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https://www.readbyqxmd.com/read/28646757/discovery-and-structure-activity-relationship-studies-of-2-benzylidene-2-3-dihydro-1h-inden-1-one-and-benzofuran-3-2h-one-derivatives-as-a-novel-class-of-potential-therapeutics-for-inflammatory-bowel-disease
#1
Tara Man Kadayat, Suhrid Banskota, Pallavi Gurung, Ganesh Bist, Til Bahadur Thapa Magar, Aarajana Shrestha, Jung-Ae Kim, Eung-Seok Lee
To develop effective therapeutics for inflammatory bowel disease (IBD), 2-benzylidene-2,3-dihydro-1H-inden-1-one and benzofuran-3(2H)-one derivatives, were designed and synthesized and their structure-activity relationships (SAR) were investigated. Compounds 7, 25, 26, 32, 39, 41, 52, 54, and 55 showed potent inhibitory effect (>70%) on the TNF-α-induced adhesion of monocytes to colon epithelial cells, which is one of the hallmark events leading to IBD. Such inhibitory activity of the compounds correlated with their suppressive activities against the TNF-α-induced production of ROS; ICAM-1 and MCP-1 expression, critical molecules involved in monocyte-epithelial adhesion; and NF-κB transcriptional activity...
June 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28646678/bioengineering-for-intestinal-organoid-cultures
#2
REVIEW
Ge-Ah Kim, Jason R Spence, Shuichi Takayama
Recent advances allow access to human cell-based intestinal organoids that recreate human physiology to levels not possible with conventional 2D cell cultures. Despite their huge potential, there are many challenges that remain. This review will cover recent bioengineering approaches to improve organoid maturation, scale up, reproducibility and analysis. The first section covers the advances in engineering the culture environment, followed by the section on tools for micro-manipulation and analysis of organoids...
June 21, 2017: Current Opinion in Biotechnology
https://www.readbyqxmd.com/read/28646634/marinisporobacter-balticus-gen-nov-sp-nov-desulfosporosinus-nitroreducens-sp-nov-and-desulfosporosinus-fructosivorans-sp-nov-new-spore-forming-bacteria-isolated-from-subsurface-sediments-of-the-baltic-sea
#3
Verona Vandieken, Helge Niemann, Bert Engelen, Heribert Cypionka
Four novel Gram-stain-positive, endospore-forming bacteria of the order Clostridiales were isolated from subsurface sediments sampled during International Ocean Discovery Program Expedition 347 to the Baltic Sea. One strain (59.4MT) grew as an obligate heterotroph by aerobic respiration and anaerobically by fermentation. Optimum growth was observed with 0.5 % NaCl at 25 °C and pH 7.0-7.3. Analysis of 16S rRNA gene sequences of 59.4MT revealed Alkaliphilus transvaalensis (92.3 % identity), Candidatus Geosporobacter ferrireducens (92...
June 20, 2017: International Journal of Systematic and Evolutionary Microbiology
https://www.readbyqxmd.com/read/28646631/synthesis-of-novel-and-functionally-selective-non-competitive-muscarinic-antagonists-as-chemical-probes
#4
John F Boulos, Jan Jakubik, John M Boulos, Jelena Momirov, Alena Randakova
Muscarinic receptors are known to play important biological roles and are drug targets for several human diseases. In a pilot study, novel muscarinic antagonists were synthesized and used as chemical probes to obtain additional information of the muscarinic pharmacophore. The design of these ligands made use of current orthosteric and allosteric models of drug-receptor interactions together with chemical motifs known to achieve muscarinic receptor selectivity. This approach has led to the discovery of several non-competitive muscarinic ligands that strongly bind at a secondary receptor site...
June 24, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28646586/vaccine-candidate-discovery-for-the-next-generation-of-malaria-vaccines
#5
REVIEW
James Tuju, Gathoni Kamuyu, Linda M Murungi, Faith H A Osier
Although epidemiological observations, IgG passive transfer studies and experimental infections in humans all support the feasibility of developing highly effective malaria vaccines, the precise antigens that induce protective immunity remain uncertain. Here, we review the methodologies applied to vaccine candidate discovery for Plasmodium falciparum malaria from the pre- to post- genomic era. Probing of genomic and/or cDNA libraries with antibodies of defined specificities or functional activity predominated the former, while reverse vaccinology encompassing high throughput in silico analyses of genomic, transcriptomic or proteomic parasite datasets is the mainstay of the latter...
June 24, 2017: Immunology
https://www.readbyqxmd.com/read/28646512/wmj-8-b-a-novel-hydroxamate-derivative-induces-mda-mb-231-breast-cancer-cell-death-via-shp-1-stat3-survivin-cascade
#6
Yu-Fan Chuang, Shiu-Wen Huang, Ya-Fen Hsu, Meng-Chieh Yu, George Ou, Wei-Jan Huang, Ming-Jen Hsu
BACKGROUND AND PURPOSE: Histone deacetylase (HDAC) inhibitors with broad-spectrum anti-tumor properties has been described and attracted lots of attention in the field of drug discovery. However, the underlying anti-tumor mechanisms of HDAC inhibitors remain incompletely understood. In this study, we aimed to characterize the underlying mechanisms of a novel hydroxamate-based HDAC inhibitor, WMJ-8-B, in inducing MDA-MB-231 breast cancer cell death. EXPERIMENTAL APPROACH: WMJ-8-B's effects on cell viability, cell cycle distribution, apoptosis, as well as signaling molecules modification and activation were analyzed by MTT assay, flowcytometric analysis, immunoblotting, reporter assay, ChIP analysis and siRNA strategy...
June 23, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28646443/recent-discoveries-in-monogenic-disorders-of-childhood-bone-fragility
#7
REVIEW
Riikka E Mäkitie, Anders J Kämpe, Fulya Taylan, Outi Mäkitie
PURPOSE OF REVIEW: This review summarizes our current knowledge on primary osteoporosis in children with focus on recent genetic findings. RECENT FINDINGS: Advances in genetic research, particularly next-generation sequencing, have found several genetic loci that associate with monogenic forms of inherited osteoporosis, widening the scope of primary osteoporosis beyond classical osteogenesis imperfecta. New forms of primary osteoporosis, such as those related to WNT1, PLS3, and XYLT2, have identified defects outside the extracellular matrix components and collagen-related pathways, in intracellular cascades directly affecting bone cell function...
June 23, 2017: Current Osteoporosis Reports
https://www.readbyqxmd.com/read/28646174/a-gpu-accelerated-algorithm-for-biclustering-analysis-and-detection-of-condition-dependent-coexpression-network-modules
#8
Anindya Bhattacharya, Yan Cui
In the analysis of large-scale gene expression data, it is important to identify groups of genes with common expression patterns under certain conditions. Many biclustering algorithms have been developed to address this problem. However, comprehensive discovery of functionally coherent biclusters from large datasets remains a challenging problem. Here we propose a GPU-accelerated biclustering algorithm, based on searching for the largest Condition-dependent Correlation Subgroups (CCS) for each gene in the gene expression dataset...
June 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28646015/determination-of-the-heart-to-mediastinum-ratio-of-123-i-mibg-uptake-using-dual-isotope-123-i-mibg-99m-tc-tetrofosmin-multi-pinhole-czt-spect-in-patients-with-heart-failure
#9
Tanguy Blaire, Alban Bailliez, Fayçal Ben Bouallègue, Dimitri Bellevre, Denis Agostini, Alain Manrique
The aim of this retrospective study was to determine the heart-to-mediastinum ratio (HMR) of (123)I-metaiodobenzylguanidine (MIBG) uptake obtained using a multi-pinhole cadmium-zinc-telluride (CZT)-based camera (Discovery NM 530c, DNM-530c, GE Healthcare, Milwaukee, WI, USA) in comparison with that obtained using conventional planar imaging (Infinia, GE Healthcare, Milwaukee, WI, USA). Methods: Forty consecutive heart failure patients underwent planar acquisition 4 h after (123)I-MIBG injection (191±41 MBq)...
June 23, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28645963/effectiveness-and-safety-of-moxibustion-treatment-for-non-specific-lower-back-pain-protocol-for-a-systematic-review
#10
Jungtae Leem, Seunghoon Lee, Yeoncheol Park, Byung-Kwan Seo, Yeeun Cho, Jung Won Kang, Yoon Jae Lee, In-Hyuk Ha, Hyun-Jong Lee, Eun-Jung Kim, Sanghoon Lee, Dongwoo Nam
INTRODUCTION: Many patients experience acute lower back pain that becomes chronic pain. The proportion of patients using complementary and alternative medicine to treat lower back is increasing. Even though several moxibustion clinical trials for lower back pain have been conducted, the effectiveness and safety of moxibustion intervention is controversial. The purpose of this study protocol for a systematic review is to evaluate the effectiveness and safety of moxibustion treatment for non-specific lower back pain patients...
June 23, 2017: BMJ Open
https://www.readbyqxmd.com/read/28645929/biophysical-stimulation-for-in%C3%A2-vitro-engineering-of-functional-cardiac-tissues
#11
REVIEW
Anastasia Korolj, Erika Yan Wang, Robert A Civitarese, Milica Radisic
Engineering functional cardiac tissues remains an ongoing significant challenge due to the complexity of the native environment. However, our growing understanding of key parameters of the in vivo cardiac microenvironment and our ability to replicate those parameters in vitro are resulting in the development of increasingly sophisticated models of engineered cardiac tissues (ECT). This review examines some of the most relevant parameters that may be applied in culture leading to higher fidelity cardiac tissue models...
July 1, 2017: Clinical Science (1979-)
https://www.readbyqxmd.com/read/28645859/discovery-of-a-novel-pan-raf-inhibitor-with-potent-anti-tumor-activity-in-preclinical-models-of-braf-v600e-mutant-cancer
#12
Sung Pyo Hong, Soon Kil Ahn
AIMS: BRAF mutations, especially BRAF V600E, are a frequent occurrence in malignant melanomas. The BRAF inhibitors are used as the care standard for BRAF-mutant metastatic melanomas. However, melanomas rapidly develop resistance to BRAF inhibitors after a median response duration of 6months, and the subsequent rapid development of cutaneous toxicity is enhanced by the paradoxical activation of CRAF. In this study, we discovered a potent and selective pan-RAF inhibitor: INU-152. The goal of this study was to investigate whether the inhibition of pan-RAF with INU-152 completely disrupts the MAPK pathway in cancer cells bearing BRAF or RAS mutations...
June 20, 2017: Life Sciences
https://www.readbyqxmd.com/read/28645852/g0s2-a-small-giant-controller-of-lipolysis-and-adipose-liver-fatty-acid-flux
#13
REVIEW
Xiaodong Zhang, Bradlee L Heckmann, Latoya E Campbell, Jun Liu
The discovery of adipose triglyceride lipase (ATGL) and its coactivator comparative gene identification-58 (CGI-58) provided a major paradigm shift in the understanding of intracellular lipolysis in both adipocytes and nonadipocyte cells. The subsequent discovery of G0/G1 switch gene 2 (G0S2) as a potent endogenous inhibitor of ATGL revealed a unique mechanism governing lipolysis and fatty acid (FA) availability. G0S2 is highly conserved in vertebrates, and exhibits cyclical expression pattern between adipose tissue and liver that is critical to lipid flux and energy homeostasis in these two tissues...
June 20, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28645536/imaging-genetics-of-schizophrenia-in-the-post-gwas-era
#14
REVIEW
Ayla Arslan
Imaging genetics is a research methodology studying the effect of genetic variation on brain structure, function, behavior, and risk for psychopathology. Since the early 2000s, imaging genetics has been increasingly used in the research of schizophrenia (SZ). SZ is a severe mental disorder with no precise knowledge of its underlying neurobiology, however, new genetic and neurobiological data generate a climate for new avenues. The accumulating data of genome wide association studies (GWAS) continuously decode SZ risk genes...
June 20, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28645531/new-protein-structures-provide-an-updated-understanding-of-phenylketonuria
#15
REVIEW
Eileen K Jaffe
Phenylketonuria (PKU) and less severe hyperphenylalaninemia (HPA) constitute the most common inborn error of amino acid metabolism, and is most often caused by defects in phenylalanine hydroxylase (PAH) function resulting in accumulation of Phe to neurotoxic levels. Despite the success of dietary intervention in preventing permanent neurological damage, individuals living with PKU clamor for additional non-dietary therapies. The bulk of disease-associated mutations are PAH missense variants, which occur throughout the entire 452 amino acid human PAH protein...
June 15, 2017: Molecular Genetics and Metabolism
https://www.readbyqxmd.com/read/28645376/proteomic-analyses-of-the-eukaryotic-replication-machinery
#16
David Cortez
DNA replication in a human cell involves hundreds of proteins that copy the DNA accurately and completely each cell division cycle. In addition to the core DNA copying machine (the replisome), accessory proteins work to respond to replication stress, correct errors, and repackage the DNA into appropriate chromatin structures. New proteomic tools have been invented in the past few years to facilitate the purification, identification, and quantification of the replication, chromatin maturation, and replication stress response machineries...
2017: Methods in Enzymology
https://www.readbyqxmd.com/read/28645356/-endocrine-control-of-serum-phosphate-from-the-discoveries-of-phosphatonins-to-novel-therapies
#17
A Linglart, C Chaussain
Phosphate is absorbed through the gut, stored in the bone and reabsorbed through the proximal renal tubule. More importantly, PTH and FGF23 have been identified as the main phosphaturic factors that control the expression of the phosphate co-transporters NaPi-IIa et IIc. By allowing the adjustment of the urinary phosphate reabsorption, these two phosphatonins play a major role in bone and tooth mineralization and growth. Recently, novel therapies have successfully targeted the FGF23 signaling pathway to treat the hypophosphatemia in patients affected with molecular defects of this pathway (mutations in the PHEX gene)...
October 2016: Annales D'endocrinologie
https://www.readbyqxmd.com/read/28645323/early-response-index-a-statistic-to-discover-potential-early-stage-disease-biomarkers
#18
Sirajul Salekin, Mehrab Ghanat Bari, Itay Raphael, Thomas G Forsthuber, Jianqiu Michelle Zhang
BACKGROUND: Identifying disease correlated features early before large number of molecules are impacted by disease progression with significant abundance change is very advantageous to biologists for developing early disease diagnosis biomarkers. Disease correlated features have relatively low level of abundance change at early stages. Finding them using existing bioinformatic tools in high throughput data is a challenging task since the technology suffers from limited dynamic range and significant noise...
June 23, 2017: BMC Bioinformatics
https://www.readbyqxmd.com/read/28645295/identification-of-the-flotillin-1-2-heterocomplex-as-a-target-of-autoantibodies-in-bona-fide-multiple-sclerosis
#19
S Hahn, G Trendelenburg, M Scharf, Y Denno, S Brakopp, B Teegen, C Probst, K P Wandinger, M Buttmann, A Haarmann, F Szabados, M Vom Dahl, T Kümpfel, P Eichhorn, H Gold, F Paul, S Jarius, N Melzer, W Stöcker, L Komorowski
BACKGROUND: Autoantibodies, in particular those against aquaporin-4 and myelin-oligodendrocyte glycoprotein (MOG), aid as biomarkers in the differential diagnosis of demyelination. Here, we report on discovery of autoantibodies against flotillin in patients with multiple sclerosis (MS). METHODS: The target antigen was identified by histo-immunoprecipitation using the patients' sera and cryosections of rat or pig cerebellum combined with mass spectrometrical analysis...
June 23, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/28645238/new-world-arenavirus-biology
#20
Nicolás Sarute, Susan R Ross
Hemorrhagic fevers caused by viruses were identified in the late 1950s in South America. These viruses have existed in their hosts, the New World rodents, for millions of years. Their emergence as infectious agents in humans coincided with changes in the environment and farming practices that caused explosions in their host rodent populations. Zoonosis into humans likely occurs because the pathogenic New World arenaviruses use human transferrin receptor 1 to enter cells. The mortality rate after infection with these viruses is high, but the mechanism by which disease is induced is still not clear...
June 23, 2017: Annual Review of Virology
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