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https://www.readbyqxmd.com/read/28534954/uncaria-alkaloids-reverse-abcb1-mediated-cancer-multidrug-resistance
#1
Bao-Yuan Huang, Yu Zeng, Ying-Jie Li, Xiao-Jun Huang, Nan Hu, Nan Yao, Min-Feng Chen, Zai-Gang Yang, Zhe-Sheng Chen, Dong-Mei Zhang, Chang-Qing Zeng
The overexpression of ATP-binding cassette (ABC) transporters is the main cause of cancer multidrug resistance (MDR), which leads to chemotherapy failure. Uncaria alkaloids are the major active components isolated from uncaria, which is a common Chinese herbal medicine. In this study, the MDR-reversal activities of uncaria alkaloids, including rhynchophylline, isorhynchophylline, corynoxeine, isocorynoxeine (Icory), hirsutine and hirsuteine, were screened; they all exhibited potent reversal efficacy when combined with doxorubicin...
May 17, 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28534562/k-junction-structure-mediated-exponential-signal-amplification-strategy-for-microrna-detection-in-electrochemiluminescence-biosensor
#2
Xue Li, Anyi Chen, Yaqin Chai, Ruo Yuan
Based on the novel designed K-junction structure, an economic and efficient exponential signal amplification strategy with simple protocol combining hemin/G-quadruplex, a mimetic peroxidase, as a catalyzer was proposed and utilized in an electrochemiluminescence biosensor for sensitive microRNA detection. It was noteworthy that the K-junction structure was formed with guanine-rich reporter DNA and substrate DNA modified by phosphate at the 5'-terminus. Thus, the activity of the reporter DNA could be inhibited and the recognition domain for the target microRNA constructed through the K-junction structure formed...
May 23, 2017: Analyst
https://www.readbyqxmd.com/read/28534506/lsd1-demethylates-hif1%C3%AE-to-inhibit-hydroxylation-and-ubiquitin-mediated-degradation-in-tumor-angiogenesis
#3
J-Y Lee, J-H Park, H-J Choi, H-Y Won, H-S Joo, D-H Shin, M K Park, B Han, K P Kim, T J Lee, C M Croce, G Kong
Lysine-specific demethylase 1 (LSD1), which has been considered as a potential therapeutic target in human cancer, has been known to regulate many biological functions through its non-histone substrates. Although LSD1-induced hypoxia-inducible factor alpha (HIF1α) demethylation has recently been proposed, the effect of LSD1 on the relationship between HIF1α post-translational modifications (PTMs) and HIF1α-induced tumor angiogenesis remains to be elucidated. Here, we identify a new methylation site of the HIF1α protein antagonized by LSD1 and the interplay between HIF1α protein methylation and other PTMs in regulating tumor angiogenesis...
May 22, 2017: Oncogene
https://www.readbyqxmd.com/read/28534368/study-on-the-molecular-mechanism-of-rac3-on-regulating-autophagy-in-human-lung-cancer-cells
#4
Xuyang Xiao, Gebang Wang, Hongxu Liu
PURPOSE: Rac3 plays an important role in regulating tumorigenesis. Autophagy plays a vital role in tumorigenesis and tumor progression. The relationship between the two remains unclear. The objective of the present study was to determine the specific molecular mechanism of intracellular Rac3 in regulating autophagy and reveal the relationship between tumor cell autophagy and apoptosis. METHODS: A laser confocal microscope was used to photograph the accumulated EGFP-MAP1LC3 spots for investigating the relationship between Rac3 and autophagy at the cellular level...
March 2017: Journal of B.U.ON.: Official Journal of the Balkan Union of Oncology
https://www.readbyqxmd.com/read/28533220/triptolide-assisted-phosphorylation-of-p53-suppresses-inflammation-induced-nf-%C3%AE%C2%BAb-survival-pathways-in-cancer-cells
#5
Li Zheng, Jia Jia, Huifang Dai, Lei Wan, Jian Liu, Lin Hu, Mian Zhou, Michael Qiu, Xufeng Chen, Lufen Chang, Jae Y Kim, Karen Reckamp, Dan J Raz, Zongping Xia, Binghui Shen
Chronic inflammation plays important roles in cancer initiation and progression. Resolving chronic inflammation or blocking inflammatory signal transduction may prevent cancer development. Here, we report that the combined low-dose use of two anti-inflammatory drugs, aspirin and triptolide, reduces spontaneous lung cancer incidence from 70% to 10% in a mouse model. Subsequent studies reveal that such treatment has little effect in resolving chronic inflammatory conditions in the lung, but it significantly blocks NF-κB-mediated expression of proliferation and survival genes in cancer cells...
May 22, 2017: Molecular and Cellular Biology
https://www.readbyqxmd.com/read/28533092/thiol-reactive-drug-substrates-of-human-p-glycoprotein-label-the-same-sites-to-activate-atpase-activity-in-membranes-or-dodecyl-maltoside-detergent-micelles
#6
Tip W Loo, David M Clarke
P-glycoprotein (P-gp, ABCB1) is an ABC drug pump that is clinically important because it is involved in multidrug resistance. Many studies have used purified P-gp in detergent (n-dodecyl-β-D-maltoside; DM) micelles to map the locations of the drug-binding sites. A potential problem is that DM could be a substrate and affect binding of drugs to P-gp. To test whether DM was a substrate of P-gp, we used an assay involving drug-rescue of the immature 150 kDa misprocessed P-gp mutant (L1260A) to show that DM is not substrate...
May 19, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28532474/detection-of-ikk%C3%AE%C2%B5-by-immunohistochemistry-in-primary-breast-cancer-association-with-egfr-expression-and-absence-of-lymph-node-metastasis
#7
Virginie Williams, Andrée-Anne Grosset, Natalia Zamorano Cuervo, Yves St-Pierre, Marie-Pierre Sylvestre, Louis Gaboury, Nathalie Grandvaux
BACKGROUND: IKKε is an oncogenic kinase that was found amplified and overexpressed in a substantial percentage of human breast cancer cell lines and primary tumors using genomic and gene expression analyses. Molecular studies have provided the rational for a key implication of IKKε in breast cancer cells proliferation and invasiveness through the phosphorylation of several substrates. METHODS: Here, we performed immunohistochemical detection of IKKε expression on tissue microarrays constituted of 154 characterized human breast cancer tumors...
May 22, 2017: BMC Cancer
https://www.readbyqxmd.com/read/28532071/in-vitro-antibacterial-and-cytotoxic-activities-of-plasma-modified-polyethylene-terephthalate-nonwoven-dressing-with-aqueous-extract-of-rhizome-atractylodes-macrocephala
#8
Yi-Ting Shu, Kuo-Ting Kao, Ching-Sung Weng
In this study, a natural and non-cytotoxic antibacterial dressing containing aqueous extract of Rhizome Atractylodes macrocephala (RAM), which has been widely used in traditional herbal medicine and documented with antibacterial activities in literatures, was developed by aid of the extraction technique, nonwoven substrates and plasma-induced grafting technology. The effectiveness of these herbal antibacterial dressings with different treatment were investigated through the assays of grafting yield, SEM, FTIR, antibacterial activities and cytotoxicity...
August 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28532068/synthetic-peptides-derived-from-salivary-proteins-and-the-control-of-surface-charge-densities-of-dental-surfaces-improve-the-inhibition-of-dental-calculus-formation
#9
Bernd Grohe
Peptides descended from the salivary proteins statherin and histatin were recently identified in saliva and the acquired enamel pellicle (AEP), a proteomic layer coated on enamel. In particular, the statherin phosphopeptide DpSpSEEKFLR (DSS) was found to adsorb to enamel-like hydroxyapatite and inhibit plaque-related crystal formation. To determine the mechanism of these processes, we studied peptide-crystal interactions based on the sequences DSS and RKFHEKHHSHRGYR (RKF). The latter is a basic histatin sequence showing antimicrobial effects...
August 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28530791/farnesyltransferase-mediated-delivery-of-a-covalent-inhibitor-overcomes-alternative-prenylation-to-mislocalize-k-ras
#10
Christopher J Novotny, Gregory L Hamilton, Frank McCormick, Kevan Shokat
Mutationally activated Ras is one of the most common oncogenic drivers found across all malignancies, and its selective inhibition has long been a goal in both pharma and academia. One of the oldest and most validated methods to inhibit overactive Ras signaling is by interfering with its post-translational processing and subsequent cellular localization. Previous attempts to target Ras processing led to the development of farnesyltransferase inhibitors, which can inhibit H-Ras localization but not K-Ras due to its ability to bypass farnesyltransterase inhibition though alternative prenylation by geranylgeranyltransferase...
May 22, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28530711/a-combinatorial-screen-of-the-cloud-uncovers-a-synergy-targeting-the-androgen-receptor
#11
Marco P Licciardello, Anna Ringler, Patrick Markt, Freya Klepsch, Charles-Hugues Lardeau, Sara Sdelci, Erika Schirghuber, André C Müller, Michael Caldera, Anja Wagner, Rebecca Herzog, Thomas Penz, Michael Schuster, Bernd Boidol, Gerhard Dürnberger, Yasin Folkvaljon, Pär Stattin, Vladimir Ivanov, Jacques Colinge, Christoph Bock, Klaus Kratochwill, Jörg Menche, Keiryn L Bennett, Stefan Kubicek
Approved drugs are invaluable tools to study biochemical pathways, and further characterization of these compounds may lead to repurposing of single drugs or combinations. Here we describe a collection of 308 small molecules representing the diversity of structures and molecular targets of all FDA-approved chemical entities. The CeMM Library of Unique Drugs (CLOUD) covers prodrugs and active forms at pharmacologically relevant concentrations and is ideally suited for combinatorial studies. We screened pairwise combinations of CLOUD drugs for impairment of cancer cell viability and discovered a synergistic interaction between flutamide and phenprocoumon (PPC)...
May 22, 2017: Nature Chemical Biology
https://www.readbyqxmd.com/read/28530234/n-alkylated-analogs-of-4-methylamphetamine-4-ma-differentially-affect-monoamine-transporters-and-abuse-liability
#12
Ernesto Solis, John S Partilla, Farhana Sakloth, Iwona Ruchala, Kathryn L Schwienteck, Louis J De Felice, Jose M Eltit, Richard A Glennon, S Stevens Negus, Michael H Baumann
Clandestine chemists synthesize novel stimulant drugs by exploiting structural templates known to target monoamine transporters for dopamine, norepinephrine and serotonin (DAT, NET, and SERT, respectively). 4-Methylamphetamine (4-MA) is an emerging drug of abuse that interacts with transporters, but limited structure-activity data are available for its analogs. Here we employed uptake and release assays in rat brain synaptosomes, voltage-clamp current measurements in cells expressing transporters, and calcium flux assays in cells co-expressing transporters and calcium channels to study the effects of increasing N-alkyl chain length of 4-MA on interactions at DAT, NET and SERT...
May 22, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28529668/diastereoselective-radical-type-cyclopropanation-of-electron-deficient-alkenes-mediated-by-the-highly-active-cobalt-ii-tetramethyltetraaza-14-annulene-catalyst
#13
Andrei Chirila, Braja Gopal Das, Nanda D Paul, Bas de Bruin
A new protocol for the catalytic synthesis of cyclopropanes using electron-deficient alkenes is presented, which is catalysed by a series of affordable, easy to synthesise and highly active substituted cobalt(II) tetraaza[14]annulenes. These catalysts are compatible with the use of sodium tosylhydrazone salts as precursors to diazo compounds in one-pot catalytic transformations to afford the desired cyclopropanes in almost quantitative yields. The reaction takes advantage of the metalloradical character of the Co complexes to activate the diazo compounds...
April 21, 2017: ChemCatChem
https://www.readbyqxmd.com/read/28529666/a-microfluidic-model-of-hemostasis-sensitive-to-platelet-function-and-coagulation
#14
R M Schoeman, K Rana, N Danes, M Lehmann, J A Di Paola, A L Fogelson, K Leiderman, K B Neeves
Hemostasis is the process of sealing a vascular injury with a thrombus to arrest bleeding. The type of thrombus that forms depends on the nature of the injury and hemodynamics. There are many models of intravascular thrombus formation whereby blood is exposed to prothrombotic molecules on a solid substrate. However, there are few models of extravascular thrombus formation whereby blood escapes into the extravascular space through a hole in the vessel wall. Here, we describe a microfluidic model of hemostasis that includes vascular, vessel wall, and extravascular compartments...
February 2017: Cellular and Molecular Bioengineering
https://www.readbyqxmd.com/read/28529040/pre-treatment-technologies-for-dark-fermentative-hydrogen-production-current-advances-and-future-directions
#15
Razieh Rafieenia, Maria Cristina Lavagnolo, Alberto Pivato
Hydrogen is regarded as a clean and non-carbon fuel and it has a higher energy content compared to carbon fuels. Dark fermentative hydrogen production from organic wastes is the most promising technology for commercialization among chemical and biological methods. Using mixed microflora is favored in terms of easier process control and substrate conversion efficiencies instead of pure cultures. However, mixed cultures should be first pre-treated in order to select sporulating hydrogen producing bacteria and suppress non-spore forming hydrogen consumers...
May 18, 2017: Waste Management
https://www.readbyqxmd.com/read/28528948/multi-functional-activities-of-citrus-flavonoid-narirutin-in-alzheimer-s-disease-therapeutics-an-integrated-screening-approach-and-in-vitro-validation
#16
Sandipan Chakraborty, Soumalee Basu
Alzheimer's disease (AD) is a complex disorder and the disease mechanism is yet to be properly characterized. Over the years, "amyloid cascade" emerges as principal pathogenic event in AD. β-Secretase 1 (BACE1) controls the rate-limiting step in amyloid beta (Aβ) generation and Aβ rapidly aggregates to form neurotoxic amyloid fibrils. Oxidative stress is one of the principal mediators of the observed neurotoxicity of amyloid fibril. The disease pathogenesis involves induction of multiple signaling cascades and the cross-talk therein...
May 18, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28528313/changes-in-nutrient-removal-and-flocs-characteristics-generated-by-presence-of-zno-nanoparticles-in-activated-sludge-process
#17
Pabel Cervantes-Avilés, Germán Cuevas-Rodríguez
The aim of this work was to evaluate the impact generated by ZnO NPs on the activated sludge process treating raw (RWW) and filtered wastewater (FWW). It was analyzed the oxygen uptake rate, nutrient removal, flocs characteristics and the morphological interactions between activated sludge and ZnO NPs, in presence of 450-2000 mg/L. The results showed that the presence of more than 450 mg/L of ZnO NPs in raw and filtered wastewater inhibited the oxygen uptake by activated sludge. The highest inhibition was 35% in presence of 1500 mg/L in RWW...
May 16, 2017: Chemosphere
https://www.readbyqxmd.com/read/28528287/population-pharmacokinetics-of-oxcarbazepine-and-its-metabolite-10-hydroxycarbazepine-in-healthy-subjects
#18
Natalicia de Jesus Antunes, Sven C van Dijkman, Vera Lucia Lanchote, Lauro Wichert-Ana, Eduardo Barbosa Coelho, Veriano Alexandre Junior, Osvaldo Massaiti Takayanagui, Eduardo Tozatto, Johan G C van Hasselt, Oscar Della Pasqua
Oxcarbazepine is indicated for the treatment of partial or generalized tonic-clonic seizures. The majority of the oxcarbazepine is converted into its active metabolite, 10-hydroxycarbazepine (MHD), which can exist as R-(-)- and S-(+)-MHD enantiomers. Here we describe the influence of the P-glycoprotein (P-gp) inhibitor verapamil, on the disposition of oxcarbazepine and MHD enantiomers, both of which are P-gp substrates. Healthy subjects (n=12) were randomized to oxcarbazepine or oxcarbazepine combined with verapamil at doses of 300mg b...
May 17, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28527994/purification-and-characterization-of-a-protease-resistant-phytase-of-aspergillus-oryzae-sbs50-whose-properties-make-it-exceptionally-useful-as-a-feed-supplement
#19
Sapna, Bijender Singh
An extracellular phytase of Aspergillus oryzae SBS50 was purified to homogeneity using ammonium sulphate precipitation, ion-exchange and gel filtration chromatography. Purified phytase has a monomeric molecular mass of ∼80kDa exhibiting its optimal activity at pH 5.0 and 50°C with a T 1/2 of 300min at 50°C. Phytase of A. oryzae displayed broad substrate specificity with Vmax and Km values of 58.82μmol/ml/min and 1.14mM, respectively, for calcium phytate. Purity and homogeneity of the phytase was confirmed by high performance liquid chromatography and MALDI-TOF analysis revealed the identification of a peptide showing homology with acid phosphatase of Aspergillus oryzae RIB40...
May 17, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28527717/inhibition-of-the-lateral-habenular-camk%C3%A2-abolishes-naloxone-precipitated-conditioned-place-aversion-in-morphine-dependent-mice
#20
Jing Wang, Min Li, Ping Wang, Yunhong Zha, Zhi He, Zicheng Li
Addictive substances mediate positive and negative states promoting compulsive drug use. However, substrates for aversive effects of drugs are not fully understood. We found that inactivation of the lateral habenula (LHb) by microinjection of tetrodotoxin (TTX) abolished naloxone-precipitated conditioned place aversion (CPA) in morphine-dependent mice. We also found that lateral habenular administration of KN-62, a specific inhibitor for calcium/calmodulin dependent protein kinase II (CaMKII), abolished naloxone-precipitated CPA in morphine-dependent mice...
May 17, 2017: Neuroscience Letters
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