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https://www.readbyqxmd.com/read/29775725/anti-hepatitis-c-virus-activity-and-synergistic-effect-of-nymphaea-alba-extracts-and-bioactive-constituents-in-liver-infected-cells
#1
Sidra Rehman, Usman Ali Ashfaq, Bushra Ijaz, Sheikh Riazuddin
BACKGROUND: Without an effective vaccine, hepatitis C virus (HCV) remains a global threat, inflicting 170-300 million carriers worldwide at risk of cirrhosis and hepatocellular carcinoma (HCC). Though various direct acting antivirals have been redeemed the hepatitis C treatment, a few restraints persist including possible side effects, viral resistance emergence, excessive cost which restricts its availability to a common person. HYPOTHESIS: There is no preventive HCV vaccine available today so the discovery of potent antiviral natural flora and their bioactive constituents may help to develop preventive cures against HCV infection...
May 15, 2018: Microbial Pathogenesis
https://www.readbyqxmd.com/read/29775690/molecular-subtyping-of-colorectal-cancer-recent-progress-new-challenges-and-emerging-opportunities
#2
REVIEW
Wei Wang, Raju Kandimalla, Hao Huang, Lina Zhu, Ying Li, Feng Gao, Ajay Goel, Xin Wang
Colorectal cancer (CRC) is one of the leading causes of cancer-related deaths worldwide. Similar to many other malignancies, CRC is a heterogeneous disease, making it a clinical challenge for optimization of treatment modalities in reducing the morbidity and mortality associated with this disease. A more precise understanding of the biological properties that distinguish patients with colorectal tumors, especially in terms of their clinical features, is a key requirement towards a more robust, targeted-drug design, and implementation of individualized therapies...
May 15, 2018: Seminars in Cancer Biology
https://www.readbyqxmd.com/read/29775627/acquisition-of-tumorigenic-potential-and-therapeutic-resistance-in-cd133-subpopulation-of-prostate-cancer-cells-exhibiting-stem-cell-like-characteristics
#3
Rajnee Kanwal, Sanjeev Shukla, Ethan Walker, Sanjay Gupta
The role of CD133 (Prominin-1) as a cancer stem cell marker may be useful for therapeutic approaches and prognostication in prostate cancer patients. We investigated the stem-cell-related function and biological features of a subpopulation of CD133+ cells isolated from established primary human prostate cancer cell lines. The CD133+ cells sorted from human prostate cancer 22Rv1 exhibited high clonogenic and tumorigenic capabilities, sphere forming capacity and serially reinitiated transplantable tumors in NOD-SCID mice...
May 15, 2018: Cancer Letters
https://www.readbyqxmd.com/read/29774951/protein-kinase-c%C3%AE-pkc%C3%AE-involved-in-the-regulation-of-pakt1-ser473-on-the-release-of-mouse-oocytes-from-diplotene-arrest
#4
Lingling Liu, Sen Li, Hanwen Li, Dahai Yu, Chunyu Li, Gensong Li, Yu Cao, Chen Feng, Xin Deng
Defects in meiotic maturation may lead to chromosome segregation errors and genomic instability. Previous reports indicated that protein kinase C delta (PKCδ) may interact with microtubule organizing center-associated protein to play a role on meiotic spindle organization of mammalian oocytes. In this study, we explored the potential role of protein kinase B alpha (PKBα/Akt1), PKCδ, and their relationship on meiotic maturation of mouse oocytes. We examined the expression and localization of pAkt1 (Ser473) and/or pPKCδ (Thr505) under the treatment of SH-6 or Sotrastaurin...
May 18, 2018: Cell Biochemistry and Function
https://www.readbyqxmd.com/read/29774657/cheminformatics-in-drug-discovery-an-industrial-perspective
#5
REVIEW
Hongming Chen, Thierry Kogej, Ola Engkvist
Cheminformatics has established itself as a core discipline within large scale drug discovery operations. It would be impossible to handle the amount of data generated today in a small molecule drug discovery project without persons skilled in cheminformatics. In addition, due to increased emphasis on "Big Data", machine learning and artificial intelligence, not only in the society in general, but also in drug discovery, it is expected that the cheminformatics field will be even more important in the future...
May 18, 2018: Molecular Informatics
https://www.readbyqxmd.com/read/29774075/plectin-targeted-liposomes-enhance-the-therapeutic-efficacy-of-a-parp-inhibitor-in-the-treatment-of-ovarian-cancer
#6
Siva Sai Krishna Dasa, Galina Diakova, Ryo Suzuki, Anne M Mills, Michael F Gutknecht, Alexander L Klibanov, Jill K Slack-Davis, Kimberly A Kelly
Advances in genomics and proteomics drive precision medicine by providing actionable genetic alterations and molecularly targeted therapies, respectively. While genomic analysis and medicinal chemistry have advanced patient stratification with treatments tailored to the genetic profile of a patient's tumor, proteomic targeting has the potential to enhance the therapeutic index of drugs like poly(ADP-ribose) polymerase (PARP) inhibitors. PARP inhibitors in breast and ovarian cancer patients with BRCA1/2 mutations have shown promise...
2018: Theranostics
https://www.readbyqxmd.com/read/29774062/-in-vivo-imaging-biomarkers-of-neuroinflammation-in-the-development-and-assessment-of-stroke-therapies-towards-clinical-translation
#7
REVIEW
Bastian Zinnhardt, Maximilian Wiesmann, Lisa Honold, Cristina Barca, Michael Schäfers, Amanda J Kiliaan, Andreas H Jacobs
Modulation of the inflammatory microenvironment after stroke opens a new avenue for the development of novel neurorestorative therapies in stroke. Understanding the spatio-temporal profile of (neuro-)inflammatory imaging biomarkers in detail thereby represents a crucial factor in the development and application of immunomodulatory therapies. The early integration of quantitative molecular imaging biomarkers in stroke drug development may provide key information about (i) early diagnosis and follow-up, (ii) spatio-temporal drug-target engagement (pharmacodynamic biomarker), (iii) differentiation of responders and non-responders in the patient cohort (inclusion/exclusion criteria; predictive biomarkers), and (iv) the mechanism of action...
2018: Theranostics
https://www.readbyqxmd.com/read/29774009/signaling-pathways-and-cellular-mechanisms-regulating-mossy-fiber-sprouting-in-the-development-of-epilepsy
#8
REVIEW
Christin M Godale, Steve C Danzer
The sprouting of hippocampal dentate granule cell axons, termed mossy fibers, into the dentate inner molecular layer is one of the most consistent findings in tissue from patients with mesial temporal lobe epilepsy. Decades of research in animal models have revealed that mossy fiber sprouting creates de novo recurrent excitatory connections in the hippocampus, fueling speculation that the pathology may drive temporal lobe epileptogenesis. Conducting definitive experiments to test this hypothesis, however, has been challenging due to the difficulty of dissociating this sprouting from the many other changes occurring during epileptogenesis...
2018: Frontiers in Neurology
https://www.readbyqxmd.com/read/29773873/therapeutic-nanoparticles-penetrate-leaves-and-deliver-nutrients-to-agricultural-crops
#9
Avishai Karny, Assaf Zinger, Ashima Kajal, Janna Shainsky-Roitman, Avi Schroeder
As the world population grows, there is a need for efficient agricultural technologies to provide global food requirements and reduce environmental toll. In medicine, nanoscale drug delivery systems grant improved therapeutic precision by overcoming biological barriers and enhancing drug targeting to diseased tissues. Here, we loaded nanoscale drug-delivery systems with agricultural nutrients, and applied them to the leaves of tomato plants. We show that the nanoparticles - liposomes composed of plant-derived lipids, penetrate the leaf and translocate in a bidirectional manner, distributing to other leaves and to the roots...
May 17, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29773584/mechanisms-in-endocrinology-cell-cycle-regulation-in-adrenocortical-carcinoma
#10
Sofia Pereira, Mariana P Monteiro, Isabelle Bourdeau, Andre Lacroix, Duarte Pignatelli
Adrenocortical carcinomas are rather rare endocrine tumors that often have a poor prognosis. The reduced survival rate associated with these tumors is due to their aggressive biological behavior, combined with the scarcity of effective treatment options that are currently available. The recent identification of the genomic alterations present in ACC have provided further molecular mechanisms to develop consistent strategies for the diagnosis, prevention of progression and treatment of advanced ACCs. Taken together, molecular and genomic advances could be leading the way to develop personalized medicine in ACCs similarly to similar developments in lung or breast cancers...
May 17, 2018: European Journal of Endocrinology
https://www.readbyqxmd.com/read/29773051/dna-topoisomerases-of-leishmania-parasites-druggable-targets-for-drug-discovery
#11
Rosa Mª Reguer, Ehab Kotb Elmahallaw, Carlos Garcia-Estrada, Ruben Carbajo-Andres, Rafael Balana-Fouce
DNA topoisomerases (Top) are a group of isomerase enzymes responsible for controlling the topological problems caused by DNA double helix in the cell during the processes of replication, transcription and recombination. Interestingly, these enzymes have been known since long to be key molecular machines in several cellular processes through overwinding or underwinding of DNA in all-living organisms. Leishmania, a trypanosomatid parasite responsible for causing fatal diseases mostly in impoverished populations of low-income countries, have a set of six classes of Top enzymes...
May 17, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29772697/structure-activity-relationships-based-on-3d-qsar-comfa-comsia-and-design-of-aryloxypropanol-amine-agonists-with-selectivity-for-the-human-%C3%AE-3-adrenergic-receptor-and-anti-obesity-and-anti-diabetic-profiles
#12
Marcos Lorca, Cesar Morales-Verdejo, David Vásquez-Velásquez, Juan Andrades-Lagos, Javier Campanini-Salinas, Jorge Soto-Delgado, Gonzalo Recabarren-Gajardo, Jaime Mella
The wide tissue distribution of the adrenergic β3 receptor makes it a potential target for the treatment of multiple pathologies such as diabetes, obesity, depression, overactive bladder (OAB), and cancer. Currently, there is only one drug on the market, mirabegron, approved for the treatment of OAB. In the present study, we have carried out an extensive structure-activity relationship analysis of a series of 41 aryloxypropanolamine compounds based on three-dimensional quantitative structure-activity relationship (3D-QSAR) techniques...
May 16, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29772403/theoretical-study-of-the-intermolecular-recognition-mechanism-between-survivin-and-substrate-based-on-conserved-binding-mode-analysis
#13
Chao Wu, Liguang Mao, Xie Huang, Weitao Fu, Xiong Cai, Yuepiao Cai, Liqun Shen, Xiaoxia Ye
Survivin is the smallest member of IAP (inhibitor of apoptosis protein) family, which plays important roles in both mitosis and apoptosis. It has become an attractive drug target due to its overexpression in many human cancers. Survivin has been proven to bind to Smac/DIABLO protein that indirectly inhibits apoptosis. Meanwhile, it is the key subunit of chromosome passenger complex (CPC) which bind to the N-terminal tail of phosphorylated histone H3T3ph during mitosis. Up to now, Survivin directly targeting inhibitor has yet to merge since the difficulty of disrupting the protein-protein interactions (PPIs) between Survivin and its substrate proteins...
May 8, 2018: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/29772085/ligand-induced-conformational-changes-in-hsp90-monitored-time-resolved-and-label-free-towards-a-conformational-activity-screening-for-drug-discovery
#14
Jörn Güldenhaupt, Marta Amaral, Carsten Kötting, Djordje Musil, Jonas Schartner, Matthias Frech, Klaus Gerwert
A detailed investigation of protein-ligand interactions is crucial during the early drug discovery process. However, most available techniques lack either structural or temporal resolution. In contrast, ATR-FTIR spectroscopy can monitor protein-ligand interactions label-free with high spatiotemporal resolution. Here we immobilize as example the heat shock protein HSP90 on an ATR-crystal. This protein is an important molecular target for drugs against several diseases including cancer. With our novel approach we investigated a ligand induced secondary structural change...
May 17, 2018: Angewandte Chemie
https://www.readbyqxmd.com/read/29771523/phosphorus-based-probes-as-molecular-tools-for-proteome-studies-recent-advances-in-probe-development-and-applications
#15
Łukasz Joachimiak, Katarzyna M Blazewska
Studies on the human proteome have engaged diverse techniques; however, none of them represent a predominant approach. Chemical biology has made a major contribution to our understanding of human biology, stimulating the generation of biological hypotheses. Tools such as functional probes have advanced studies on biological mechanisms and helped in elucidating off-target reactivity and potential toxicities of drugs and drug candidates. Here, we accentuate the recent developments in the design and applications of phosph(on)ate-containing probes...
May 17, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29771124/genistein-ameliorates-non-alcoholic-fatty-liver-disease-by-targeting-thromboxane-a2-pathway
#16
Wenzhe Wang, Junliang Chen, Jinyan Mao, Hongling Li, Mingfu Wang, Hao Zhang, Haitao Li, Wei Chen
Non-alcoholic fatty liver disease (NAFLD) is now a public health issue worldwide, but no drug has received approval yet. Genistein, an isoflavonoid derived from soybean, ameliorates high fat diet-induced NAFLD in mice, but the molecular underpinnings remain largely elusive. Arachidonic acid is a major ingredient of animal fats, and arachidonic acid cascade has been implicated in chronic inflammation. In this study, we investigated whether genistein against NAFLD by targeting arachidonic acid cascade. By using a mouse model, we showed that genistein supplementation improved high-fat diet induced NAFLD by normalizing hepatomegaly, liver steatosis, aminotransferase abnormalities and glucose tolerance...
May 17, 2018: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/29770869/curcumin-inhibits-autocrine-growth-hormone-mediated-invasion-and-metastasis-by-targeting-nf-%C3%AE%C2%BAb-signaling-and-polyamine-metabolism-in-breast-cancer-cells
#17
Ajda Coker-Gurkan, Merve Celik, Merve Ugur, Elif-Damla Arisan, Pinar Obakan-Yerlikaya, Zeynep Begum Durdu, Narcin Palavan-Unsal
Curcumin is assumed to be a plant-derived therapeutic drug that triggers apoptotic cell death in vitro and in vivo by affecting different molecular targets such as NF-κB. Phase I/II trial of curcumin alone or with chemotherapeutic drugs has been accomplished in pancreatic, colon, prostate and breast cancer cases. Recently, autocrine growth hormone (GH) signaling-induced cell growth, metastasis and drug resistance have been demonstrated in breast cancer. In this study, our aim was to investigate the potential therapeutic effect of curcumin by evaluating the molecular machinery of curcumin-triggered apoptotic cell death via focusing on NF-κB signaling and polyamine (PA) metabolism in autocrine GH-expressing MCF-7, MDA-MB-453 and MDA-MB-231 breast cancer cells...
May 16, 2018: Amino Acids
https://www.readbyqxmd.com/read/29770579/cholinesterase-targeting-by-polyphenols-a-therapeutic-approach-for-the-treatment-of-alzheimer-s-disease
#18
REVIEW
Nasimudeen R Jabir, Fayaz Rahman Khan, Shams Tabrez
Alzheimer's disease (AD) is a progressive irreversible neurodegenerative disorder characterized by excessive deposition of β-amyloid (Aβ) oligomers, and neurofibrillary tangles (NFTs), comprising of hyperphosphorylated tau proteins. The cholinergic system has been suggested as the earliest and most affected molecular mechanism that describes AD pathophysiology. Moreover, cholinesterase inhibitors (ChEIs) are the potential class of drugs that can amplify cholinergic activity to improve cognition and global performance and reduce psychiatric and behavioral disturbances...
May 16, 2018: CNS Neuroscience & Therapeutics
https://www.readbyqxmd.com/read/29770330/the-prediction-of-drug-disease-correlation-based-on-gene-expression-data
#19
Hui Cui, Menghuan Zhang, Qingmin Yang, Xiangyi Li, Michael Liebman, Ying Yu, Lu Xie
The explosive growth of high-throughput experimental methods and resulting data yields both opportunity and challenge for selecting the correct drug to treat both a specific patient and their individual disease. Ideally, it would be useful and efficient if computational approaches could be applied to help achieve optimal drug-patient-disease matching but current efforts have met with limited success. Current approaches have primarily utilized the measureable effect of a specific drug on target tissue or cell lines to identify the potential biological effect of such treatment...
2018: BioMed Research International
https://www.readbyqxmd.com/read/29770277/a-strategy-to-find-novel-candidate-anti-alzheimer-s-disease-drugs-by-constructing-interaction-networks-between-drug-targets-and-natural-compounds-in-medical-plants
#20
Bi-Wen Chen, Wen-Xing Li, Guang-Hui Wang, Gong-Hua Li, Jia-Qian Liu, Jun-Juan Zheng, Qian Wang, Hui-Juan Li, Shao-Xing Dai, Jing-Fei Huang
Background: Alzheimer' disease (AD) is an ultimately fatal degenerative brain disorder that has an increasingly large burden on health and social care systems. There are only five drugs for AD on the market, and no new effective medicines have been discovered for many years. Chinese medicinal plants have been used to treat diseases for thousands of years, and screening herbal remedies is a way to develop new drugs. Methods: We used molecular docking to screen 30,438 compounds from Traditional Chinese Medicine (TCM) against a comprehensive list of AD target proteins...
2018: PeerJ
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