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Carbonic anhydrase 3

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https://www.readbyqxmd.com/read/28324887/association-between-hypoxic-volume-and-underlying-hypoxia-induced-gene-expression-in-oropharyngeal-squamous-cell-carcinoma
#1
Yae-Eun Suh, Katherine Lawler, Rhonda Henley-Smith, Lucy Pike, Russell Leek, Sally Barrington, Edward W Odell, Tony Ng, Francesco Pezzella, Teresa Guerrero-Urbano, Mahvash Tavassoli
BACKGROUND: Hypoxia imaging is a promising tool for targeted therapy but the links between imaging features and underlying molecular characteristics of the tumour have not been investigated. The aim of this study was to compare hypoxia biomarkers and gene expression in oropharyngeal squamous cell carcinoma (OPSCC) diagnostic biopsies with hypoxia imaged with (64)Cu-ATSM PET/CT. METHODS: (64)Cu-ATSM imaging, molecular and clinical data were obtained for 15 patients...
March 21, 2017: British Journal of Cancer
https://www.readbyqxmd.com/read/28318894/synthesis-and-human-bacterial-carbonic-anhydrase-inhibition-with-a-series-of-sulfonamides-incorporating-phthalimido-moieties
#2
Menshawy A Mohamed, Alaa A-M Abdel-Aziz, Helmy M Sakr, Adel S El-Azab, Silvia Bua, Claudiu T Supuran
A series of sulfonamides was obtained by reacting substituted-2-(1,3-dioxo-1,3-dihydroisobenzofuran-5-carboxamido)benzoic acids with aromatic sulfonamides incorporating primary amino moieties. The new compounds were investigated as inhibitor of four carbonic anhydrase (CA, EC 4.2.1.1) isoforms, the human (h) hCA I and II, and the α- and β-class CAs from the pathogenic bacterium Vibrio cholerae, VchCAα and VhcCAβ. hCA I was effectively inhibited by the new sulfonamides, with inhibition constants in the range of 4...
March 9, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28303650/enzymatic-electrosynthesis-of-formic-acid-through-co2-reduction-in-bioelectrochemical-system-bes-effect-of-immobilization-and-carbonic-anhydrase-addition
#3
Sandipam Srikanth, Yolanda Alvarez Gallego, Karolien Vanbroekhoven, Deepak Pant
Enzymatic electrosynthesis of formic acid from carbon dioxide (CO2) reduction using formate dehydrogenase (FDH) as catalyst at cathode both in its free and immobilized forms was studied in detail in bioelectrochemical system (BES). The essential role of solubilizing CO2 for its conversion was also studied by adding carbonic anhydrase (CA) to the FDH enzyme both in free and immobilized forms. FDH alone in the free form showed large variation in reduction current (-6.2±3.9 A/m2), while the immobilized form showed less variation (-3...
March 17, 2017: Chemphyschem: a European Journal of Chemical Physics and Physical Chemistry
https://www.readbyqxmd.com/read/28302311/the-first-synthesis-of-4-phenylbutenone-derivative-bromophenols-including-natural-products-and-their-inhibition-profiles-for-carbonic-anhydrase-acetylcholinesterase-and-butyrylcholinesterase-enzymes
#4
Çetin Bayrak, Parham Taslimi, İlhami Gülçin, Abdullah Menzek
The first synthesis of (E)-4-(3-bromo-4,5-dihydroxyphenyl)but-3-en-2-one (1), (E)-4-(2-bromo-4,5-dihydroxyphenyl)but-3-en-2-one (2), and (E)-4-(2,3-dibromo-4,5-dihydroxyphenyl)but-3-en-2-one (3) was realized as natural bromophenols. Derivatives with mono OMe of 2 and 3 were obtained from the reactions of their derivatives with di OMe with AlCl3. These novel 4-phenylbutenone derivatives were effective inhibitors of the cytosolic carbonic anhydrase I and II isoenzymes (hCA I and II), acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with Ki values in the range of 158...
March 2, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28293806/morpho-physiological-and-transcriptome-profiling-reveal-novel-zinc-deficiency-responsive-genes-in-rice
#5
Tirthankar Bandyopadhyay, Poonam Mehra, Suboot Hairat, Jitender Giri
Intensive farming has depleted the soil zinc (Zn) availability resulting in decreased crop productivity. Here, we attempt to understand the Zn deficiency response in rice through temporal transcriptome analysis. For this, rice seedlings were raised under Zn-deficient conditions up to 4 weeks followed by Zn re-supply for 3 days. Zn-deficient plants developed characteristic deficiency symptoms such as leaf bronzing, decrease in biomass, total chlorophyll, PSII efficiency, decreased carbonic anhydrase activity and increased ROS production...
March 14, 2017: Functional & Integrative Genomics
https://www.readbyqxmd.com/read/28293195/comparative-investigation-of-copper-tolerance-and-identification-of-putative-tolerance-related-genes-in-tardigrades
#6
Thomas L Hygum, Dannie Fobian, Maria Kamilari, Aslak Jørgensen, Morten Schiøtt, Martin Grosell, Nadja Møbjerg
Tardigrades are microscopic aquatic animals renowned for their tolerance toward extreme environmental conditions. The current study is the first to investigate their tolerance toward heavy metals and we present a novel tardigrade toxicant tolerance assay based on activity assessments as a measure of survival. Specifically, we compare tolerance toward copper in four species representing different evolutionary lineages, habitats and adaptation strategies, i.e., a marine heterotardigrade, Echiniscoides sigismundi, a limno-terrestrial heterotardigrade, Echiniscus testudo, a limno-terrestrial eutardigrade, Ramazzottius oberhaeuseri, and a marine eutardigrade, Halobiotus crispae...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28277280/bortezomib-inhibits-mammalian-carbonic-anhydrases
#7
Claudiu T Supuran
We investigated the carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity of the clinically used antitumor agent bortezomib, a marketed proteasome inhibitor, against all the catalytically active mammalian isoforms CA I-VII, IX, XII-XV. Bortezomib effectively inhibited all these CAs in the micromolar range. hCA II, the physiologically dominant cytosolic isoform showed the highest affinity for the drug, with a KI of 1.16μM. The cytosolic slow isoform hCA I was also effectively inhibited, with a KI of 1.29μM, whereas the next best affinity was observed for the membrane-anchored form mCA XV, with a KI of 2...
October 19, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28275953/design-and-comparative-evaluation-of-the-anticonvulsant-profile-carbonic-anhydrate-inhibition-and-teratogenicity-of-novel-carbamate-derivatives-of-branched-aliphatic-carboxylic-acids-with-4-aminobenzensulfonamide
#8
David Bibi, Hafiz Mawasi, Alessio Nocentini, Claudiu T Supuran, Bogdan Wlodarczyk, Richard H Finnell, Meir Bialer
Epilepsy is one of the most common neurological diseases, with between 34 and 76 per 100,000 people developing epilepsy annually. Epilepsy therapy for the past 100(+) years is based on the use of antiepileptic drugs (AEDs). Despite the availability of more than twenty old and new AEDs, approximately 30% of patients with epilepsy are not seizure-free with the existing medications. In addition, the clinical use of the existing AEDs is restricted by their side-effects, including the teratogenicity associated with valproic acid that restricts its use in women of child-bearing age...
March 9, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28272885/lead-development-of-thiazolylsulfonamides-with-carbonic-anhydrase-inhibitory-action
#9
Fabrizio Carta, Alexander Birkmann, Tamara Pfaff, Helmut Buschmann, Wilfried Schwab, Holger Zimmermann, Alfonso Maresca, Claudiu T Supuran
A series of congeners structurally related to pritelivir, N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide, a helicase-primase inhibitor for the treatment of herpes simplex virus infections, was prepared. The synthesized primary and secondary sulfonamides were investigated as inhibitors of six physiologically and pharmacologically relevant human (h) carbonic anhydrase (hCA, EC 4.2.1.1) isoforms, the cytosolic enzymes hCA I and II, the mitochondrial ones hCA VA and VB, and the transmembrane, tumor associated hCA IX and XII...
March 17, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28272780/microfluidic-encapsulation-of-prickly-zinc-doped-copper-oxide-nanoparticles-with-vd1142-modified-spermine-acetalated-dextran-for-efficient-cancer-therapy
#10
Hongbo Zhang, Dongfei Liu, Liang Wang, Zehua Liu, Runrun Wu, Agne Janoniene, Ming Ma, Guoqing Pan, Lina Baranauskiene, Linlin Zhang, Wenguo Cui, Vilma Petrikaite, Daumantas Matulis, Hongxia Zhao, Jianming Pan, Hélder A Santos
Structural features of nanoparticles have recently been explored for different types of applications. To explore specific particles as nanomedicine and physically destroy cancer is interesting, which might avoid many obstacles in cancer treatment, for example, drug resistance. However, one key element and technical challenge of those systems is to selectively target them to cancer cells. As a proof-of-concept, Prickly zinc-doped copper oxide (Zn-CuO) nanoparticles (Prickly NPs) have been synthesized, and subsequently encapsulated in a pH-responsive polymer; and the surface has been modified with a novel synthesized ligand, 3-(cyclooctylamino)-2,5,6-trifluoro-4-[(2-hydroxyethyl)sulfonyl] benzenesulfonamide (VD1142)...
March 8, 2017: Advanced Healthcare Materials
https://www.readbyqxmd.com/read/28272358/comparison-of-the-sulfonamide-inhibition-profiles-of-the-%C3%AE-and-%C3%AE-carbonic-anhydrases-from-the-pathogenic-bacterium-burkholderia-pseudomallei
#11
Daniela Vullo, Sonia Del Prete, Pietro Di Fonzo, Vincenzo Carginale, W Alexander Donald, Claudiu T Supuran, Clemente Capasso
We have cloned, purified, and characterized a β-carbonic anhydrase (CA, EC 4.2.1.1), BpsCAβ, from the pathogenic bacterium Burkholderia pseudomallei, responsible for the tropical disease melioidosis. The enzyme showed high catalytic activity for the physiologic CO₂ hydration reaction to bicarbonate and protons, with the following kinetic parameters: kcat of 1.6 × 10⁵ s(-1) and kcat/KM of 3.4 × 10⁷ M(-1) s(-1). An inhibition study with a panel of 38 sulfonamides and one sulfamate-including 15 compounds that are used clinically-revealed an interesting structure-activity relationship for the interaction of this enzyme with these inhibitors...
March 7, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28263753/the-maternal-plasma-proteome-changes-as-a-function-of-gestational-age-in-normal-pregnancy-a-longitudinal-study
#12
Roberto Romero, Offer Erez, Eli Maymon, Piya Chaemsaithong, Zhonghui Xu, Percy Pacora, Tinnakorn Chaiworapongsa, Bogdan Done, Sonia S Hassan, Adi L Tarca
OBJECTIVE: Pregnancy is accompanied by dramatic physiologic changes in maternal plasma proteins. Characterization of the maternal plasma proteome in normal pregnancy is an essential step for understanding changes to predict pregnancy outcome. The objective of this study was to describe maternal plasma proteins that change in abundance with advancing gestational age, and determine biological processes that are perturbed in normal pregnancy. MATERIALS AND METHODS: A longitudinal study included 43 normal pregnancies that had a term delivery of an infant who was appropriate for gestational age (AGA) without maternal or neonatal complications...
March 2, 2017: American Journal of Obstetrics and Gynecology
https://www.readbyqxmd.com/read/28260401/microwave-assisted-synthesis-and-bioevaluation-of-new-sulfonamides
#13
Halise Inci Gul, Cem Yamali, Fatma Yesilyurt, Hiroshi Sakagami, Kaan Kucukoglu, Ilhami Gulcin, Mustafa Gul, Claudiu T Supuran
In this study, 4-[5-(4-hydroxyphenyl)-3-aryl-4,5-dihydro-1H-pyrazol-1-yl]benzenesulfonamide derivatives (8-14) were synthesized for the first time by microwave irradiation and their chemical structures were confirmed by (1)H NMR, (13)C NMR and HRMS. Cytotoxic activities and inhibitory effects on carbonic anhydrase I and II isoenzymes of the compounds were investigated. The compounds 9 (PSE = 4.2), 12 (PSE = 4.1) and 13 (PSE = 3.9) with the highest potency selectivity expression (PSE) values in cytotoxicity experiments and the compounds 13 (Ki = 3...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28257333/recent-advances-for-measurement-of-protein-synthesis-rates-use-of-the-virtual-biopsy-approach-and-measurement-of-muscle-mass
#14
Marc Hellerstein, William Evans
PURPOSE OF REVIEW: Flux-rate measurements of protein synthesis and breakdown (turnover) in muscle represent an ideal class of mechanism-based biomarkers for conditions of altered muscle mass and function. We describe here new metabolic labeling techniques for flux-rate measurements in humans, focusing on skeletal muscle. RECENT FINDINGS: Dynamics of the muscle proteome are accurately measured in humans by combining long-term heavy water labeling with tandem mass spectrometry...
March 2, 2017: Current Opinion in Clinical Nutrition and Metabolic Care
https://www.readbyqxmd.com/read/28256371/synthesis-of-bulky-tailed-sulfonamides-incorporating-pyrido-2-3-d-1-2-4-triazolo-4-3-a-pyrimidin-1-5h-yl-moieties-and-evaluation-of-their-carbonic-anhydrases-i-ii-iv-and-ix-inhibitory-effects
#15
Mohamed Fares, Radwa A Eladwy, Alessio Nocentini, Soha R Abd El Hadi, Hazem A Ghabbour, Ashraf Abdel-Megeed, Wagdy M Eldehna, Hatem A Abdel-Aziz, Claudiu T Supuran
Using celecoxib as lead, two novel series of sulfonamides incorporating the pyridotriazolopyrimidine scaffold have been synthesized and evaluated in vitro as inhibitors against four relevant human (h) carbonic anhydrases (CAs, EC 4.2.1.1), the cytosolic and ubiquitous hCA I and II as well as the transmembrane hCA IV and hCA IX. Most of the reported sulfonamides acted as efficient, low micromolar inhibitors of hCAI, II and IV, whereas they displayed higher efficacy in inhibiting the tumor-associated isoform hCA IX...
February 21, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28253618/discovery-of-benzenesulfonamides-with-potent-human-carbonic-anhydrase-inhibitory-and-effective-anticonvulsant-action-design-synthesis-and-pharmacological-assessment
#16
Chandra Bhushan Mishra, Shikha Kumari, Andrea Angeli, Simona Maria Monti, Martina Buonanno, Manisha Tiwari, Claudiu T Supuran
We report two series of novel benzenesulfonamide derivatives acting as effective carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. The synthesized compounds were tested against human (h) isoforms hCA I, hCA II, hCA VII, and hCA XII. The first series of compounds, 4-(3-(2-(4-substitued piperazin-1-yl)ethyl)ureido)benzenesulfonamides, showed low nanomolar inhibitory action against hCA II, being less effective against the other isoforms. The second series, 2-(4-substitued piperazin-1-yl)-N-(4-sulfamoylphenyl)acetamide derivatives, showed low nanomolar inhibitory activity against hCA II and hCA VII, isoforms involved in epileptogenesis...
March 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28247450/influence-of-salivary-parameters-in-the-caries-development-in-orthodontic-patients-an-observational-clinical-study
#17
Andréia A Cardoso, Lenita M Lopes, Lívia P Rodrigues, Jéssica J Teixeira, Carolina Steiner-Oliveira, Marinês Nobre-Dos-Santos
BACKGROUND: Previous studies have shown during the orthodontic treatment, the prevalence of active caries lesions (ACL) in 30 to 70% of patients. AIM: To evaluate the effect of orthodontic treatment on salivary properties considering caries development. DESIGN: Twenty two individuals (11-22 years) were assessed regarding caries, oral hygiene, sugar exposure, salivary flow rate (SFR), buffering capacity, pH, carbonic anhydrase VI (CA VI) and amylase activity, at baseline, 1, 3 and 6 months after the orthodontic appliances placement...
March 1, 2017: International Journal of Paediatric Dentistry
https://www.readbyqxmd.com/read/28238511/comparison-of-the-anion-inhibition-profiles-of-the-%C3%AE-and-%C3%AE-carbonic-anhydrases-from-the-pathogenic-bacterium-burkholderia-pseudomallei
#18
Sonia Del Prete, Daniela Vullo, Pietro di Fonzo, Vincenzo Carginale, Claudiu T Supuran, Clemente Capasso
We report the cloning, purification and characterization of BpsβCA, a β-class carbonic anhydrase (CA, EC 4.2.1.1) from the pathogenic bacterium Burkholderia pseudomallei, the etiological agent of melioidosis, and compare its activity and inhibition with those of the γ-CA from the same organism, BpsγCA, recently investigated by our groups. BpsβCA showed a significant catalytic activity for the physiologic, CO2 hydration reaction, with the following kinetic parameters, kcat of 1.6×10(5)s(-1) and kcat/Km of 3...
February 16, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28237553/human-carbonic-anhydrase-inhibitory-profile-of-mono-and-bis-sulfonamides-synthesized-via-a-direct-sulfochlorination-of-3-and-4-hetero-arylisoxazol-5-amine-scaffolds
#19
Mikhail Krasavin, Mikhail Korsakov, Zhanna Zvonaryova, Evgenii Semyonychev, Tiziano Tuccinardi, Stanislav Kalinin, Muhammet Tanç, Claudiu T Supuran
Three distinct series of isoxazole-based primary mono- and bis-sulfonamides have been synthesized via direct sulfochlorination, each of them delivering nanomolar inhibitors of human carbonic anhydrase. Certain pronounced SAR trends have been established and rationalized by in silico docking. These findings expand the structure-activity knowledge base for heterocycle-containing sulfonamide carbonic anhydrase inhibitors and further validate the power of direct electrophilic sulfochlorination as a means of introducing the pharmacophoric primary sulfonamide group into structurally diverse aromatic precursors...
February 13, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28234904/biotransformation-of-a-potent-anabolic-steroid-mibolerone-with-cunninghamella-blakesleeana-c-echinulata-and-macrophomina-phaseolina-and-biological-activity-evaluation-of-its-metabolites
#20
Mahwish Siddiqui, Malik Shoaib Ahmad, Atia-Tul- Wahab, Sammer Yousuf, Narjis Fatima, Nimra Naveed Shaikh, Atta-Ur- Rahman, M Iqbal Choudhary
Seven metabolites were obtained from the microbial transformation of anabolic-androgenic steroid mibolerone (1) with Cunninghamella blakesleeana, C. echinulata, and Macrophomina phaseolina. Their structures were determined as 10β,17β-dihydroxy-7α,17α-dimethylestr-4-en-3-one (2), 6β,17β-dihydroxy-7α,17α-dimethylestr-4-en-3-one (3), 6β,10β,17β-trihydroxy-7α,17α-dimethylestr-4-en-3-one (4), 11β,17β-dihydroxy-(20-hydroxymethyl)-7α,17α-dimethylestr-4-en-3-one (5), 1α,17β-dihydroxy-7α,17α-dimethylestr-4-en-3-one (6), 1α,11β,17β-trihydroxy-7α,17α-dimethylestr-4-en-3-one (7), and 11β,17β-dihydroxy-7α,17α-dimethylestr-4-en-3-one (8), on the basis of spectroscopic studies...
2017: PloS One
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