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Carbonic anhydrase 3

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https://www.readbyqxmd.com/read/28416105/do-clear-cell-papillary-renal-cell-carcinomas-have-malignant-potential-diolombi-ml-cheng-l-argani-p-epstein-ji-am-j-surg-pathol-december-2015-39-12-1621-1634
#1
Oleksandr N Kryvenko
There have been no recurrences or metastases of clear cell papillary renal cell carcinoma (CCPRCC) in 268 reported cases with follow-up in the English-language literature. We identified all our cases of CCPRCC (1990-2013), reviewing all cases that preceded the formal designation of the entity. Immunohistochemical stains were performed on 32 cases during their initial workup. In addition, stains for carbonic anhydrase IX and cytokeratin 7 were performed on 2 cases, one with atypical follow-up and the other with a more compact morphology, although not performed initially...
April 13, 2017: Urologic Oncology
https://www.readbyqxmd.com/read/28416101/n-substituted-and-ring-opened-saccharin-derivatives-selectively-inhibit-transmembrane-tumor-associated-carbonic-anhydrases-ix-and-xii
#2
Jekaterīna Ivanova, Fabrizio Carta, Daniela Vullo, Janis Leitans, Andris Kazaks, Kaspars Tars, Raivis Žalubovskis, Claudiu T Supuran
A series of N-substituted saccharins incorporating aryl, alkyl and alkynyl moieties, as well as some ring opened derivatives were prepared and investigated as inhibitors of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1). The widespread cytosolic isoforms CA I and II were not inhibited by these sulfonamides whereas transmembrane, tumor-associated ones were effectively inhibited, with KIs in the range of 22.1-481nM for CA IX and of 3.9-245nM for hCA XII. Although the inhibition mechanism of these tertiary/secondary sulfonamides is unknown for the moment, the good efficacy and especially selectivity for the inhibition of the tumor-associated over the cytosolic, widespread isoforms, make these derivatives of considerable interest as enzyme inhibitors with various pharmacologic applications...
April 7, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28405482/the-relationship-between-serum-carbonic-anhydrase-i-ii-autoantibody-levels-and-diabetic-retinopathy-in-type-1-diabetes-patients
#3
Adem Türk, Süleyman Mollamehmetoğlu, Ahmet Alver, Ahmet Menteşe, İrfan Nuhoğlu, Cihangir Erem, Halil İbrahim İmamoğlu
OBJECTIVES: To investigate the relationship between serum carbonic anhydrase I-II (CA-I and II) autoantibody levels and diabetic retinopathy (DRP) in cases with type 1 diabetes. MATERIALS AND METHODS: A total of 37 type-1 diabetic patients, 17 with DRP (group 1) and 20 without (group 2), and 38 healthy control subjects (group 3) were included. CA-I and CA-II autoantibody levels were measured in serum samples obtained from each of the three groups and compared statistically...
April 2017: Turkish Journal of Ophthalmology
https://www.readbyqxmd.com/read/28396658/characterisation-of-aerotolerant-forms-of-a-robust-chicken-colonizing-campylobacter-coli
#4
Peter M O'Kane, Ian F Connerton
Campylobacter contaminated poultry meat is a major source of human foodborne illness. Campylobacter coli strain OR12 is a robust colonizer of chickens that was previously shown to outcompete and displace other Campylobacter strains from the chicken's gastrointestinal tract. This strain is capable of aerobic growth on blood agar. Serial aerobic passage increased this aerotolerance as assessed by quantitative assays for growth and survival on solid media. Aerotolerance was also associated with increased peroxide stress resistance...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28391155/an-approach-to-clarify-the-effect-mechanism-of-glyphosate-on-body-malformations-during-embryonic-development-of-zebrafish-daino-rerio
#5
Ekrem Sulukan, Mine Köktürk, Hamid Ceylan, Şükrü Beydemir, Mesut Işik, Muhammed Atamanalp, Saltuk Buğrahan Ceyhun
In this study, it has been investigated that the effects of glyphosate, which is a herbicide within organophosphate and unselective widely used in agriculture on enzyme activity of carbonic anhydrase, production of reactive oxygen species, cell apoptosis and body morphology during the embryonic development of zebrafish. To this end, it has been treated embryo with 1, 5, 10 and 100 mg/L gyphosate at 96 h. The embryos treated with glyphosate from 4 hpf were evaluated by considering the survival rates, hatching rates, body malformations under the stereo microscope in 24, 48, 72 and 96th hours...
April 5, 2017: Chemosphere
https://www.readbyqxmd.com/read/28390994/carbohydrazones-as-new-class-of-carbonic-anhydrase-inhibitors-synthesis-kinetics-and-ligand-docking-studies
#6
Sarosh Iqbal, Muhammad Saleem, M Kamran Azim, Muhammad Taha, Uzma Salar, Khalid Mohammed Khan, Shahnaz Perveen, M Iqbal Choudhary
Discovery and development of carbonic anhydrase inhibitors is crucial for their clinical use as antiepileptic, diurectic and antiglaucoma agents. Keeping this in mind, we have synthesized carbohydrazones 1-27 and evaluated them for their in vitro carbonic anhydrase inhibitory potential. Out of twenty-seven compounds, compounds 1 (IC50=1.33±0.01µM), 2 (IC50=1.85±0.24µM), 3 (IC50=1.37±0.06µM), and 9 (IC50=1.46±0.12µM) have showed carbonic anhydrase inhibition better than the standard drug zonisamide (IC50=1...
March 30, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28389112/synthesis-of-new-3-2-mercapto-4-oxo-4h-quinazolin-3-yl-benzenesulfonamides-with-strong-inhibition-properties-against-the-tumor-associated-carbonic-anhydrases-ix-and-xii
#7
Murat Bozdag, Ahmed Mahmoud Alafeefy, Abdul Malik Altamimi, Fabrizio Carta, Claudiu T Supuran, Daniela Vullo
We report a series of novel metanilamide-based derivatives 3a-q bearing the 2-mercapto-4-oxo-4H-quinazolin-3-yl moiety as tail. All compounds were synthesized by means of straightforward condensation procedures and were investigated in vitro for their inhibition potency against the human (h) carbonic anhydrase (CA; EC 4.2.1.1.1) isoforms I, II, IX and XII. Among all compounds tested the 6-iodo 3g and the 7-fluoro 3i derivatives were the most potent inhibitors against the tumor associated CA IX and XII isoform (KIs 1...
May 15, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28385087/design-synthesis-and-evaluation-of-18-f-labeled-cationic-carbonic-anhydrase-ix-inhibitors-for-pet-imaging
#8
Zhengxing Zhang, Joseph Lau, Chengcheng Zhang, Nadine Colpo, Alessio Nocentini, Claudiu T Supuran, François Bénard, Kuo-Shyan Lin
Carbonic anhydrase IX (CA-IX) is a marker for tumor hypoxia, and its expression is negatively correlated with patient survival. CA-IX represents a potential target for eliminating hypoxic cancers. We synthesized fluorinated cationic sulfonamide inhibitors 1-3 designed to target CA-IX. The binding affinity for CA-IX ranged from 0.22 to 0.96 μM. We evaluated compound 2 as a diagnostic PET imaging agent. Compound 2 was radiolabeled with (18)F in 10 ± 4% decay-corrected radiochemical yield with 85.1 ± 70...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28382581/the-prominent-proteins-expressed-in-healthy-gingiva-a-pilot-exploratory-tissue-proteomics-study
#9
Emre Yaprak, Murat Kasap, Gürler Akpınar, Sibel Kayaaltı-Yüksek, Alper Sinanoğlu, Nil Guzel, Husniye Demirturk Kocasarac
Gingiva is a unique tissue which protects the underlying periodontal tissues from consistent mechanical and bacterial aggressions. Molecular analysis of gingiva is likely to improve our understanding of the underlying biological processes at work. The aim of this preliminary exploratory study is to analyze the proteomic profile of healthy gingiva and to detect prominently expressed proteins. Gingival tissue samples were obtained from periodontally healthy individuals who underwent surgical crown lengthening procedure...
April 5, 2017: Odontology
https://www.readbyqxmd.com/read/28380234/the-lock-is-the-key-development-of-novel-drugs-through-receptor-based-combinatorial-chemistry
#10
REVIEW
Nikola Maraković, Goran Šinko
Modern drug discovery is mainly based on the de novo synthesis of a large number of compounds with a diversity of chemical functionalities. Though the introduction of combinatorial chemistry enabled the preparation of large libraries of compounds from so-called building blocks, the problem of successfully identifying leads remains. The introduction of a dynamic combinatorial chemistry method served as a step forward due to the involvement of biological macromolecular targets (receptors) in the synthesis of high affinity products...
2017: Acta Chimica Slovenica
https://www.readbyqxmd.com/read/28371704/seasonal-variations-of-carbonic-anhydrase-activity-in-chongqing-urban-section-of-jialing-river-and-its-influencing-factors
#11
Yudong Nie, Zhi Zhang, Min Wang, Qian Shen, Yinfan Li, Wenjing Gao, Lu Yang
Carbonic anhydrase (CA) is an enzyme in algal carbon-utilization that plays an important role in the formation of algal blooms. A year-long monitoring program in the shore area of Chongqing Urban Section of the Jialing River (JR) was launched to determine the variations in carbonic anhydrase activity (CAA) and its change mechanism in the hydro-fluctuation belt of the tributaries in the Three Gorges Reservoir (TGR) area. The variations in basic water quality parameters, different carbon forms, and CAA were investigated from November 2013 to October 2014...
July 2017: Chemosphere
https://www.readbyqxmd.com/read/28362240/microvascularization-of-grade-i-meningiomas-effect-on-tumor-volume-blood-loss-and-patient-outcome
#12
Michael Karsy, Brian Burnett, Antonio Di Ieva, Michael D Cusimano, Randy L Jensen
OBJECTIVE Quantitative assessment of tumor microvascularity has the potential to improve prognostication, advance understanding of tumor biology, and help narrow potential molecular therapies. While the role of tumor microvascularity has been widely studied in meningiomas, this study examines both the role of automated measurements and the impact on surgical outcome. METHODS Two hundred seven patients with Grade I meningiomas underwent surgery between 1996 and 2011. Tissue samples from each patient were retrospectively evaluated for histopathological measures of microvascularity, including staining for von Willebrand factor (vWF), CD31, CD105, hypoxia-inducible factor 1 (HIF-1), vascular endothelial growth factor, glucose transporter 1, and carbonic anhydrase IX...
March 31, 2017: Journal of Neurosurgery
https://www.readbyqxmd.com/read/28345583/synergistic-effects-of-micro-electrolysis-photocatalysis-on-water-treatment-and-fish-performance-in-saline-recirculating-aquaculture-system
#13
Zhangying Ye, Shuo Wang, Weishan Gao, Haijun Li, Luowei Pei, Mingwei Shen, Songming Zhu
A new physico-chemical process for TAN (total ammonia nitrogen) removal and disinfection is introduced in saline recirculating aquaculture system (RAS), in which the biofilter is replaced with an integrated electrolysis cell and an activated carbon filter. The electrolysis cell which is based on micro current electrolysis combined with UV-light was self-designed. After the fundamental research, a small pilot scale RAS was operated for 30 days to verify the technical feasibility. The system was stocked by 42 GIFT tilapia (Oreochromis niloticus) fish with the rearing density of 13 kg/m(3)...
March 27, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28324887/association-between-hypoxic-volume-and-underlying-hypoxia-induced-gene-expression-in-oropharyngeal-squamous-cell-carcinoma
#14
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...
April 11, 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
#15
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-carbon-dioxide-reduction-in-a-bioelectrochemical-system-effect-of-immobilization-and-carbonic-anhydrase-addition
#16
Sandipam Srikanth, Yolanda Alvarez-Gallego, Karolien Vanbroekhoven, Deepak Pant
The enzymatic electrosynthesis of formic acid from the reduction of carbon dioxide (CO2 ) by using formate dehydrogenase (FDH) as a catalyst at the cathode in both its free and immobilized forms was studied in detail in a bioelectrochemical system (BES). The essential role of solubilizing CO2 for its conversion was also studied by adding carbonic anhydrase (CA) to the FDH enzyme in both its free and immobilized forms. FDH alone in the free form showed large variation in the reduction current [(-6.2±3.9) A m(-2) ], whereas 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
#17
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
#18
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
#19
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
#20
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
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