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https://www.readbyqxmd.com/read/28538738/solid-phase-synthesis-cyclization-and-site-specific-functionalization-of-aziridine-containing-tetrapeptides
#1
Benjamin K W Chung, Christopher J White, Andrei K Yudin
Cyclic tetrapeptides comprise a potent and selective class of molecules with a wide range of biological activities, including the phytotoxic activity of tentoxin and the histone deacetylase (HDAC) inhibitory effects of chlamydocin. The incorporation of a functional aziridine group within cyclic peptides enables their conformational control and allows for late-stage and site-selective functionalization of these molecules, thereby creating the potential for covalent protein labeling. This protocol describes the solid-phase synthesis, cyclization, and site-specific structural modification of aziridine-containing tetrapeptides...
June 2017: Nature Protocols
https://www.readbyqxmd.com/read/28538693/preparation-characterization-and-antioxidant-activity-evaluation-of-liposomes-containing-water-soluble-hydroxytyrosol-from-olive
#2
Jiao-Jiao Yuan, Frank G F Qin, Jun-Ling Tu, Bing Li
Due to the multiple hydroxyl groups in its structure, hydroxytyrosol (HT) is very sensitive to air and light and has very strong instability and hydrophilicity that affect its biological activity. This study attempted to prepare liposomes containing water-soluble HT to improve the bioavailability and biocompatibility of the target drug. The preparation process factors (temperature, mass ratio of phospholipid (PL) and cholesterol (CH), Tween-80 volume, HT mass) were studied and response surface methodology (RSM) was applied to optimize the conditions...
May 24, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28538687/on-forgotten-topological-indices-of-some-dendrimers-structure
#3
Yasir Bashir, Adnan Aslam, Muhammad Kamran, Muhammad Imran Qureshi, Adnan Jahangir, Muhammad Rafiq, Nargis Bibi, Nazeer Muhammad
A series of previously conducted experiments pertaining to various chemicals and drugs uncover a natural linkage between the molecular structures and the bio-medical and pharmacological characteristics. The forgotten topological index computed for the molecular structures of various chemical compounds and drugs has proven significant in medical and pharmaceutical fields by predicting biological features of new chemical compounds and drugs. A topological index can be considered as the transformation of chemical structure into a real number...
May 24, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28537745/deciphering-cryptic-binding-sites-on-proteins-by-mixed-solvent-molecular-dynamics
#4
S Roy Kimura, Haipeng Hu, Anatoly M Ruvinsky, Woody B Sherman, Angelo D Favia
In recent years, molecular dynamics simulations of proteins in explicit mixed-solvents have been applied to various problems in protein biophysics and drug discovery, including protein folding, protein surface characterization, fragment screening, allostery, and druggability assessment. In this study, we perform a systematic study on how mixtures of organic solvent probes in water can reveal cryptic ligand binding pockets that are not evident in crystal structures of apo proteins. We examine a diverse set of eight PDB proteins that show pocket opening induced by ligand binding and investigate whether solvent MD simulations on the apo structures can induce the binding site observed in the holo structures...
May 24, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28537720/chromone-as-a-privileged-scaffold-in-drug-discovery-recent-advances
#5
Joana Reis, Alexandra Gaspar, Nuno Milhazes, Fernanda M Borges
The use of privileged structures in drug discovery has proven to be an effective strategy allowing the generation of innovative hits/leads and successful optimization processes. Chromone is actually recognized as a privileged structure and a valid template for the design of novel compounds with potential pharmacological interest, particularly in the field of neurodegenerative, inflammatory and infectious diseases as well as diabetes and cancer. Within this framework, this review provides the reader with a literature update following the preceding article entitled Chromone: a valid scaffold in Medicinal Chemistry...
May 24, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28535606/isolation-purification-and-characterization-of-five-active-diketopiperazine-derivatives-from-endophytic-streptomyces-suk-25-with-antimicrobial-and-cytotoxic-activities
#6
Muhanna M Alshaibani, Juriyati Jalil, Nik M Sidik, Siti Junaidah Ahmad, Nurkhalida Kamal, Ruangelie Edrada-Ebel, Noraziah M Zin
On our search for new sources of bioactive secondary metabolites from Streptomyces sp., the ethyl acetate extracts from the endophytic Streptomyces SUK 25 afforded five active diketopiperazines compounds. The aim of this study was to characterize the bioactive compounds isolated from endophytic Streptomyces SUK 25 and evaluate its bioactivity against multiple drug resistance (MDR) bacteria such as Enterococcus raffinosus, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumanii, Pseudomonas aeruginosa and Enterobacter spp...
May 24, 2017: Journal of Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28535587/bicyclol-exerts-an-anti-tumor-effect-via-ros-mediated-endoplasmic-reticulum-stress-in-human-renal-cell-carcinoma-cells
#7
Jing Wu, Weichao Zheng, Ling Rong, Yingru Xing, Dong Hu
Renal cell carcinoma (RCC) is the most common subtype of kidney cancer. Currently, there is a lack of efficient treatment for RCC. Bicyclol, an anti-hepatitis drug, has been demonstrated to possess anti-tumor properties. However, the effect of bicyclol in RCC remains elusive. Therefore, the aim of this study is to investigate the biological effects of bicyclol on RCC and the underlying mechanisms. The data from this study indicated that bicyclol markedly induced cell apoptosis and cell cycle arrest and increased the production of reactive oxygen species (ROS) in RCC cells...
May 19, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28535545/portuguese-recommendations-for-the-use-of-methotrexate-in-rheumatic-diseases-2016-update
#8
Ana Catarina Duarte, Daniela Santos-Faria, Maria João Gonçalves, Alexandre Sepriano, Ana Filipa Mourão, Cátia Duarte, Joana Sousa Neves, Ana Filipa Águeda, Pedro Ávila Ribeiro, Alexandra Daniel, Adriano Neto, Ana Cordeiro, Ana Rodrigues, Anabela Barcelos, Cândida Silva, Cristina Ponte, Elsa Vieira-Sousa, Filipa Teixeira, Filipa Oliveira-Ramos, Filipe Araújo, Filipe Barcelos, Helena Canhão, Helena Santos, João Ramos, Joaquim Pereira, José Costa, José António Melo Gomes, Luís Cunha-Miranda, Lúcia Costa, Marcos Cerqueira, Margarida Cruz, Maria José Santos, Miguel Bernardes, Paula Oliveira, Pedro Abreu, Ricardo Figueira, Rita Barros, Sandra Falcão, Patrícia Pinto, Sofia Pimenta, Susana Capela, Vitor Teixeira, João Eurico Fonseca
BACKGROUND: Methotrexate (MTX) is the first-line drug in the treatment of rheumatoid arthritis (RA) and the most commonly prescribed disease modifying anti-rheumatic drug. Moreover, it is also used as an adjuvant drug in patients under biologic therapies, enhancing the efficacy of biologic agents. OBJECTIVES: To review the literature and update the Portuguese recommendations for the use of MTX in rheumatic diseases first published in 2009. METHODS: The first Portuguese guidelines for the use of MTX in rheumatic diseases were published in 2009 and were integrated in the multinational 3E Initiative (Evidence Expertise Exchange) project...
May 9, 2017: Acta Reumatológica Portuguesa
https://www.readbyqxmd.com/read/28534859/workplace-hazards-faced-by-nursing-assistants-in-the-united-states-a-focused-literature-review
#9
REVIEW
AnnMarie Lee Walton, Bonnie Rogers
Nursing assistants (NAs) make up a large share of the healthcare provider workforce and their numbers are expected to grow. NAs are predominantly women who earn a low wage and report financial, work, and family demands. Working as a NA is hazardous; this manuscript specifically examines the biological/infectious, chemical, enviromechanical, physical and psychosocial hazards that appear in the literature to date. A focused search strategy was used to review literature about hazards that fell into each of the five aforementioned domains...
May 19, 2017: International Journal of Environmental Research and Public Health
https://www.readbyqxmd.com/read/28534676/applications-of-raman-spectroscopy-in-biopharmaceutical-manufacturing-a-short-review
#10
Kevin Buckley, Alan G Ryder
The production of active pharmaceutical ingredients (APIs) is currently undergoing its biggest transformation in a century. The changes are based on the rapid and dramatic introduction of protein- and macromolecule-based drugs (collectively known as biopharmaceuticals) and can be traced back to the huge investment in biomedical science (in particular in genomics and proteomics) that has been ongoing since the 1970s. Biopharmaceuticals (or biologics) are manufactured using biological-expression systems (such as mammalian, bacterial, insect cells, etc...
June 2017: Applied Spectroscopy
https://www.readbyqxmd.com/read/28534602/the-management-of-moderate-to-severe-chronic-plaque-psoriasis
#11
Annalisa Tonini, Salvatore Panduri, Angelo M D'Erme, Francesca Papadia, Marco Romanelli, James G Krueger, Andrea Chiricozzi
Recent approval and marketization of novel treatments have widened the range of therapeutic opportunities for moderate-to-severe psoriasis. In the next years, this panorama will be further enlarged as many other agents, both oral small molecules and biologics, have passed phase III and are expected to be approved, and subsequently marketed, shortly. In spite of this array of therapeutic possibilities, there is still an unmet need for an appropriate treatment in a large number of cases. This review was aimed to describe general principles regarding the therapeutic approach to moderate-severe plaque psoriasis, providing an updated overview of the therapeutic armamentarium that is specifically available in Italy, drug prescribility, and some peculiar limitations for reimbursement defined by our National Health Care System...
May 23, 2017: Giornale Italiano di Dermatologia e Venereologia: Organo Ufficiale, Società Italiana di Dermatologia e Sifilografia
https://www.readbyqxmd.com/read/28534601/management-of-psoriatic-arthritis-psa-among-cutaneous-psoriasis-from-pathogenesis-to-therapy
#12
Pauline Hoelt, Cyrille Confavreux, Denis Jullien, Axel P Villani
Psoriatic arthritis (PsA) is an inflammatory rheumatism belonging to spondylarthritis family and which occurs in about 30% of patients with psoriasis. The pathogenesis entails a genetic predisposition, environmental and immunologic factors. Most of the time, cutaneous lesions precede apparition of articular manifestations and dermatologists who treat psoriatic patients have to regularly screen for early PsA, especially in patients with risk factors (notably nail psoriasis). Early detection greatly increases the chances for successful treatment and can prevent slow joint destruction...
May 23, 2017: Giornale Italiano di Dermatologia e Venereologia: Organo Ufficiale, Società Italiana di Dermatologia e Sifilografia
https://www.readbyqxmd.com/read/28534531/unravelling-the-biology-of-sclc-implications-for-therapy
#13
REVIEW
Joshua K Sabari, Benjamin H Lok, James H Laird, John T Poirier, Charles M Rudin
Small-cell lung cancer (SCLC) is an aggressive malignancy associated with a poor prognosis. First-line treatment has remained unchanged for decades, and a paucity of effective treatment options exists for recurrent disease. Nonetheless, advances in our understanding of SCLC biology have led to the development of novel experimental therapies. Poly [ADP-ribose] polymerase (PARP) inhibitors have shown promise in preclinical models, and are under clinical investigation in combination with cytotoxic therapies and inhibitors of cell-cycle checkpoints...
May 23, 2017: Nature Reviews. Clinical Oncology
https://www.readbyqxmd.com/read/28534445/differential-expression-of-micro-rnas-and-their-predicted-targets-in-renal-cells-exposed-to-amphotericin-b-and-its-complex-with-copper-ii-ions
#14
Joanna Magdalena Gola, Barbara Strzałka-Mrozik, Celina Kruszniewska-Rajs, Jolanta Adamska, Mariusz Gagoś, Urszula Mazurek
MicroRNAs (miRNAs) have been reported to regulate essential biological processes, and their expression was shown to be affected by pathological processes and drug-induced toxicity. Amphotericin B (AmB) can cause liver and kidney injury, but a recently developed complex of AmB with copper (II) ions (AmB-Cu(2+)) exhibits a lower toxicity to human renal cells while retaining a high antifungal activity. The aim of our study was to assess AmB-Cu(2+)- induced changes in the miRNA profile of renal cells and to examine which biological processes are significantly affected by AmB-Cu(2+)...
May 23, 2017: Toxicology Mechanisms and Methods
https://www.readbyqxmd.com/read/28534432/gastrointestinal-microphysiological-systems
#15
Sarah E Blutt, James R Broughman, Winnie Zou, Xi-Lei Zeng, Umesh C Karandikar, Julie In, Nicholas C Zachos, Olga Kovbasnjuk, Mark Donowitz, Mary K Estes
Gastrointestinal diseases are a significant health care and economic burden. Prevention and treatment of these diseases have been limited by the available human biologic models. Microphysiological systems comprise organ-specific human cultures that recapitulate many structural, biological, and functional properties of the organ in smaller scale including aspects of flow, shear stress and chemical gradients. The development of intestinal microphysiological system platforms represents a critical component in improving our understanding, prevention, and treatment of gastrointestinal diseases...
January 1, 2017: Experimental Biology and Medicine
https://www.readbyqxmd.com/read/28534292/development-and-characterization-of-a-neutralizing-anti-idiotype-antibody-against-mirvetuximab-for-analysis-of-clinical-samples
#16
Sven Loebrich, Mingfang Shen, Erika Cohen, Gillian Payne, Ying Chen, Megan Bogalhas, Yiwei Zhao
Antibody-drug-conjugates (ADCs) are an emerging class of biological therapeutics. Mirvetuximab soravtansine is a novel folate receptor alpha (FRα)-targeting ADC which represents a potential new treatment for patients with ovarian and other FRα-positive cancers. Since patient immune responses to biological therapeutics may negatively affect drug efficacy and patient safety, regulatory authorities require rigorous monitoring of patient samples. Taking advantage of the immune system's ability to generate highly specific antibodies, the field has turned to anti-idiotype antibodies as powerful tools for the development of sensitive and specific bioassays...
May 22, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28534288/physicochemical-and-biological-characterization-of-sustained-isopropyl-unoprostone-release-device-made-of-poly-ethyleneglycol-dimethacrylates
#17
Nobuhiro Nagai, Yasuko Izumida, Yoshimasa Yamazaki, Hirokazu Kaji, Junichi Kawasaki, Matsuhiko Nishizawa, Toshiaki Abe
Transscleral drug delivery is becoming increasingly popular to manage posterior eye diseases. To evaluate the clinical application of a transscleral, sustained, unoprostone (UNO)-release device (URD) constructed of photopolymerized tri(ethyleneglycol) dimethacrylate and poly(ethyleneglycol) dimethacrylate, we evaluated physicochemical and biological properties of this device. The URD consists of a drug-impermeable reservoir and a semi-permeable cover. The in vitro release rate of UNO from the URD increased with increasing temperatures from 20 to 45 °C...
July 2017: Journal of Materials Science. Materials in Medicine
https://www.readbyqxmd.com/read/28533920/inflammatory-bowel-disease-efficient-remission-maintenance-is-crucial-for-cost-containment
#18
REVIEW
Giovanni C Actis, Rinaldo Pellicano
The inflammatory bowel diseases (IBD) are chronic incurable inflammatory disorders of the gut. Some 10% run a downhill course, requiring emergency medical support and often surgery; another small subset are monogenic, and, threatening pediatric patients, are the challenge of these days. The majority of the IBDs, however, are polygenic low-penetrance diseases, running a lifetime waxing-and-waning course. The prevalent trend is towards a slow worsening and steady cost increase. Each and all drugs of the available arsenal exhibit strengths and weaknesses: Mesalamines are chiefly effectively for mild-moderate colitis, and do not work in Crohn's; steroids do not control some 40% of the ulcerative colitis cases, and are not indicated for Crohn's; thiopurines are effective in the maintenance of the IBDs but do not prevent relapses on withdrawal; biologics are still being used empirically (not monitored) causing further increase of their cost over that of hospitalization...
May 6, 2017: World Journal of Gastrointestinal Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28533919/combination-therapy-for-inflammatory-bowel-disease
#19
REVIEW
Keith S Sultan, Joshua C Berkowitz, Sundas Khan
Biologic therapies such as infliximab and adalimumab have become mainstays of treatment for inflammatory bowel disease. Early studies suggested that combination therapy (CT) with infliximab and an immunomodulator drug such as azathioprine may help optimize biologic pharmacokinetics, minimize immunogenicity, and improve outcomes. The landmark SONIC trial in Crohn's disease and the UC SUCCESS trial in ulcerative colitis demonstrated CT with infliximab and azathioprine to be superior to monotherapy with either agent alone at inducing clinical remission in treatment naïve patients with moderate to severe disease...
May 6, 2017: World Journal of Gastrointestinal Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28533524/enhancing-the-genome-editing-toolbox-genome-wide-crispr-arrayed-libraries
#20
Emmanouil Metzakopian, Alex Strong, Vivek Iyer, Alex Hodgkins, Konstantinos Tzelepis, Liliana Antunes, Mathias J Friedrich, Qiaohua Kang, Teresa Davidson, Jacob Lamberth, Christina Hoffmann, Gregory D Davis, George S Vassiliou, William C Skarnes, Allan Bradley
CRISPR-Cas9 technology has accelerated biological research becoming routine for many laboratories. It is rapidly replacing conventional gene editing techniques and has high utility for both genome-wide and gene-focussed applications. Here we present the first individually cloned CRISPR-Cas9 genome wide arrayed sgRNA libraries covering 17,166 human and 20,430 mouse genes at a complexity of 34,332 sgRNAs for human and 40,860 sgRNAs for the mouse genome. For flexibility in generating stable cell lines the sgRNAs have been cloned in a lentivirus backbone containing PiggyBac transposase recognition elements together with fluorescent and drug selection markers...
May 22, 2017: Scientific Reports
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