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Carbonic anhydrase 3

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https://www.readbyqxmd.com/read/28076854/open-angle-glaucoma-drug-development-pipeline-during-the-last-20-years-1995-2015
#1
André Vicente, Sylvie Prud'homme, Joana Ferreira, Luís Abegão Pinto, Ingeborg Stalmans
OBJECTIVES: To analyse drug development for open-angle glaucoma during the last 20 years. METHODS: Research was performed by referring to clinical trials registered at the International Clinical Trials Registry Platform (ICTRP). A search for the condition "open-angle glaucoma" with the intervention "drug" was performed. We included trials registered from 01/01/1995 to 01/01/2015, only involving studies in phases 1, 2, and 3. Only studies resorting to novel treatment strategies (either novel drugs or yet-untested fixed associations of approved medication) were considered...
January 12, 2017: Ophthalmic Research
https://www.readbyqxmd.com/read/28057408/dithiocarbamates-effectively-inhibit-the-%C3%AE-carbonic-anhydrase-from-the-dandruff-producing-fungus-malassezia-globosa
#2
Daniela Vullo, Sonia Del Prete, Alessio Nocentini, Sameh M Osman, Zeid AlOthman, Clemente Capasso, Murat Bozdag, Fabrizio Carta, Paola Gratteri, Claudiu T Supuran
A series of dithiocarbamates (DTCs) was investigated for the inhibition of the β-class carbonic anhydrase (CAs, EC 4.2.1.1) from the fungal parasite Malassezia globosa, MgCA, a validated anti-dandruff drug target. These DTCs incorporate various scaffold, among which those of N,N-dimethylaminoethylenediamine, the aminoalcohols with 3-5 carbon atoms in their molecule, 3-amino-quinuclidine, piperidine, morpholine and piperazine derivatives, as well as phenethylamine and its 4-sulfamoylated derivative. Several DTCs resulted more effective in inhibiting MgCA compared to the standard sulfonamide drug acetazolamide (KI of 74μM), with KIs ranging between 383 and 6235nM...
December 27, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28055960/-genetic-disruption-of-the-phi-regulating-proteins-na-h-exchanger-1-slc9a1-and-carbonic-anhydrase-9-severely-reduces-growth-of-colon-cancer-cells
#3
Scott K Parks, Yann Cormerais, Jerome Durivault, Jacques Pouyssegur
Hypoxia and extracellular acidosis are pathophysiological hallmarks of aggressive solid tumors. Regulation of intracellular pH (pHi) is essential for the maintenance of tumor cell metabolism and proliferation in this microenvironment and key proteins involved in pHi regulation are of interest for therapeutic development. Carbonic anhydrase 9 (CA9) is one of the most robustly regulated proteins by the hypoxia inducible factor (HIF) and contributes to pHi regulation. Here, we have investigated for the first time, the role of CA9 via complete genomic knockout (ko) and compared its impact on tumor cell physiology with the essential pHi regulator Na+/H+ exchanger 1 (NHE1)...
December 30, 2016: Oncotarget
https://www.readbyqxmd.com/read/28051026/blood-oxygenation-level-dependent-magnetic-resonance-imaging-of-breast-cancer-correlation-with-carbonic-anhydrase-ix-and-vascular-endothelial-growth-factor
#4
Ying Wang, Min Liu, Mu-Lan Jin
BACKGROUND: Blood oxygenation level-dependent magnetic resonance imaging (BOLD-MRI) is a functional MRI technique which involves using the paramagnetic properties of deoxyhemoglobin to image the local tissue oxygen concentration. The purpose of this study was to investigate whether BOLD-MRI could evaluate hypoxia and angiogenesis of breast invasive ductal carcinoma (IDC). METHODS: Ninety-eight female patients with IDC were retrospectively included in this research...
2017: Chinese Medical Journal
https://www.readbyqxmd.com/read/28043719/synthesis-characterization-anticancer-antimicrobial-and-carbonic-anhydrase-inhibition-profiles-of-novel-3ar-4s-7r-7as-2-4-e-3-3-aryl-acryloyl-phenyl-3a-4-7-7a-tetrahydro-1h-4-7-methanoisoindole-1-3-2h-dione-derivatives
#5
Umit M Kocyigit, Yakup Budak, Meliha Burcu Gürdere, Şaban Tekin, Tuğba Kul Köprülü, Fatih Ertürk, Kezban Özcan, İlhami Gülçin, Mustafa Ceylan
In the present study, a series of new hybrid compounds containing chalcone and methanoisoindole units 7a-n ((3aR,4S,7R,7aS)-2-(4-((E)-3-(3-aryl)acryloyl) phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione) were synthesized, characterized and investigated for their anticancer activity against C6 gliocarcinoma cell in rats, and antimicrobial activity against some human pathogen microorganisms. The compounds 7e, 7h, 7j, 7k, 7L and 7n showed very high anticancer activity with the inhibition range of 80...
December 23, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28038999/carbonic-anhydrase-inhibition-boosts-the-antitumor-effects-of-imatinib-mesylate-via-potentiating-the-antiangiogenic-and-antimetastatic-machineries
#6
Amal A Abd-El Fattah, Hebatallah A Darwish, Nevine Fathy, Samia A Shouman
Carbonic anhydrase inhibitors have emerged in the past few years as an interesting candidate for the development of novel unconventional strategies. Despite their effect in tumor regression via inhibition of tumor acidification, their potential role is not yet fully elucidated. Herein, we investigated whether acetazolamide (AZ) could modulate imatinib (IM) anticancer activity, both in breast cancer cells (T47D) and in isolated tumor specimens of Ehrlich ascites carcinoma (EAC). The impact of this combination on angiogenesis was evidenced by decreasing PDGF-A expression and enhancing that of TSP-1...
December 28, 2016: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28025002/sulfonamide-inhibition-profile-of-the-%C3%AE-carbonic-anhydrase-identified-in-the-genome-of-the-pathogenic-bacterium-burkholderia-pseudomallei-the-etiological-agent-responsible-of-melioidosis
#7
Sonia Del Prete, Daniela Vullo, Pietro Di Fonzo, Sameh M Osman, Zeid AlOthman, William A Donald, Claudiu T Supuran, Clemente Capasso
A new γ-carbonic anhydrase (CA, EC 4.1.1.1) was cloned and characterized kinetically in the genome of the bacterial pathogen Burkholderia pseudomallei, the etiological agent of melioidosis, an endemic disease of tropical and sub-tropical regions of the world. The catalytic activity of this new enzyme, BpsCAγ, is significant with a kcat of 5.3×10(5)s(-1) and kcat/Km of 2.5×10(7)M(-1)×s(-1) for the physiologic CO2 hydration reaction. The inhibition constant value for this enzyme for 39 sulfonamide inhibitors was obtained...
December 12, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28009604/renal-cell-carcinoma-with-chromosome-6p-amplification-including-the-tfeb-gene-a-novel-mechanism-of-tumor-pathogenesis
#8
Sean R Williamson, David J Grignon, Liang Cheng, Laura Favazza, Dibson D Gondim, Shannon Carskadon, Nilesh S Gupta, Dhananjay A Chitale, Shanker Kalyana-Sundaram, Nallasivam Palanisamy
Amplification of chromosome 6p has been implicated in aggressive behavior in several cancers, but has not been characterized in renal cell carcinoma (RCC). We identified 9 renal tumors with amplification of chromosome 6p including the TFEB gene, 3 by fluorescence in situ hybridization, and 6 from the Cancer Genome Atlas (TCGA) databases. Patients' ages were 28 to 78 years (median, 61 y). Most tumors were high stage (7/9 pT3a, 2/9 pN1). Using immunohistochemistry, 2/4 were positive for melanocytic markers and cathepsin K...
December 22, 2016: American Journal of Surgical Pathology
https://www.readbyqxmd.com/read/28001003/intrinsic-thermodynamics-and-structures-of-2-4-and-3-4-substituted-fluorinated-benzenesulfonamides-binding-to-carbonic-anhydrases
#9
Asta Zubrienė, Alexey Smirnov, Virginija Dudutienė, David D Timm, Jurgita Matulienė, Vilma Michailovienė, Audrius Zakšauskas, Elena Manakova, Saulius Gražulis, Daumantas Matulis
The goal of rational drug design is to understand structure-thermodynamics correlations in order to predict the chemical structure of a drug that would exhibit excellent affinity and selectivity for a target protein. In this study we explored the contribution of added functionalities of benzenesulfonamide inhibitors to the intrinsic binding affinity, enthalpy, and entropy for recombinant human carbonic anhydrases (CA) CA I, CA II, CA VII, CA IX, CA XII, and CA XIII. The binding enthalpies of compounds possessing similar chemical structures and affinities were found to be very different, spanning a range from -90 to +10 kJ mol(-1) , and are compensated by a similar opposing entropy contribution...
December 21, 2016: ChemMedChem
https://www.readbyqxmd.com/read/27984137/novel-eugenol-derivatives-potent-acetylcholinesterase-and-carbonic-anhydrase-inhibitors
#10
Fevzi Topal, Ilhami Gulcin, Arif Dastan, Murat Guney
Eugenol was used as starting material to obtain some phenolic compounds. The synthesis of these phenolic compounds was performed in a two-step procedure. The structures of the formed products (novel eugenol derivatives 1-6) have been determined on the basis of NMR spectroscopy and other spectroscopic methods. The compounds were tested in terms of carbonic anhydrase (CA) inhibition potency. Carbonic anhydrases (CAs, EC 4.2.1.1) are metalloenzymes, which catalyse the reaction between carbon dioxide (CO2) and water (H2O), to generate bicarbonate (HCO3(-)) and protons (H(+))...
October 28, 2016: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/27939347/coumarins-and-other-fused-bicyclic-heterocycles-with-selective-tumor-associated-carbonic-anhydrase-isoforms-inhibitory-activity
#11
Murat Bozdag, Ahmed Mahmoud Alafeefy, Abdul Malik Altamimi, Daniela Vullo, Fabrizio Carta, Claudiu T Supuran
Herein we report for the first time a series of 2-benzamido-N-(2-oxo-4-(methyl/trifluoromethyl)-2H-chromen-7-yl) benzamide 3a-f and substituted quinazolin-4(3H)-ones and 2H-benzo[e][1,2,4]thiadiazin-3(4H)-one 1,1-dioxides (5, 6, 8 and 10a-c) as selective inhibitors of the tumor associated hCA IX and XII isoforms. Among the compounds reported the trifluoromethyl derivative 3d resulted the most potent against these CA isoforms with KIs of 10.9 and 6.7nM.
January 15, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27933963/benzenesulfonamides-incorporating-flexible-triazole-moieties-are-highly-effective-carbonic-anhydrase-inhibitors-synthesis-and-kinetic-crystallographic-computational-and-intraocular-pressure-lowering-investigations
#12
Alessio Nocentini, Marta Ferraroni, Fabrizio Carta, Mariangela Ceruso, Paola Gratteri, Cecilia Lanzi, Emanuela Masini, Claudiu T Supuran
Herein we report the synthesis of two series of benzenesulfonamide containing compounds that incorporate the phenyl-1,2,3-triazole moieties. We explored the insertion of appropriate linkers, such as ether, thioether, and amino type, into the inner section of the molecules with the intent to confer additional flexibility. All obtained compounds were screened in vitro as inhibitors of the physiologically relevant human (h) isoforms of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1). Many of them were low nanomolar or subnanomolar hCA II, IX, and XII inhibitors, whereas they did not potently inhibit hCA I...
December 8, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27919611/discovery-of-4-sulfamoyl-phenyl-%C3%AE-lactams-as-a-new-class-of-potent-carbonic-anhydrase-isoforms-i-ii-iv-and-vii-inhibitors-the-first-example-of-subnanomolar-ca-iv-inhibitors
#13
Srinivas Angapelly, P V Sri Ramya, Andrea Angeli, Simona Maria Monti, Martina Buonanno, Mallika Alvala, Cladiu T Supuran, Mohammed Arifuddin
A series of benzenesulfonamides incorporating 1,3,4-trisubstituted-β-lactam moieties was prepared from sulfanilamide Schiff bases and in situ obtained ketenes, by using the Staudinger cycloaddition reaction. The new compounds were assayed as inhibitors of four human isoforms of the metalloenzyme carbonic anhydrase (hCA, EC 4.2.1.1) involved in various physiological/pathological conditions, hCA I, II, IV and VII. Excellent inhibitory activity was observed against all these isoforms, as follows: hCA I, involved in some eye diseases was inhibited with KIs in the range of 7...
January 15, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27914949/anion-inhibition-profiles-of-the-%C3%AE-carbonic-anhydrase-from-the-pathogenic-bacterium-burkholderia-pseudomallei-responsible-of-melioidosis-and-highly-drug-resistant-to-common-antibiotics
#14
Sonia Del Prete, Daniela Vullo, Pietro Di Fonzo, Sameh M Osman, Zeid AlOthman, Claudiu T Supuran, Clemente Capasso
Burkholderia pseudomallei is a Gram-negative saprophytic bacterium responsible of melioidosis, an endemic disease of tropical and sub-tropical regions of the world. A recombinant γ-CA (BpsγCA) identified in the genome of this bacterium was cloned and purified. Its catalytic activity and anion inhibition profiles were investigated. The enzyme was an efficient catalyst for the CO2 hydration showing a kcat of 5.3×10(5)s(-1) and kcat/Km of 2.5×10(7)M(-1)×s(-1). The best BpsγCA inhibitors were sulfamide, sulfamic acid, phenylboronic acid and phenylarsonic acid, which showed KI in the range of 49-83μM (these inhibitors showed millimolar inhibition constant against hCA II), followed by diethyldithiocarbamate, selenate, tellurate, perrhenate, selenocyanate, trithiocarbonate, tetraborato, pyrophosphate, stannate, carbonate, bicarbonate, azide, cyanide, thiocyanate and cyanate with KIs in the range of 0...
January 15, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27913439/retinitis-pigmentosa-associated-cystoid-macular-oedema-pathogenesis-and-avenues-of-intervention
#15
REVIEW
S Strong, G Liew, M Michaelides
Hereditary retinal diseases are now the leading cause of blindness certification in the working age population (age 16-64 years) in England and Wales, of which retinitis pigmentosa (RP) is the most common disorder. RP may be complicated by cystoid macular oedema (CMO), causing a reduction of central vision. The underlying pathogenesis of RP-associated CMO (RP-CMO) remains uncertain, however, several mechanisms have been proposed, including: (1) breakdown of the blood-retinal barrier, (2) failure (or dysfunction) of the pumping mechanism in the retinal pigment epithelial, (3) Müller cell oedema and dysfunction, (4) antiretinal antibodies and (5) vitreous traction...
January 2017: British Journal of Ophthalmology
https://www.readbyqxmd.com/read/27894244/umbelliferone-decreases-intracellular-ph-and-sensitizes-melanoma-cell-line-a375-to-dacarbazin-comparison-with-acetazolamide
#16
Clémentine Puech, Morgane Chatard, Delphine Felder-Flesch, Nathalie Prevot, Nathalie Perek
The high degree of malignancy of tumour cells is linked to alterations of many physiological parameters like the intracellular pH (pHi). The pHi in cancer cell line is regulated by the anhydrase carbonique IX (CA IX). The main enzymatic function of the CA IX protein is to catalyze the hydration of carbon dioxide into bicarbonate ions and protons. Inhibiton of transmembrane tumor associated isozyme carbonic anhydrase IX (CA IX) with specific inhibitors is a promising and expanding field as CA IX is involved in tumor progression...
November 28, 2016: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/27859585/synthesis-and-carbonic-anhydrase-inhibition-of-novel-2-4-aryl-thiazole-2-yl-3a-4-7-7a-tetrahydro-1h-4-7-methanoisoindole-1-3-2h-dione-derivatives
#17
Umit M Kocyigit, Osman Nuri Aslan, Ilhami Gulcin, Yusuf Temel, Mustafa Ceylan
Carbonic anhydrase (CA, EC 4.2.1.1) is a member of the metalloenzyme family. It catalyzes the rapid conversion of carbon dioxide (CO2 ) and water to bicarbonate (HCO3(-) ) and protons (H(+) ) and also plays an important role in biochemical and physiological processes. In this study, a number of novel 2-(4-(aryl)thiazole-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives were synthesized and evaluated for their inhibitory characteristics against the human CA isoenzymes I and II (hCA I and hCA II)...
December 2016: Archiv der Pharmazie
https://www.readbyqxmd.com/read/27858178/proteome-analysis-of-hemofilter-adsorbates-to-identify-novel-substances-of-sepsis-a-pilot-study
#18
Tomoaki Hashida, Taka-Aki Nakada, Mamoru Satoh, Keisuke Tomita, Rui Kawaguchi, Fumio Nomura, Shigeto Oda
Blood purification therapy using hemofilters with high adsorbing capabilities has been reported to remove excessive humoral mediators from the blood of patients with sepsis. However, there are insufficient studies of the adsorbates bound to hemofilter membranes. We hypothesized that these adsorbates in acute kidney injury (AKI) patients with sepsis were different from those in patients without sepsis and that proteome analysis of the adsorbates would identify novel substances of sepsis. This study included 20 patients who had AKI upon admission to intensive care units (ICUs) and who received continuous renal replacement therapy using polymethyl methacrylate hemofilters...
November 17, 2016: Journal of Artificial Organs: the Official Journal of the Japanese Society for Artificial Organs
https://www.readbyqxmd.com/read/27852754/ammonia-excretion-in-the-marine-polychaete-eurythoe-complanata-annelida
#19
Daniel Thiel, Maja Hugenschütt, Heiko Meyer, Achim Paululat, Alex R Quijada-Rodriguez, Günter Purschke, Dirk Weihrauch
Ammonia is a toxic waste product from protein metabolism and needs to be either converted into less toxic molecules or, in the case of fish and aquatic invertebrates, excreted directly as is. In contrast to fish, very little is known regarding the ammonia excretion mechanism and the participating excretory organs in marine invertebrates. In the current study ammonia excretion in the marine burrowing polychaete Eurythoe complanata was investigated. As a potential site for excretion the 100-200 micrometer long, 30-50 micrometer wide and up to 25 micrometer thick dentrically branched, well ventilated and vascularized branchiae (gills) were identified...
November 16, 2016: Journal of Experimental Biology
https://www.readbyqxmd.com/read/27833999/methyl-%C3%AE-cyclodextrin-treatment-combined-to-incubation-with-interleukin-4-reproduces-major-features-of-atopic-dermatitis-in-a-3d-culture-model
#20
Tatiana do Nascimento Pedrosa, Evelyne De Vuyst, Abdallah Mound, Catherine Lambert de Rouvroit, Silvya Stuchi Maria-Engler, Yves Poumay
Atopic dermatitis (AD) skin is characterized by over-expression of interleukin (IL)-4, IL-13 and IL-25. When methyl-β-cyclodextrin (MβCD) treatment preceded exposure to these interleukins, combination of both treatments was found to mimic hallmarks of AD in vitro, such as barrier weakening, histological alterations and typical signaling responses in a reconstructed human epidermis (RHE). However, the respective role of each IL and whether any of them is critical when combined with MβCD treatment was unknown...
January 2017: Archives of Dermatological Research
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