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https://www.readbyqxmd.com/read/28098893/systematic-analysis-of-microarray-datasets-to-identify-parkinson-s-disease%C3%A2-associated-pathways-and-genes
#1
Yinling Feng, Xuefeng Wang
In order to investigate commonly disturbed genes and pathways in various brain regions of patients with Parkinson's disease (PD), microarray datasets from previous studies were collected and systematically analyzed. Different normalization methods were applied to microarray datasets from different platforms. A strategy combining gene co‑expression networks and clinical information was adopted, using weighted gene co‑expression network analysis (WGCNA) to screen for commonly disturbed genes in different brain regions of patients with PD...
January 16, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28098779/unravelling-the-diversity-of-the-cyclopiazonic-acid-family-of-mycotoxins-in-aspergillus-flavus-by-uhplc-triple-tof-hrms
#2
Valdet Uka, Geromy G Moore, Natalia Arroyo-Manzanares, Dashnor Nebija, Sarah De Saeger, José Diana Di Mavungu
Cyclopiazonic acid (α-cyclopiazonic acid, α-CPA) is an indole-hydrindane-tetramic acid neurotoxin produced by various fungal species, including the notorious food and feed contaminant Aspergillus flavus. Despite its discovery in A. flavus cultures approximately 40 years ago, its contribution to the A. flavus mycotoxin burden is consistently minimized by our focus on the more potent carcinogenic aflatoxins also produced by this fungus. Here, we report the screening and identification of several CPA-type alkaloids not previously found in A...
January 13, 2017: Toxins
https://www.readbyqxmd.com/read/28098763/new-abietane-and-kaurane-type-diterpenoids-from-the-stems-of-tripterygium-regelii
#3
Dongsheng Fan, Shuangyan Zhou, Zhiyuan Zheng, Guo-Yuan Zhu, Xiaojun Yao, Ming-Rong Yang, Zhi-Hong Jiang, Li-Ping Bai
Eleven new abietane type (1‒11), and one new kaurane (12), diterpenes, together with eleven known compounds (13-23), were isolated and identified from the stems of Tripterygium regelii, which has been used as a traditional folk Chinese medicine for the treatment of rheumatoid arthritis in China. The structures of new compounds were characterized by means of the interpretation of high-resolution electrospray ionization mass spectrometry (HRESIMS), extensive nuclear magnetic resonance (NMR) spectroscopic data and comparisons of their experimental CD spectra with calculated electronic circular dichroism (ECD) spectra...
January 13, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28098484/romanowsky-staining-the-romanowsky-effect-and-thoughts-on-the-question-of-scientific-priority
#4
A V Bezrukov
I give an historical account and analysis of the scientific priority of the discovery of the polychrome staining of microscopic biological preparations provided by mixtures of eosin plus methylene blue and its derivatives, especially azure B. I maintain that both the formal priority for the discovery of the polychrome staining phenomenon and credit for initiating the development of a technique of polychrome staining properly belong to D. L. Romanowsky. His scientific work demonstrated the possibility of using a simple technique to stain hematological preparations selectively to give good contrast, high resolution and the ability to identify malaria parasites...
January 18, 2017: Biotechnic & Histochemistry: Official Publication of the Biological Stain Commission
https://www.readbyqxmd.com/read/28098449/targeting-type-2-diabetes-with-c-glucosyl-dihydrochalcones-as-selective-sodium-glucose-co-transporter-2-sglt2-inhibitors-synthesis-and-biological-evaluation
#5
Ana R Jesus, Diogo Vila-Viçosa, Miguel Machuqueiro, Ana P Marques, Timothy M Dore, Amélia P Rauter
Inhibiting glucose reabsorption by sodium glucose co-transporter proteins (SGLTs) in the kidneys is a relatively new strategy for treating type 2 diabetes. Selective inhibition of SGLT2 over SGLT1 is critical for minimizing adverse side effects associated with SGLT1 inhibition. A library of C-glucosyl dihydrochalcones and their dihydrochalcone and chalcone precursors was synthesized and tested as SGLT1/SGLT2 inhibitors using a cell-based fluorescence assay of glucose uptake. The most potent inhibitors of SGLT2 (IC50 = 9-23 nM) were considerably weaker inhibitors of SGLT1 (IC50 = 10-19 μM)...
January 18, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28098396/the-effects-of-chronic-cobalt-and-chromium-exposure-after-metal-on-metal-hip-resurfacing-an-epigenome-wide-association-pilot-study
#6
Julia Steinberg, Karan M Shah, Alison Gartland, Eleftheria Zeggini, J Mark Wilkinson
Metal-on-metal (MOM) hip resurfacing has recently been a popular prosthesis choice for the treatment of symptomatic arthritis, but results in the release of cobalt and chromium ions into the circulation that can be associated with adverse clinical effects. The mechanism underlying these effects remains unclear. While chromosomal aneuploidy and translocations are associated with this exposure, the presence of subtle structural epigenetic modifications in patients with MOM joint-replacements remains unexplored...
January 18, 2017: Journal of Orthopaedic Research: Official Publication of the Orthopaedic Research Society
https://www.readbyqxmd.com/read/28098342/the-evolution-of-rgs-proteins-as-drug-targets-20%C3%A2-years-in-the-making-iuphar-review-x
#7
REVIEW
B Sjögren
Regulators of G protein signaling (RGS) proteins are celebrating the 20(th) anniversary of their discovery. The unveiling of this new family of negative regulators of G protein signaling in the mid-1990's solved a persistent conundrum in the G protein signaling field, in which the rate of deactivation of signaling cascades in vivo could not be replicated in exogenous systems. Since then, there has been tremendous advancement in the knowledge of RGS protein structure, function, regulation and their role as novel drug targets...
January 18, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28098285/kb-po4-f-a-novel-acentric-deep-ultraviolet-material
#8
Ji-Hong Jiang, Lin-Chuan Zhang, Ya-Xi Huang, Zhi-Mei Sun, Yuanming Pan, Jin-Xiao Mi
Two challenges to grow KBe2BO3F2 (KBBF), the best known deep-ultraviolet nonlinear optical (NLO) material to date, are the limited crystal sizes and the use of a highly toxic element (Be). Herein we report on the discovery of a novel anhydrous non-centrosymmetric alkali fluorinated borophosphate KB(PO4)F (KBPF) featuring a cut-off wavelength of less than 200 nm and a large second-harmonic generation (SHG) effect similar to KH2PO4 (KDP), hence representing a new promising deep-ultraviolet NLO material. The KBPF crystals consisting of common elements can be grown using green and cost effective processes and do not show any detectable hygroscopicity...
January 18, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/28098260/hepatitis-b-virus-x-protein-is-capable-of-down-regulating-protein-level-of-host-antiviral-protein-apobec3g
#9
Ruidong Chen, Xue Zhao, Yongxiang Wang, Youhua Xie, Jing Liu
The apolipoprotein B mRNA editing catalytic polypeptide-like (APOBEC) family proteins bind RNA and single-stranded DNA, and create C-to-U base modifications through cytidine deaminase activity. APOBEC3G restricts human immunodeficiency virus 1 (HIV-1) infection by creating hypermutations in proviral DNA, while HIV-1-encoded vif protein antagonizes such restriction by targeting APOBEC3G for degradation. APOBEC3G also inhibits hepatitis B virus (HBV): APOBEC3G co-expression inhibits HBV replication and evidences exist indicating APOBEC3G-mediated HBV hypermutations in patients...
January 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28098202/superresolution-imaging-of-clinical-formalin-fixed-paraffin-embedded-breast-cancer-with-single-molecule-localization-microscopy
#10
Matthew K Creech, Jing Wang, Xiaolin Nan, Summer L Gibbs
Millions of archived formalin-fixed, paraffin-embedded (FFPE) specimens contain valuable molecular insight into healthy and diseased states persevered in their native ultrastructure. To diagnose and treat diseases in tissue on the nanoscopic scale, pathology traditionally employs electron microscopy (EM), but this platform has significant limitations including cost and painstaking sample preparation. The invention of single molecule localization microscopy (SMLM) optically overcame the diffraction limit of light to resolve fluorescently labeled molecules on the nanoscale, leading to many exciting biological discoveries...
January 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28098147/nanoparticle-induced-unusual-melting-and-solidification-behaviours-of-metals
#11
Chao Ma, Lianyi Chen, Chezheng Cao, Xiaochun Li
Effective control of melting and solidification behaviours of materials is significant for numerous applications. It has been a long-standing challenge to increase the melted zone (MZ) depth while shrinking the heat-affected zone (HAZ) size during local melting and solidification of materials. In this paper, nanoparticle-induced unusual melting and solidification behaviours of metals are reported that effectively solve this long-time dilemma. By introduction of Al2O3 nanoparticles, the MZ depth of Ni is increased by 68%, while the corresponding HAZ size is decreased by 67% in laser melting at a pulse energy of 0...
January 18, 2017: Nature Communications
https://www.readbyqxmd.com/read/28097905/discovery-of-novel-dual-inhibitors-of-receptor-tyrosine-kinases-egfr-and-igf-1r
#12
Cornelius Hempel, Frank Totzke, Christoph Schächtele, Abdulkarim Najjar, Wolfgang Sippl, Christoph Ritter, Andreas Hilgeroth
Novel 4-benzylamino benzo-anellated pyrrolo[2,3-b]pyridines have been synthesized with varied substitution patterns both at the molecular scaffold of the benzo-anellated ring and at the 4-benzylamino residue. With a structural similarity to substituted thieno[2,3-d]pyrimidines as epidermal growth factor receptor (EGFR) inhibitors, we characterized the inhibition of EGFR for our novel compounds. As receptor heterodimerization gained certain interest as mechanism of cancer cells to become resistant against novel protein kinase inhibitors, we additionally measured the inhibition of insulin-like growth factor receptor IGF-1R which is a prominent receptor for such heterodimerizations with EGFR...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097901/skin-whitening-agents-medicinal-chemistry-perspective-of-tyrosinase-inhibitors
#13
Thanigaimalai Pillaiyar, Manoj Manickam, Vigneshwaran Namasivayam
Melanogenesis is a process to synthesize melanin, which is a primary responsible for the pigmentation of human skin, eye and hair. Although numerous enzymatic catalyzed and chemical reactions are involved in melanogenesis process, the enzymes such as tyrosinase and tyrosinase-related protein-1 (TRP-1) and TRP-2 played a major role in melanin synthesis. Specifically, tyrosinase is a key enzyme, which catalyzes a rate-limiting step of the melanin synthesis, and the downregulation of tyrosinase is the most prominent approach for the development of melanogenesis inhibitors...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097887/pseudokinases-update-on-their-functions-and-evaluation-as-new-drug-targets
#14
Dominic P Byrne, Daniel M Foulkes, Patrick A Eyers
The pseudokinase complement of the human kinase superfamily consists of approximately 60 signaling proteins, which lacks one or more of the amino acids typically required to correctly align ATP and metal ions, and phosphorylate protein substrates. Recent studies in the pseudokinase field have begun to expose the biological relevance of pseudokinases, which are now thought to perform a diverse range of physiological roles and are connected to a multitude of human diseases, including cancer. In this review, we discuss how and why members of the 'pseudokinome' represent important new targets for drug discovery, and describe how knowledge of protein structure and function provides informative clues to help guide the rational chemical design or repurposing of inhibitors to target pseudokinases...
January 18, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28097886/reagent-free-lc-ms-ms-based-pharmacokinetic-quantification-of-polyhistidine-tagged-therapeutic-proteins
#15
Jianxia Shi, Jing Man Wong, Ji Ma, Tiffany Dickerson, Colin Hall, Dan A Rock, Timothy J Carlson
AIM: Immobilized metal ion affinity chromatography is widely employed for purifying polyhistidine-tagged recombinant proteins from cell lysates. The technique can be applied for quantification of therapeutic proteins in biological matrices by LC-MS/MS. RESULTS: A protein reagent-free workflow was developed for quantifying polyhistidine-tagged proteins by LC-MS/MS. The workflow includes target protein enrichment by immobilized metal ion affinity chromatography, on-bead trypsin digestion and quantification of signature peptides by LC-MS/MS...
January 18, 2017: Bioanalysis
https://www.readbyqxmd.com/read/28097822/synthetic-lethality-emerging-targets-and-opportunities-in-melanoma
#16
REVIEW
Nicola Thompson, David Adams, Marco Ranzani
Great progress has been made in the treatment of melanoma through use of targeted therapies and immunotherapy. One approach that has not been fully explored is synthetic lethality, which exploits somatically acquired changes, usually driver mutations, to specifically kill tumour cells. We outline the various approaches that may be applied to identify synthetic lethal interactions and define how these interactions may drive drug discovery efforts. This article is protected by copyright. All rights reserved.
January 17, 2017: Pigment Cell & Melanoma Research
https://www.readbyqxmd.com/read/28097798/discovery-of-novel-cinchona-alkaloid-inspired-oxazatwistane-autophagy-inhibitors
#17
Luca Laraia, Kosuke Ohsawa, Georgios Konstantinidis, Lucas Robke, Yao-Wen Wu, Kamal Kumar, Herbert Waldmann
The cinchona alkaloids are a privileged class of natural products and are endowed with diverse bioactivities. However, for compounds with the closely-related oxazatricyclo[4.4.0.0]decane ("oxazatwistane") scaffold, which are accessible from cinchonidine and quinidine by means of ring distortion and modification, biological activity has not been identified. We report the synthesis of an oxazatwistane compound collection through employing state-of-the-art C-H functionalization, and metal-catalyzed cross-coupling reactions as key late diversity-generating steps...
January 18, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28097765/a-false-positive-screening-hit-in-fragment-based-lead-discovery-watch-out-for-the-red-herring
#18
Jonathan Cramer, Johannes Schiebel, Tobias Wulsdorf, Kristof Grohe, Eszter Eva Najbauer, Frederik R Ehrmann, Nedyalka Radeva, Nina Zitzer, Uwe Linne, Rasmus Linser, Andreas Heine, Gerhard Klebe
With the rising popularity of fragment-based approaches in drug development, more and more attention has to be devoted to the detection of false-positive screening results. In particular, the small size and low affinity of fragments drives screening techniques to their limit. The pursuit of a false-positive hit can cause significant loss of time and resources. Here, we present an instructive and intriguing investigation into the origin of misleading assay results for a fragment that emerged as the most potent binder for the aspartic protease endothiapepsin (EP) across multiple screening assays...
January 18, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28097641/natural-products-diversity-of-marine-ascidians-tunicates-ascidiacea-and-successful-drugs-in-clinical-development
#19
REVIEW
Satheesh Kumar Palanisamy, N M Rajendran, Angela Marino
This present study reviewed the chemical diversity of marine ascidians and their pharmacological applications, challenges and recent developments in marine drug discovery reported during 1994-2014, highlighting the structural activity of compounds produced by these specimens. Till date only 5% of living ascidian species were studied from <3000 species, this study represented from family didemnidae (32%), polyclinidae (22%), styelidae and polycitoridae (11-12%) exhibiting the highest number of promising MNPs...
January 17, 2017: Natural Products and Bioprospecting
https://www.readbyqxmd.com/read/28097425/a-personal-perspective-on-the-discovery-of-dioxygen-adducts-of-copper-and-iron-by-nobumasa-kitajima
#20
REVIEW
Kiyoshi Fujisawa
Transition metal-dioxygen complexes have fascinated bioinorganic and inorganic chemists for over half a century. The late Nobumasa Kitajima was one of the very successful researchers in this field. Despite his short career (40 years old), he made many important contributions. This Commentary highlights his important accomplishments and how they have impacted subsequent work in this area.
January 17, 2017: Journal of Biological Inorganic Chemistry: JBIC
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