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https://www.readbyqxmd.com/read/28719188/phage-selection-of-cyclic-peptides-for-application-in-research-and-drug-development
#1
Kaycie Deyle, Xu-Dong Kong, Christian Heinis
Cyclic peptides can bind to protein targets with high affinities and selectivities, which makes them an attractive modality for the development of research reagents and therapeutics. Additional properties, including low inherent toxicity, efficient chemical synthesis, and facile modification with labels or immobilization reagents, increase their attractiveness. Cyclic peptide ligands against a wide range of protein targets have been isolated from natural sources such as bacteria, fungi, plants, and animals...
July 18, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28717570/chip-on-the-tip-compact-flexible-endoscopic-epifluorescence-video-microscope-for-in-vivo-imaging-in-medicine-and-biomedical-research
#2
Gregor Matz, Bernhard Messerschmidt, Werner Göbel, Severin Filser, Christian S Betz, Matthias Kirsch, Ortrud Uckermann, Marcel Kunze, Sven Flämig, André Ehrhardt, Klaus-Martin Irion, Mareike Haack, Mario M Dorostkar, Jochen Herms, Herbert Gross
We demonstrate a 60 mg light video-endomicroscope with a cylindrical shape of the rigid tip of only 1.6 mm diameter and 6.7 mm length. A novel implementation method of the illumination unit in the endomicroscope is presented. It allows for the illumination of the biological sample with fiber-coupled LED light at 455 nm and the imaging of the red-shifted fluorescence light above 500 nm in epi-direction. A large numerical aperture of 0.7 leads to a sub-cellular resolution and yields to high-contrast images within a field of view of 160 μm...
July 1, 2017: Biomedical Optics Express
https://www.readbyqxmd.com/read/28717259/a-computerized-tutor-prototype-for-prostate-cryotherapy-key-building-blocks-and-system-evaluation
#3
Yoed Rabin, Kenji Shimada, Purva Joshi, Anjali Sehrawat, Robert Keelan, Dona M Wilfong, James T McCormick
This paper focuses on the evaluation of a prototype for a computer-based tutoring system for prostate cryosurgery, while reviewing its key building blocks and their benchmark performance. The tutoring system lists geometrical constraints of cryoprobe placement, displays a rendered shape of the prostate, simulates cryoprobe insertion, enables distance measurements, simulates the corresponding thermal history, and evaluates the mismatch between the target region shape and a pre-selected planning isotherm. The quality of trainee planning is measured in comparison with a computer-generated plan, created for each case study by a previously developed planning algorithm, known as bubble-packing...
January 28, 2017: Proceedings of SPIE
https://www.readbyqxmd.com/read/28717105/ephedrine-induced-mitophagy-via-oxidative-stress-in-human-hepatic-stellate-cells
#4
Ah Young Lee, Yoonjeong Jang, Seong-Ho Hong, Seung-Hee Chang, Sungjin Park, Sanghwa Kim, Kyung-Sun Kang, Ji-Eun Kim, Myung-Haing Cho
The herb Ephedra sinica (also known as Chinese ephedra or Ma Huang), used in traditional Chinese medicine, contains alkaloids identical to ephedrine and pseudoephedrine as its principal active constituents. Recent studies have reported that ephedrine has various side effects in the cardiovascular and nervous systems. In addition, herbal Ephedra, a plant containing many pharmacologically active alkaloids, principally ephedrine, has been reported to cause acute hepatitis. Many studies reported clinical cases, however, the cellular mechanism of liver toxicity by ephedrine remains unknown...
2017: Journal of Toxicological Sciences
https://www.readbyqxmd.com/read/28716821/abnormalities-in-alternative-splicing-in-diabetes-therapeutic-targets
#5
REVIEW
Zodwa Dlamini, Fortunate Mokoena, Rodney Hull
Diabetes mellitus (DM) is a non-communicable, metabolic disorder that affects 416 million individuals worldwide. Type 2 diabetes contributes to a vast 85-90% of the diabetes incidences while 10-15% of patients suffer from type 1 diabetes. These two predominant forms of DM cause a significant loss of functional pancreatic β-cell mass causing different degrees of insulin deficiency, most likely, due to increased β-cell apoptosis. Treatment options involve the use of insulin sensitisers, α-glucosidase inhibitors, and β-cell secretagogues which are often expensive, limited in efficacy and carry detrimental adverse effects...
August 2017: Journal of Molecular Endocrinology
https://www.readbyqxmd.com/read/28716677/incidence-of-active-tuberculosis-in-individuals-with-latent-tuberculosis-infection-in-rural-china-follow-up-results-of-a-population-based-multicentre-prospective-cohort-study
#6
Lei Gao, Xiangwei Li, Jianmin Liu, Xinhua Wang, Wei Lu, Liqiong Bai, Henan Xin, Haoran Zhang, Hengjing Li, Zongde Zhang, Yu Ma, Mufei Li, Boxuan Feng, Jiang Du, Hongtao Sui, Rong Zhao, Haoxiang Su, Shouguo Pan, Ling Guan, Fei Shen, Jian He, Shumin Yang, Hongyan Si, Xu Cheng, Zuhui Xu, Yunhong Tan, Tianzhu Chen, Weiguo Xu, Hong Peng, Zhijian Wang, Tao Zhu, Xiaoyou Chen, Xinhua Zhou, Xueling Guan, Qi Jin
BACKGROUND: The management of latent Mycobacterium tuberculosis infection is a new priority action for the WHO End Tuberculosis (TB) Strategy. However, national guidelines on latent tuberculosis infection testing and treatment have not yet been developed in China. Here, we present the results from the 2-year follow-up of a study that aimed to track the development of active disease in individuals with latent tuberculosis infection, identify priority populations for latent infection management, and explore the most suitable latent infection diagnostic approach...
July 14, 2017: Lancet Infectious Diseases
https://www.readbyqxmd.com/read/28716664/advances-and-challenges-in-the-search-for-d2-and-d3-dopamine-receptor-selective-compounds
#7
REVIEW
Amy E Moritz, R Benjamin Free, David R Sibley
Compounds that target D2-like dopamine receptors (DRs) are currently used as therapeutics for several neuropsychiatric disorders including schizophrenia (antagonists) and Parkinson's disease (agonists). However, as the D2R and D3R subtypes are highly homologous, creating compounds with sufficient subtype-selectivity as well as drug-like properties for therapeutic use has proved challenging. This review summarizes the progress that has been made in developing D2R- or D3R-selective antagonists and agonists, and also describes the experimental conditions that need to be considered when determining the selectivity of a given compound, as apparent selectivity can vary widely depending on assay conditions...
July 14, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28716651/significance-of-a-to-i-rna-editing-of-transcripts-modulating-pharmacokinetics-and-pharmacodynamics
#8
REVIEW
Masataka Nakano, Miki Nakajima
RNA editing is a post-transcriptional process that alters the nucleotide sequence of RNA transcripts to generate transcriptome diversity. Among the various types of RNA editing, adenosine-to-inosine (A-to-I) RNA editing is the most frequent type of RNA editing in mammals. Adenosine deaminases acting on RNA (ADAR) enzymes, ADAR1 and ADAR2, convert adenosines in double-stranded RNA structures into inosines by hydrolytic deamination. Inosine forms a base pair with cytidine as if it were guanosine; therefore, the conversion may affect the amino acid sequence, splicing, microRNA targeting, and miRNA maturation...
July 14, 2017: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28716571/antiviral-effect-of-forsythoside-a-from-forsythia-suspensa-thunb-vahl-fruit-against-influenza-a-virus-through-reduction-of-viral-m1-protein
#9
Anna Hing-Yee Law, Cindy Lai-Hung Yang, Allan Sik-Yin Lau, Godfrey Chi-Fung Chan
ETHNOPHARMACOLOGICAL RELEVANCE: Yinqiaosan is a classical traditional Chinese medicine formula, which has been used to treat respiratory diseases since ancient China. It consists of nine herbs and among them, Forsythia suspensa (Thunb.) Vahl fruit is one of the major herbal components. Despite the long history of Yinqiaosan, the active compounds and the mechanisms of action of this formula remain elusive. AIM OF THE STUDY: The present study aimed to examine the suppressive effect of Yinqiaosan on influenza virus and to identify the active components in the formula targeting influenza...
July 14, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28716187/impact-of-albumin-based-approaches-in-nanomedicine-imaging-targeting-and-drug-delivery
#10
REVIEW
Bharat Bhushan, Vitaly Khanadeev, Boris Khlebtsov, Nikolai Khlebtsov, P Gopinath
A major challenge in the field of nanomedicine is to transform laboratory innovations into commercially successful clinical products. In this campaign, a variety of nanoenabled approaches have been designed and investigated for their role in biomedical applications. The advantages associated with the unique structure of albumin imparts it with the ability to interact with variety of molecules, while the functional groups present on their surface provide base for large number of modifications making it as an ideal nanocarrier system...
July 1, 2017: Advances in Colloid and Interface Science
https://www.readbyqxmd.com/read/28716121/identification-of-trunk-mutations-in-gastric-carcinoma-a-case-study
#11
Zhan Zhou, Shanshan Wu, Jun Lai, Yuan Shi, Chixiao Qiu, Zhe Chen, Yufeng Wang, Xun Gu, Jie Zhou, Shuqing Chen
BACKGROUND: Intratumor heterogeneity (ITH) poses an urgent challenge for cancer precision medicine because it can cause drug resistance against cancer target therapy and immunotherapy. The search for trunk mutations that are present in all cancer cells is therefore critical for each patient. CASE PRESENTATION: In this study, we aimed to evaluate the efficiency of multiregional sequencing for the identification of trunk mutations present in all regions of a tumor as a case study...
July 17, 2017: BMC Medical Genomics
https://www.readbyqxmd.com/read/28715874/detection-of-bacterial-infection-by-a-technetium-99m-labeled-peptidoglycan-aptamer
#12
Iêda Mendes Ferreira, Camila Maria de Sousa Lacerda, Sara Roberta Dos Santos, André Luís Branco de Barros, Simone Odília Fernandes, Valbert Nascimento Cardoso, Antero Silva Ribeiro de Andrade
Nuclear medicine clinicians are still waiting for the optimal scintigraphic imaging agents capable of distinguishing between infection and inflammation, and between fungal and bacterial infections. Aptamers have several properties that make them suitable for molecular imaging. In the present study, a peptidoglycan aptamer (Antibac1) was labeled with (99m)Tc and evaluated by biodistribution studies and scintigraphic imaging in infection-bearing mice. Labeling with (99m)Tc was performed by the direct method and the complex stability was evaluated in saline, plasma and in the molar excess of cysteine...
July 13, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28715203/a-bioinorganic-approach-to-fragment-based-drug-discovery-targeting-metalloenzymes
#13
Seth M Cohen
Metal-dependent enzymes (i.e., metalloenzymes) make up a large fraction of all enzymes and are critically important in a wide range of biological processes, including DNA modification, protein homeostasis, antibiotic resistance, and many others. Consequently, metalloenzymes represent a vast and largely untapped space for drug development. The discovery of effective therapeutics that target metalloenzymes lies squarely at the interface of bioinorganic and medicinal chemistry and requires expertise, methods, and strategies from both fields to mount an effective campaign...
July 17, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28714878/integrated-metabolomics-assessment-of-human-dried-blood-spots-and-urine-strips
#14
Jeremy Drolet, Vladimir Tolstikov, Brian A Williams, Bennett P Greenwood, Collin Hill, Vivek K Vishnudas, Rangaprasad Sarangarajan, Niven R Narain, Michael A Kiebish
(1) Background: Interest in the application of metabolomics toward clinical diagnostics development and population health monitoring has grown significantly in recent years. In spite of several advances in analytical and computational tools, obtaining a sufficient number of samples from patients remains an obstacle. The dried blood spot (DBS) and dried urine strip (DUS) methodologies are a minimally invasive sample collection method allowing for the relative simplicity of sample collection and minimal cost...
July 15, 2017: Metabolites
https://www.readbyqxmd.com/read/28714500/exploring-the-immunomodulatory-and-anticancer-properties-of-zerumbone
#15
REVIEW
Md Areeful Haque, Ibrahim Jantan, Laiba Arshad, Syed Nasir Abbas Bukhari
Plant-derived immunomodulators and anti-cancer agents have attracted a lot of interest from natural product scientists for their efficacy and safety and their significant contribution towards understanding targeted drug action and drug delivery mechanisms. Zerumbone, the main constituent of Zingiber zerumbet rhizomes, has been investigated for its wide-spectrum role in treating multitargeted diseases. The rhizomes have been used as food flavoring agents in various cuisines and in herbal medicine. Many in vivo and in vitro studies have provided evidence of zerumbone as a potent immunomodulator as well as a potential anti-cancer agent...
July 17, 2017: Food & Function
https://www.readbyqxmd.com/read/28714473/prioritizing-multiple-therapeutic-targets-in-parallel-using-automated-dna-encoded-library-screening
#16
Carl A Machutta, Christopher S Kollmann, Kenneth E Lind, Xiaopeng Bai, Pan F Chan, Jianzhong Huang, Lluis Ballell, Svetlana Belyanskaya, Gurdyal S Besra, David Barros-Aguirre, Robert H Bates, Paolo A Centrella, Sandy S Chang, Jing Chai, Anthony E Choudhry, Aaron Coffin, Christopher P Davie, Hongfeng Deng, Jianghe Deng, Yun Ding, Jason W Dodson, David T Fosbenner, Enoch N Gao, Taylor L Graham, Todd L Graybill, Karen Ingraham, Walter P Johnson, Bryan W King, Christopher R Kwiatkowski, Joël Lelièvre, Yue Li, Xiaorong Liu, Quinn Lu, Ruth Lehr, Alfonso Mendoza-Losana, John Martin, Lynn McCloskey, Patti McCormick, Heather P O'Keefe, Thomas O'Keeffe, Christina Pao, Christopher B Phelps, Hongwei Qi, Keith Rafferty, Genaro S Scavello, Matt S Steiginga, Flora S Sundersingh, Sharon M Sweitzer, Lawrence M Szewczuk, Amy Taylor, May Fern Toh, Juan Wang, Minghui Wang, Devan J Wilkins, Bing Xia, Gang Yao, Jean Zhang, Jingye Zhou, Christine P Donahue, Jeffrey A Messer, David Holmes, Christopher C Arico-Muendel, Andrew J Pope, Jeffrey W Gross, Ghotas Evindar
The identification and prioritization of chemically tractable therapeutic targets is a significant challenge in the discovery of new medicines. We have developed a novel method that rapidly screens multiple proteins in parallel using DNA-encoded library technology (ELT). Initial efforts were focused on the efficient discovery of antibacterial leads against 119 targets from Acinetobacter baumannii and Staphylococcus aureus. The success of this effort led to the hypothesis that the relative number of ELT binders alone could be used to assess the ligandability of large sets of proteins...
July 17, 2017: Nature Communications
https://www.readbyqxmd.com/read/28714419/design-of-multi-target-agents-for-the-treatment-of-alzheimer-s-disease-based-on-tacrine
#17
Hongzhi Lin, Qi Li, Kai Gu, Jie Zhu, Xueyang Jiang, Yao Chen, Haopeng Sun
Alzheimer's disease (AD) is one of the most common forms of dementia in elderly people. To date, efficacious therapeutic agent for the treatment of AD is still very limited, so it has long been a challenging and attractive task to discover new anti-AD drugs. Considering the multifactorial nature of AD, recently, the concept of multi-target-directed ligands (MTDLs) has emerged as a new strategy for designing therapeutic agents on AD. MTDLs are believed to exert their effects through simultaneously affecting multiple targets which contribute to etiology of AD...
July 17, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28714120/partial-fourier-techniques-in-single-shot-cross-term-spatiotemporal-encoded-mri
#18
Zhiyong Zhang, Lucio Frydman
PURPOSE: Cross-term spatiotemporal encoding (xSPEN) is a single-shot approach with exceptional immunity to field heterogeneities, the images of which faithfully deliver 2D spatial distributions without requiring a priori information or using postacquisition corrections. xSPEN, however, suffers from signal-to-noise ratio penalties due to its non-Fourier nature and due to diffusion losses-especially when seeking high resolution. This study explores partial Fourier transform approaches that, acting along either the readout or the spatiotemporally encoded dimensions, reduce these penalties...
July 16, 2017: Magnetic Resonance in Medicine: Official Journal of the Society of Magnetic Resonance in Medicine
https://www.readbyqxmd.com/read/28714033/evaluation-of-velvet-antler-total-protein-effect-on-bone-marrow%C3%A2-derived-endothelial-progenitor-cells
#19
Xiang Xiao, Lin Li, Shuqiang Xu, Min Mao, Ruiyan Pan, Yanjun Li, Jiayun Wu, Li Huang, Xiaoyun Zheng
Lu Rong, velvet antler (VA), is a traditional Chinese medicine, which is used as a food supplement and therapeutic drug in China, Japan, Russia, New Zealand and Southeast Asia. The regenerative characteristics of VA have resulted in great research interest, particularly regarding the fields of organ grafting and stem cell differentiation. Various VA proteomic studies verified that proteins act as the primary bioactive components of VA. The present study aimed to investigate if VA proteins (VA‑pro) influence endothelial progenitor cell (EPC) viability...
July 15, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28713966/spica-prunellae-extract-suppresses-the-growth-of-human-colon-carcinoma-cells-by-targeting-multiple-oncogenes-via-activating-mir-34a
#20
Yi Fang, Ling Zhang, Jianyu Feng, Wei Lin, Qiaoyan Cai, Jun Peng
Spica Prunellae is the spike of the herb Prunella vulgaris L. in traditional Chinese medicine which is often used for the treatment of various cancers including colorectal cancer. In the present study, we found that a key tumor suppressor, microRNA-34a (miR-34a) is involved in the antitumor activity for Spica Prunellae. Human colon carcinoma HCT-8 cells treated with an ethanol extract of Spica Prunellae (EESP) had significantly decreased cell proliferation and viability, in a dose-dependent manner. Flow cytometry analysis with Annexin V/PI staining analysis revealed that EESP treatment could induce apoptosis of HCT-8 cells...
July 6, 2017: Oncology Reports
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