-antibiotics-against-multidrug-resistant-superbugs
#1
Antoine Abou Fayad, Jennifer Herrmann, Rolf Müller
Antimicrobial resistance is increasing at an alarming rate. Polymyxin, one of the few antibiotics of last resort, is heavily affected. In this issue of Cell Chemical Biology, Velkov et al. (2018) present a promising alternative: octapeptin lipopeptide antibiotics active against multidrug- and extensively drug-resistant Gram-negative bacteria, which might help overcoming resistance toward polymyxins.
April 19, 2018: Cell Chemical Biology
https://www.readbyqxmd.com/read/29677376/endothelial-protein-c-targeting-liposomes-show-enhanced-uptake-and-improved-therapeutic-efficacy-in-human-retinal-endothelial-cells
#2
Anthoula Arta, Anne Z Eriksen, Fredrik Melander, Paul Kempen, Michael Larsen, Thomas L Andresen, Andrew J Urquhart
Purpose: To determine whether human retinal endothelial cells (HRECs) express the endothelial cell protein C receptor (EPCR) and to realize its potential as a targeting moiety by developing novel single and dual corticosteroid-loaded functionalized liposomes that exhibit both enhanced uptake by HRECs and superior biologic activity compared to nontargeting liposomes and free drug. Methods: EPCR expression of HRECs was investigated through flow cytometry and Western blot assays...
April 1, 2018: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/29677130/lipid-biosynthesis-as-an-antifungal-target
#3
REVIEW
Jiao Pan, Cuiting Hu, Jae-Hyuk Yu
Lipids, commonly including phospholipids, sphingolipids, fatty acids, sterols, and triacylglycerols (TAGs), are important biomolecules for the viability of all cells. Phospholipids, sphingolipids, and sterols are important constituents of biological membranes. Many lipids play important roles in the regulation of cell metabolism by acting as signaling molecules. Neutral lipids, including TAGs and sterol esters (STEs), are important storage lipids in cells. In view of the importance of lipid molecules, this review briefly summarizes the metabolic pathways for sterols, phospholipids, sphingolipids, fatty acids, and neutral lipids in fungi and illustrates the differences between fungal and human (or other mammalian) cells, especially in relation to lipid biosynthetic pathways...
April 20, 2018: Journal of Fungi (Basel, Switzerland)
https://www.readbyqxmd.com/read/29677107/imprinted-oxide-and-mip-oxide-hybrid-nanomaterials-for-chemical-sensors-%C3%A2
#4
REVIEW
Adeel Afzal, Franz L Dickert
The oxides of transition, post-transition and rare-earth metals have a long history of robust and fast responsive recognition elements for electronic, optical, and gravimetric devices. A wide range of applications successfully utilized pristine or doped metal oxides and polymer-oxide hybrids as nanostructured recognition elements for the detection of biologically relevant molecules, harmful organic substances, and drugs as well as for the investigative process control applications. An overview of the selected recognition applications of molecularly imprinted sol-gel phases, metal oxides and hybrid nanomaterials composed of molecularly imprinted polymers (MIP) and metal oxides is presented herein...
April 20, 2018: Nanomaterials
https://www.readbyqxmd.com/read/29676924/paclitaxel-loaded-ph-sensitive-liposome-new-insights-on-structural-and-physicochemical-characterization
#5
Liziane Oliveira Fonseca Monteiro, Angelo Malachias, Gwenaelle Pound-Lana, Rogerio Magalhães-Paniago, Vanessa Carla Furtado Mosqueira, Mônica Cristina Oliveira, Andre Branco de Barros, Elaine Amaral Leite
A long-circulating and pH-sensitive liposome containing PTX (SpHL-PTX) was recently developed by our group. Once at an acidic environment, e.g. tumor, these liposomes undergo destabilization releasing the encapsulated drug. In this way, the aim of this study was evaluate the molecular and supramolecular interactions between the lipid bilayer and PTX in similar biological environment conditions. High sensitivity analyses of SpHL-PTX structures were obtained by small angle X-ray scattering (SAXS) technique combined with other techniques such as DLS, AF4, TEM and HPLC...
April 20, 2018: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/29676591/a-retrospective-observational-study-on-biological-drug-treatment-in-a-daily-practice-serving-patients-with-psoriasis-in-japan
#6
Chika Ohata, Bungo Ohyama, Aya Nanri, Takako Shintani, Takekuni Nakama
BACKGROUND: In Japan, more than 5 years have passed since emergence of the first 3 biologics, infliximab, adalimumab, and ustekinumab, became available in daily practice; however, no data for drug survival was reported from Japan. OBJECTIVE: To study the long-term drug survival of infliximab, adalimumab, and ustekinumab used for Japanese psoriatic patients. METHODS: We retrieved data on all patients treated with biological agents and calculated the long-term drug survival for infliximab, adalimumab, and ustekinumab using our psoriasis registry (Kurume Psoriasis Registry: KURUPR) consisted of 343 patients by the end of March 2017...
April 20, 2018: Journal of Dermatological Treatment
https://www.readbyqxmd.com/read/29676564/parasites-under-the-spotlight-applications-of-vibrational-spectroscopy-to-malaria-research
#7
David Perez-Guaita, Katarzyna M Marzec, Andrew Hudson, Corey Evans, Tatyana Chernenko, Christian Matthäus, Milos Miljkovic, Max Diem, Philip Heraud, Jack S Richards, Dean Andrew, David A Anderson, Christian Doerig, Jose Garcia-Bustos, Don McNaughton, Bayden R Wood
New technologies to diagnose malaria at high sensitivity and specificity are urgently needed in the developing world where the disease continues to pose a huge burden on society. Infrared and Raman spectroscopy-based diagnostic methods have a number of advantages compared with other diagnostic tests currently on the market. These include high sensitivity and specificity for detecting low levels of parasitemia along with ease of use and portability. Here, we review the application of vibrational spectroscopic techniques for monitoring and detecting malaria infection...
April 20, 2018: Chemical Reviews
https://www.readbyqxmd.com/read/29676523/characterization-of-low-abundance-species-in-the-active-pharmaceutical-ingredient-of-cigb-300-a-clinical-grade-anticancer-synthetic-peptide
#8
Hilda Garay, Luis Ariel Espinosa, Yasser Perera, Aniel Sánchez, David Diago, Silvio E Perea, Vladimir Besada, Osvaldo Reyes, Luis Javier González
CIGB-300 is a first-in-class synthetic peptide-based drug of 25 amino acids currently undergoing clinical trials in cancer patients. It contains an amidated disulfide cyclic undecapeptide fused to the TAT cell-penetrating peptide through a beta-alanine spacer. CIGB-300 inhibits the CK2-mediated phosphorylation leading to apoptosis of tumor cells in vitro, and in vivo in cancer patients. Despite the clinical development of CIGB-300, the characterization of peptide-related impurities present in the active pharmaceutical ingredient has not been reported earlier...
April 20, 2018: Journal of Peptide Science: An Official Publication of the European Peptide Society
https://www.readbyqxmd.com/read/29676414/thioacids-synthons-for-amide-bond-formation-and-ligation-reactions-assembly-of-peptides-and-peptidomimetics
#9
REVIEW
Narendra N, Vishwanatha M Thimmalapura, Basavaprabhu Hosamani, Girish Prabhu, L Roopesh Kumar, Vommina V Sureshbabu
The synthesis of α-amino thioacids and peptide thioacids and their applications in chemoselective amide bond formation, ligation of peptides/proteins/glycopeptides and synthesis of peptidomimetics are reviewed. A variety of successful methods including both C-terminal and N-terminal activations for the coupling of α-amino thioacids and peptide thioacids have ascertained the thioacid-based protocol as a benign alternative to some of the traditional methods of amide/peptide bond formation which employs carboxyl activation...
April 20, 2018: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/29676229/viral-induced-oxidative-and-inflammatory-response-in-alzheimer-s-disease-pathogenesis-with-identification-of-potential-drug-candidates-a-systematic-review-using-systems-biology-approach
#10
Puneet Talwar, Renu Gupta, Suman Kushwaha, Rachna Agarwal, Luciano Saso, Shrikant Kukreti, Ritushree Kukreti
Alzheimer's disease (AD) is genetically complex with multifactorial etiology. Here, we aim to identify the potential viral pathogens leading to aberrant inflammatory and oxidative stress response in AD along with potential drug candidates using systems biology approach. We retrieved protein interactions of amyloid precursor protein (APP) and tau protein (MAPT) from NCBI and genes for oxidative stress from NetAge, for inflammation from NetAge and InnateDB databases. Genes implicated in aging were retrieved from GenAge database and two GEO expression datasets...
April 19, 2018: Current Neuropharmacology
https://www.readbyqxmd.com/read/29676228/glaucoma-pathogenesis-and-neurotrophins-focus-on-the-molecular-and-genetic-basis-for-therapeutic-prospects
#11
Nitin Chitranshi, Yogita Dheer, Mojdeh Abbasi, Yuyi You, Stuart L Graham, Vivek Gupta
BACKGROUND: Retinal ganglion cell (RGC) degeneration is a major feature of glaucoma pathology. Neuroprotective approaches that delay or halt the progression of RGC loss are needed to prevent vision loss which can occur even after conventional medical or surgical treatments to lower intraocular pressure. OBJECTIVE: The aim of this review was to examine the progress in genetics and cellular mechanisms associated with endoplasmic reticulum (ER) stress, RGC dysfunction and cell death pathways in glaucoma...
April 19, 2018: Current Neuropharmacology
https://www.readbyqxmd.com/read/29676195/in-vitro-inhibitory-effects-of-sophocarpine-on-human-liver-cytochrome-p450-enzymes
#12
Jingwei Zhang, Chuansheng Li, Jingfa Zhang, Fan Zhang
1. Sophocarpine is a biologically active component isolated from the foxtail-like sophora herb and seed that is often orally administered for the treatment of cancer and chronic bronchial asthma. However, whether sophocarpine affects the activity of human liver cytochrome P450 (CYP) enzymes remains unclear. 2. In this study, the inhibitory effects of sophocarpine on the eight human liver CYP isoforms (CYP1A2, 3A4, 2A6, 2E1, 2D6, 2C9, 2C19, and 2C8) were investigated in vitro using human liver microsomes (HLMs)...
April 20, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29676189/association-between-clinical-factors-and-dose-modification-strategies-in-the-treatment-with-ustekinumab-for-moderate-to-severe-plaque-psoriasis
#13
Rosa M Romero-Jimenez, Vicente Escudero-Vilaplana, Ofelia Baniandres Rodriguez, Estela García Martín, Ana Mateos Mayo, Maria Sanjurjo Saez
PURPOSE: The aim of this study was to identify clinical factors associated with dose reduction and dose escalation in the treatment with ustekinumab in patients with moderate to severe plaque psoriasis. MATERIALS AND METHODS: An observational, longitudinal and retrospective study was conducted using patients with moderate to severe plaque psoriasis. We reviewed clinical histories and variables were recorded on a database (patients' characteristics, pharmacotherapeutics, effectiveness and safety)...
April 20, 2018: Journal of Dermatological Treatment
https://www.readbyqxmd.com/read/29676153/quantifying-cellular-internalization-with-a-fluorescent-click-sensor
#14
Laura Ina Selby, Luigi Aurelio, Daniel Yuen, Bim Graham, Angus P R Johnston
The ability to determine the amount of material endocytosed by a cell is important for our understanding of cell biology and in the de-sign of effective carriers for drug delivery. To quantify internalization by fluorescence, the signal from material remaining on the cell sur-face must be differentiated from endocytosed material. Sensors for internalization offer advantages over traditional methods for achiev-ing this as they exhibit improved sensitivity, allow for multiple fluorescent markers to be used simultaneously, and are amenable to high throughput analysis...
April 20, 2018: ACS Sensors
https://www.readbyqxmd.com/read/29676151/activation-of-human-natural-killer-cells-by-graphene-oxide-templated-antibody-nanoclusters
#15
Christian Loftus, Mezida Saeed, Daniel M Davis, Iain E Dunlop
An emerging new paradigm is that immune cell activation is controlled by transient interactions between supramolecular assemblies of receptors and ligands. Current immunotherapy biologic pharmaceuticals that activate or desensitize NK cells are, however, individual molecules that do not replicate this nanoscale organization of proteins. Here, we use nanoscale graphene oxide (NGO) as a template to generate soluble nanoscale clusters of Natural Killer cell-activating antibodies. We control nanocluster size and molecular number to mimic reported values for cell surface proteins...
April 20, 2018: Nano Letters
https://www.readbyqxmd.com/read/29676112/-effect-of-animal-medicines-for-extinguishing-wind-to-arrest-convulsions-on-central-nervous-system-diseases
#16
REVIEW
Zhi-Jie Yu, Jin-Song Li, Wei Peng, Ping Wang, Liang Xiong, Yu-Jie Liu, Ying Xu, Tao Sun
The human health is seriously affected by central nervous system(CNS) diseases, but the pathogenesis of CNS diseases is still not completely clear. Currently, the drugs used to treat CNS diseases are mainly receptor modulators and neurotransmitter inhibitors, which have serious side effects; and there are short of drugs for treating CNS diseases clinically. Studies suggest that animal medicines mainly include protein, polypeptide and small-molecule compounds, and have such pharmacological effects in calming, resisting convulsions and improving brain tissues...
March 2018: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29676106/-medication-regularity-and-potential-targets-of-professor-xu-jing-fan-s-prescription-for-treating-ulcerative-colitis
#17
Li-Qin Ning, Bai Ye, Hong Shen, Wei-Min Lu, Dan-Hua Xu, Jing Yan, Chang Tan, De-Cai Tang
Ulcerative colitis (UC) is a chronic nonspecific inflammation mainly involving rectum and colon mucosa, which seriously affects the health and quality of life of patients, and is listed as one of modern refractory diseases by WHO. Professor XU Jing-fan, a great master of traditional Chinese medicine, has accumulated rich experiences in the treatment of UC. The study collected Professor XU's 77 prescriptions of treating UC, analyzed the frequency of traditional Chinese medicines and there categories, and investigated the medication regularity by the system clustering method...
March 2018: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29676100/-synthesis-biological-activity-computer-aided-drug-design-of-alpha-pinene-derivatives
#18
Meng-Die Yang, Qiu-Xiang Xu, Lian-Bao Ye, Ming Li, Yu Feng, Wei-Qiang Chen
Based on the anticancer mechanism of biological alkylating agent, we designed and synthesized two alpha pinene derivatives:(1R,5S)-(6,6-dimethylbicyclo[3,1,1]hept-2-en-2-yl)methyl benzenesulfonate and (1R,5S)-(6,6-dimethylbicyclo[3,1,1]hept-2-en-2-yl)methyl 4-methylbenzenesulfonate, of which structures were confirmed by ¹H-NMR, HPLC and MS date. These two compounds showed a good inhibition of tumor cells' proliferation. Further, the computer siuulation of molecular docking and metabolic kinetics indicated that these two copounds may have stable molecular complexation with protein CDK2, which closely related to the cell cycle...
March 2018: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29675788/recent-advances-in-tuberculosis-diagnostics-in-resource-limited-settings
#19
REVIEW
Mitsuko Seki, Chang-Ki Kim, Satoshi Hayakawa, Satoshi Mitarai
Smear-negative and drug-resistant cases of tuberculosis (TB) disease necessitate the development of new diagnostic methods, especially in resource-limited settings. To improve the current TB situations, sensitive and specific TB point-of-care tests (POCTs) should be developed. This review addresses the current status of TB, novel diagnostic methodologies for TB, and the impact of those new diagnostics on TB control in such situations. Moreover, the perspective of TB management based on laboratory examinations is described...
April 19, 2018: European Journal of Clinical Microbiology & Infectious Diseases
https://www.readbyqxmd.com/read/29675647/fabrication-of-agarose-concave-petridish-for-3d-culture-microarray-method-for-spheroids-formation-of-hepatic-cells
#20
Binbin Zhang, Yang Li, Gaoshang Wang, Zhidong Jia, Haiyan Li, Qing Peng, Yi Gao
Liver is one of the most important organ in the body. But there are many limitations about liver transplantation for liver failure. It is quite important to develop the xenogeneic biological liver for providing an alternation to transplantation or liver regeneration. In this paper, we proposed a method to construct a novel kind of agarose 3D-culture concave microwell array for spheroids formation of hepatic cells. Using the 3D printing method, the microwell array was fabricated with an overall size of 6.4 mm × 6...
April 19, 2018: Journal of Materials Science. Materials in Medicine
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