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https://www.readbyqxmd.com/read/28813027/sulfonamide-linked-ciprofloxacin-sulfadiazine-and-amantadine-derivatives-as-a-novel-class-of-inhibitors-of-jack-bean-urease-synthesis-kinetic-mechanism-and-molecular-docking
#1
Pervaiz Ali Channar, Aamer Saeed, Fernando Albericio, Fayaz Ali Larik, Qamar Abbas, Mubashir Hassan, Hussain Raza, Sung-Yum Seo
Sulfonamide derivatives serve as an important building blocks in the drug design discovery and development (4D) process. Ciprofloxacin-, sulfadiazine- and amantadine-based sulfonamides were synthesized as potent inhibitors of jack bean urease and free radical scavengers. Molecular diversity was explored and electronic factors were also examined. All 24 synthesized compounds exhibited excellent potential against urease enzyme. Compound 3e (IC50 = 0.081 ± 0.003 µM), 6a (IC50 = 0.0022 ± 0.0002 µM), 9e (IC50 = 0...
August 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28811709/bone-marrow-derived-monocyte-infusion-improves-hepatic-fibrosis-by-decreasing-osteopontin-tgf-%C3%AE-1-il-13-and-oxidative-stress
#2
Veruska Cintia Alexandrino de Souza, Thiago Almeida Pereira, Valéria Wanderley Teixeira, Helotonio Carvalho, Maria Carolina Accioly Brelaz de Castro, Carolline Guimarães D'assunção, Andréia Ferreira de Barros, Camila Lima Carvalho, Virgínia Maria Barros de Lorena, Vláudia Maria Assis Costa, Álvaro Aguiar Coelho Teixeira, Regina Celia Bressan Queiroz Figueiredo, Sheilla Andrade de Oliveira
AIM: To evaluate the therapeutic effects of bone marrow-derived CD11b(+)CD14(+) monocytes in a murine model of chronic liver damage. METHODS: Chronic liver damage was induced in C57BL/6 mice by administration of carbon tetrachloride and ethanol for 6 mo. Bone marrow-derived monocytes isolated by immunomagnetic separation were used for therapy. The cell transplantation effects were evaluated by morphometry, biochemical assessment, immunohistochemistry and enzyme-linked immunosorbent assay...
July 28, 2017: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/28811547/up-regulation-of-nadph-oxidase-mediated-redox-signaling-contributes-to-the-loss-of-barrier-function-in-krit1-deficient-endothelium
#3
Luca Goitre, Peter V DiStefano, Andrea Moglia, Nicholas Nobiletti, Eva Baldini, Lorenza Trabalzini, Julie Keubel, Eliana Trapani, Vladimir V Shuvaev, Vladimir R Muzykantov, Ingrid H Sarelius, Saverio Francesco Retta, Angela J Glading
The intracellular scaffold KRIT1/CCM1 is an established regulator of vascular barrier function. Loss of KRIT1 leads to decreased microvessel barrier function and to the development of the vascular disorder Cerebral Cavernous Malformation (CCM). However, how loss of KRIT1 causes the subsequent deficit in barrier function remains undefined. Previous studies have shown that loss of KRIT1 increases the production of reactive oxygen species (ROS) and exacerbates vascular permeability triggered by several inflammatory stimuli, but not TNF-α...
August 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28811345/inhibitors-of-the-histone-methyltransferases-ezh2-1-induce-a-potent-antiviral-state-and-suppress-infection-by-diverse-viral-pathogens
#4
Jesse H Arbuckle, Paul J Gardina, David N Gordon, Heather D Hickman, Jonathan W Yewdell, Theodore C Pierson, Timothy G Myers, Thomas M Kristie
Epigenetic regulation is based on a network of complexes that modulate the chromatin character and structure of the genome to impact gene expression, cell fate, and development. Thus, epigenetic modulators represent novel therapeutic targets used to treat a range of diseases, including malignancies. Infectious pathogens such as herpesviruses are also regulated by cellular epigenetic machinery, and epigenetic therapeutics represent a novel approach used to control infection, persistence, and the resulting recurrent disease...
August 15, 2017: MBio
https://www.readbyqxmd.com/read/28811220/euphorbia-lunulata-extract-acts-on-multidrug-resistant-gastric-cancer-cells-to-inhibit-cell-proliferation-migration-and-invasion-arrest-cell-cycle-progression-and-induce-apoptosis
#5
Zhaoying Fu, Xiaodong Han, Juan Du, Xiaoxiao Han, Weipeng Liu, Shumei Shao, Xiaobin Liu
ETHNOPHARMACOLOGICAL RELEVANCE: The milky sap or the aboveground part of the plant Euphorbia lunulata has long been used by Chinese people to treat noncancerous growths and cancerous ailments but the specific mode of action and the action mechanism remain to be elucidated. AIM OF THE STUDY: To investigate the effects of Euphorbia lunulata extract on cell proliferation, migration, invasion, cell cycle progression, and apoptosis of multidrug resistant human gastric cancer cells; To study the mechanism of apoptosis induction by Euphorbia lunulata extract in multidrug resistant human gastric cancer cells...
August 12, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28811143/nadph-oxidases-as-drug-targets-and-biomarkers-in-neurodegenerative-diseases-what-is-the-evidence
#6
REVIEW
Silvia Sorce, Roland Stocker, Tamara Seredenina, Rikard Holmdahl, Adriano Aguzzi, Adriano Chio, Antoine Depaulis, Freddy Heitz, Peter Olofsson, Tomas Olsson, Venceslas Duveau, Despina Sanoudou, Sara Skosgater, Antonia Vlahou, Dominique Wasquel, Karl-Heinz Krause, Vincent Jaquet
Neurodegenerative disease are frequently characterized by microglia activation and/or leukocyte infiltration in the parenchyma of the central nervous system and at the molecular level by increased oxidative modifications of proteins, lipids and nucleic acids. NADPH oxidases (NOX) emerged as a novel promising class of pharmacological targets for the treatment of neurodegeneration due to their role in oxidant generation and presumably in regulating microglia activation. The unique function of NOX is the generation of superoxide anion (O2(•-)) and hydrogen peroxide (H2O2)...
August 12, 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28811133/arylamidonaphtalene-sulfonate-compounds-as-a-novel-class-of-heparanase-inhibitors
#7
Riccardo Rondanin, Sara Fochi, Riccardo Baruchello, Tatiana Bernardi, Paola Oliva, Floriana Semeraro, Daniele Simoni, Giuseppe Giannini
The search for antimetastatic agents for cancer therapy may involve the ability of new compounds to maintain the tissue extracellular matrix integrity. Among known factors, heparanase, an endoglucuronidase responsible for heparan sulfate cleavage, is a promising target whose inhibition could represent a strong obstacle for metastatic cancerous mechanisms. The antimetastatic activity of some suramin derivatives reported in literature suggests a possible involvement of the heparanase enzyme. To confirm such hypothesis, we have investigated FCE27266, a molecule known for its antiangiogenic and antimetastatic properties...
August 8, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28810191/structure-function-studies-of-bpp-brachynh2-and-synthetic-analogues-thereof-with-angiotensin-i-converting-enzyme
#8
Daniel D R Arcanjo, Andreanne G Vasconcelos, Lucas A Nascimento, Ana Carolina Mafud, Alexandra Plácido, Michel M M Alves, Cristina Delerue-Matos, Marcelo P Bemquerer, Nuno Vale, Paula Gomes, Eduardo B Oliveira, Francisco C A Lima, Yvonne P Mascarenhas, Fernando Aécio A Carvalho, Ulf Simonsen, Ricardo M Ramos, José Roberto S A Leite
The vasoactive proline-rich oligopeptide termed BPP-BrachyNH2 (H-WPPPKVSP-NH2) induces in vitro inhibitory activity of angiotensin I-converting enzyme (ACE) in rat blood serum. In the present study, the removal of N-terminal tryptophan or C-terminal proline from BPP-BrachyNH2 was investigated in order to predict which structural components are important or required for interaction with ACE. Furthermore, the toxicological profile was assessed by in silico prediction and in vitro MTT assay. Two BPP-BrachyNH2 analogues (des-Trp(1)-BPP-BrachyNH2 and des-Pro(8)-BPP-BrachyNH2) were synthesized, and in vitro and in silico ACE inhibitory activity and toxicological profile were assessed...
August 7, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28809952/computational-and-experimental-analysis-of-short-peptide-motifs-for-enzyme-inhibition
#9
Jinglin Fu, Luca Larini, Anthony J Cooper, John W Whittaker, Azka Ahmed, Junhao Dong, Minyoung Lee, Ting Zhang
The metabolism of living systems involves many enzymes that play key roles as catalysts and are essential to biological function. Searching ligands with the ability to modulate enzyme activities is central to diagnosis and therapeutics. Peptides represent a promising class of potential enzyme modulators due to the large chemical diversity, and well-established methods for library synthesis. Peptides and their derivatives are found to play critical roles in modulating enzymes and mediating cellular uptakes, which are increasingly valuable in therapeutics...
2017: PloS One
https://www.readbyqxmd.com/read/28809420/rapid-identification-of-%C3%AE-glucosidase-inhibitors-from-dioscorea-opposita-thunb-peel-extract-by-enzyme-functionalized-fe3o4-magnetic-nanoparticles-coupled-with-hplc-ms-ms
#10
Songsong Zhang, Dandan Wu, Huan Li, Jinhua Zhu, Weiping Hu, Minghua Lu, Xiuhua Liu
Dioscorea opposita Thunb, commonly known as "yam" that has a long dietary therapy history for diabetes, is widely consumed as a botanical dietary supplement and widely cultivated in China. In this work, a method for rapid screening of α-glucosidase inhibitors from Dioscorea opposita Thunb peel extract was developed using α-glucosidase functionalized magnetic nanoparticles (αG-MNPs) as a solid phase extraction absorbent in combination with high performance liquid chromatography-mass spectrometry (HPLC-MS)...
August 15, 2017: Food & Function
https://www.readbyqxmd.com/read/28809106/structural-characteristics-and-function-of-a-new-kind-of-thermostable-trehalose-synthase-from-thermobaculum-terrenum
#11
Junqing Wang, Xudong Ren, Ruiming Wang, Jing Su, Feng Wang
Trehalose has important applications in the food industry and pharmaceutical manufacturing. The thermostable enzyme trehalose synthase from Thermobaculum terrenum (TtTS) catalyzes the reversible interconversion of maltose and trehalose. Here, we investigated the structural characteristics of TtTS in complex with the inhibitor TriS. TtTS exhibits the typical three domain glycoside hydrolase family 13 structure. The catalytic cleft consists of Asp202-Glu244-Asp310 and various conserved substrate-binding residues...
August 15, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28809002/probing-protein-kinase-atp-interactions-using-a-fluorescent-atp-analog
#12
Leslie E W LaConte, Sarika Srivastava, Konark Mukherjee
Eukaryotic protein kinases are an intensely investigated class of enzymes which have garnered attention due to their usefulness as drug targets. Determining the regulation of ATP binding to a protein kinase is not only critical for understanding function in a cellular context but also for designing kinase-specific molecular inhibitors. Here, we provide a general procedure for characterizing ATP binding to eukaryotic protein kinases. The protocol can be adapted to identify the conditions under which a particular kinase is activated...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28808995/high-resolution-parallel-reaction-monitoring-with-electron-transfer-dissociation-for-middle-down-proteomics-an-application-to-study-the-quantitative-changes-induced-by-histone-modifying-enzyme-inhibitors-and-activators
#13
Michael J Sweredoski, Annie Moradian, Sonja Hess
With the advent of new methodologies, proteomics-based assays are increasingly used to study the efficacy of drugs on a molecular level. For these studies to be meaningful, the proteomics assays need to be sensitive, selective, accurate, and reproducible. This is often accomplished through a targeted approach, either using single or multiple reaction monitoring (SRM/MRM) or, more recently, parallel reaction monitoring (PRM). In PRM, the parallel detection of all product ions in a high-resolution mass spectrometer affords higher selectivity than SRM/MRM...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28808769/the-genetic-characteristics-in-cytology-and-plant-physiology-of-two-wheat-triticum-aestivum-near-isogenic-lines-with-different-freezing-tolerances
#14
Wenqiang Wang, Qunqun Hao, Wenlong Wang, Qinxue Li, Wei Wang
Freezing tolerance in taft plants relied more upon an ABA-independent- than an ABA-dependent antifreeze signaling pathway. Two wheat (Triticum aestivum) near isogenic lines (NIL) named tafs (freezing sensitivity) and taft (freezing tolerance) were isolated in the laboratory and their various cytological and physiological characteristics under freezing conditions were studied. Proplastid, cell membrane, and mitochondrial ultrastructure were less damaged by freezing treatment in taft than tafs plants. Chlorophyll, ATP, and thylakoid membrane protein contents were significantly higher, but malondialdehyde content was significantly lower in taft than tafs plants under freezing condition...
August 14, 2017: Plant Cell Reports
https://www.readbyqxmd.com/read/28808443/angiotensin-converting-enzyme-inhibition-and-parathyroid-hormone-secretion
#15
Sarah Zaheer, Jenifer M Brown, Molly Connors, Jonathan S Williams, Gail K Adler, Anand Vaidya
BACKGROUND: Prior studies suggest that renin-angiotensin-aldosterone system (RAAS) inhibitors decrease parathyroid hormone (PTH) secretion. OBJECTIVE: To evaluate the effect of angiotensin-converting enzyme inhibitors (ACEi) on serum PTH in participants with and without primary hyperparathyroidism (P-HPT). METHODS: An open-label, single-arm, pilot study whereby participants with and without P-HPT had PTH were evaluated before and after 1 week of maximally tolerated lisinopril therapy...
2017: International Journal of Endocrinology
https://www.readbyqxmd.com/read/28808272/a-combinatorial-approach-for-the-discovery-of-cytochrome-p450-2d6-inhibitors-from-nature
#16
Johannes Hochleitner, Muhammad Akram, Martina Ueberall, Rohan A Davis, Birgit Waltenberger, Hermann Stuppner, Sonja Sturm, Florian Ueberall, Johanna M Gostner, Daniela Schuster
The human cytochrome P450 2D6 (CYP2D6) enzyme is part of phase-I metabolism and metabolizes at least 20% of all clinically relevant drugs. Therefore, it is an important target for drug-drug interaction (DDI) studies. High-throughput screening (HTS) assays are commonly used tools to examine DDI, but show certain drawbacks with regard to their applicability to natural products. We propose an in silico - in vitro workflow for the reliable identification of natural products with CYP2D6 inhibitory potential. In order to identify candidates from natural product-based databases that share similar structural features with established inhibitors, a pharmacophore model was applied...
August 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28808226/atr-inhibition-facilitates-targeting-of-leukemia-dependence-on-convergent-nucleotide-biosynthetic-pathways
#17
Thuc M Le, Soumya Poddar, Joseph R Capri, Evan R Abt, Woosuk Kim, Liu Wei, Nhu T Uong, Chloe M Cheng, Daniel Braas, Mina Nikanjam, Peter Rix, Daria Merkurjev, Jesse Zaretsky, Harley I Kornblum, Antoni Ribas, Harvey R Herschman, Julian Whitelegge, Kym F Faull, Timothy R Donahue, Johannes Czernin, Caius G Radu
Leukemia cells rely on two nucleotide biosynthetic pathways, de novo and salvage, to produce dNTPs for DNA replication. Here, using metabolomic, proteomic, and phosphoproteomic approaches, we show that inhibition of the replication stress sensing kinase ataxia telangiectasia and Rad3-related protein (ATR) reduces the output of both de novo and salvage pathways by regulating the activity of their respective rate-limiting enzymes, ribonucleotide reductase (RNR) and deoxycytidine kinase (dCK), via distinct molecular mechanisms...
August 14, 2017: Nature Communications
https://www.readbyqxmd.com/read/28807926/use-of-antihypertensive-medications-and-risk-of-adverse-breast-cancer-outcomes-in-a-seer-medicare-population
#18
Lu Chen, Jessica Chubak, Denise M Boudreau, William E Barlow, Noel S Weiss, Christopher I Li
BACKGROUND: It is unclear if use of common antihypertensive medications influences the risk of adverse breast cancer outcomes. METHODS: Using the linked Surveillance, Epidemiology and End-Results (SEER)-Medicare database, we identified 14,766 women between ages 66 and 80 years diagnosed with incident stage I/II breast cancer between 2007-2011. Medicare Part D data were obtained to characterize women's post-cancer use of various antihypertensive medications. Outcomes included a second breast cancer event (SBCE, a composite outcome defined as the first of a recurrence or a second contralateral primary breast cancer), breast cancer recurrence, and breast-cancer specific mortality...
August 14, 2017: Cancer Epidemiology, Biomarkers & Prevention
https://www.readbyqxmd.com/read/28807908/activity-of-the-%C3%AE-lactamase-inhibitor-ln-1-255-against-carbapenem-hydrolyzing-class-d-%C3%AE-lactamases-from-acinetobacter-baumannii
#19
Juan Carlos Vázquez-Ucha, María Maneiro, Marta Martínez-Guitián, John Buynak, Christopher R Bethel, Robert A Bonomo, Germán Bou, Margarita Poza, Concepción González-Bello, Alejandro Beceiro
The number of infections caused by Gram-negative pathogens carrying carbapenemases is increasing, and the group of carbapenem-hydrolyzing class D β-lactamases (CHDLs) is especially problematic. Several clinically important CHDLs have been identified in A. baumannii, including OXA-23, OXA-24/40, OXA-58, OXA-143, OXA-235, and the chromosomally encoded OXA-51. The selection and dissemination of carbapenem-resistant A. baumannii strains constitutes a serious global threat. Carbapenems have been successfully utilized as last resort antibiotics for the treatment of multi-drug-resistant A...
August 14, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28807596/the-role-of-angiotensin-ii-in-parietal-epithelial-cell-proliferation-and-crescent-formation-in-glomerular-diseases
#20
Paola Rizzo, Rubina Novelli, Cinzia Rota, Elena Gagliardini, Barbara Ruggiero, Daniela Rottoli, Ariela Benigni, Giuseppe Remuzzi
Crescentic glomerulonephritis (GN) is a devastating disease with rapidly progressive deterioration in kidney function, which, histologically, manifests as crescent formation in most glomeruli. We previously found that crescents derive from the aberrant proliferation and migration of parietal epithelial cells (PECs)/progenitor cells, and that the angiotensin (ang) II/ang II type-1 (AT1) receptor pathway may participate, together with the stromal cell-derived factor-1 (SDF-1)/CXCR4 axis, in the development of those lesions...
August 11, 2017: American Journal of Pathology
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