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Carbonic anhydrase 3

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https://www.readbyqxmd.com/read/28524139/-ocular-hypotensive-effect-of-systemic-beta-blockers-in-patients-with-primary-glaucoma-and-arterial-hypertension
#1
A L Onishchenko, A V Kolbasko, A V Zakharova, E G Onishchenko, N M Zhilina
AIM: to evaluate the ocular hypotensive efficacy of systemic beta-blockers in primary glaucoma patients suffering from arterial hypertension (AH). MATERIAL AND METHODS: The study included 29 patients with POAG (58 eyes) aged from 47 to 83 years. Patients with stage I-III POAG received instillations of prostaglandin analogs and carbonic anhydrase inhibitors. All POAG patients also suffered from arterial hypertension and were prescribed selective beta-blockers (metoprolol, bisoprolol, or nebivalol) as monotherapy or as part of combination therapy (if the target arterial pressure had not been achieved under the initial treatment)...
2017: Vestnik Oftalmologii
https://www.readbyqxmd.com/read/28524136/-clinical-evaluation-of-the-effectiveness-of-cholinesterase-inhibition-with-neuromidin-in-the-treatment-of-primary-glaucoma-patients
#2
I A Zakharova, R V Avdeev, V A Pristavka, S N Surnin, V Yu Makhmutov, I I Savrasova
AIM: to investigate neuromidin effectiveness in the treatment of patients with primary glaucoma and compensated intraocular pressure (IOP). MATERIAL AND METHODS: A total of 40 patients (80 eyes) were examined. Of them, 10 eyes with early glaucoma, 36 eyes with moderate-stage glaucoma, 33 eyes with advanced glaucoma, and 1 eye with end-stage glaucoma. In 19 eyes, IOP was controlled through beta-blockers, in 11 eyes - through carbonic anhydrase inhibitors, in 10 eyes - through prostaglandin analogues, and in 39 eyes - through combination drugs...
2017: Vestnik Oftalmologii
https://www.readbyqxmd.com/read/28511907/potential-inhibitors-of-human-carbonic-anhydrase-isozymes-i-and-ii-design-synthesis-and-docking-studies-of-new-1-3-4-thiadiazole-derivatives
#3
Mehlika Dilek Altıntop, Belgin Sever, Ahmet Özdemir, Kaan Kucukoglu, Hicran Onem, Hayrunnisa Nadaroglu, Zafer Asım Kaplancıklı
In the last years, inhibition of carbonic anhydrase (CA) has emerged as a promising approach for pharmacologic intervention in a variety of disorders such as glaucoma, epilepsy, obesity, and cancer. As a consequence, the design of CA inhibitors (CAIs) is a highly dynamic field of medicinal chemistry. Due to the therapeutic potential of thiadiazoles as CAIs, new 1,3,4-thiadiazole derivatives were synthesized and investigated for their inhibitory effects on hCA I and hCA II. Although the tested compounds did not carry a sulfonamide group, an important pharmacophore for CA inhibitory activity, it was a remarkable finding that most of them were more effective on hCAs than acetazolamide (AAZ), the reference agent...
May 5, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28498313/identifying-the-genes-regulated-by-atwrky6-using-comparative-transcript-and-proteomic-analysis-under-phosphorus-deficiency
#4
Li-Qin Li, Lu-Ping Huang, Gang Pan, Lun Liu, Xi-Yao Wang, Li-Ming Lu
Phosphorus (P) is an important mineral nutrient for plant growth and development. Overexpressing AtWRKY6 (35S:WRKY6-9) was more sensitive and wrky6 (wrky6-1) was more resistant under low Pi conditions. To better understand the function of AtWRKY6 under low phosphate stress conditions, we applied two-dimensional gel electrophoresis (2-DE) to analyse differentially expressed proteins in the shoots and roots between wild type, 35S:WRKY6-9 and wrky6-1 after phosphorus deficiency treatment for three days. The results showed 88 differentially abundant protein spots, which were identified between the shoots and roots of 35S:WRKY6-9 and wrky6-1 plants...
May 12, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28497265/proteomics-analysis-of-pleomorphic-adenoma-of-the-human-parotid-gland
#5
Ahmet Mutlu, Murat Ozturk, Gurler Akpinar, Murat Kasap, Aylin Kanli
The objective of this study is to perform proteomic analysis of pleomorphic adenoma (PA) in the human parotid gland (PG) with comparison of normal PG. This is an individual prospective randomized controlled trial. This study was performed in a tertiary referral center. Tissue samples of PG and PA were taken after surgical excision of PG from 13 patients. Protein extracts were prepared and protein pools created from the soluble extracts were subjected to 2D-DIGE analysis. Proteins displaying regulation in their abundance were determined and identified using MALDIT-OF/TOF analysis...
May 11, 2017: European Archives of Oto-rhino-laryngology
https://www.readbyqxmd.com/read/28496310/patient-satisfaction-with-fixed-combination-bimatoprost-timolol-ophthalmic-solution-a-survey-study-in-patients-with-glaucoma-in-china
#6
Xinghuai Sun, Mingkai Lin, Xuanchu Duan, Chun Zhang, Jian Ming
BACKGROUND: Poor adherence to treatment is a problem in glaucoma, and patient dissatisfaction with topical glaucoma medication is a barrier to adherence. The objective of this study was to evaluate glaucoma patients' satisfaction with fixed-combination bimatoprost/timolol ophthalmic solution (BTFC). METHODS: This observational, multicenter study was conducted in China in adults with glaucoma treated with BTFC for 1-3 months. Five hundred patients answered a questionnaire concerning their demographic characteristics, history of glaucoma and topical glaucoma treatment, and use of BTFC...
2017: Patient Preference and Adherence
https://www.readbyqxmd.com/read/28490422/cftr-mediated-anion-secretion-across-intestinal-epithelium-like-caco-2-monolayer-under-pth-stimulation-is-dependent-on-intermediate-conductance-k-channels
#7
Walailak Jantarajit, Kornkamon Lertsuwan, Jarinthorn Teerapornpuntakit, Nateetip Krishnamra, Narattaphol Charoenphandhu
Parathyroid hormone (PTH), a pleiotropic hormone that maintains mineral homeostasis, is also essential for controlling pH balance and ion transport across renal and intestinal epithelia. Optimization of luminal pH is important for absorption of trace elements, e.g., calcium and phosphorus. We have previously demonstrated that PTH rapidly stimulated electrogenic HCO3(-) secretion in intestinal epithelial-like Caco-2 monolayer, but the underlying cellular mechanism, contributions of other ions, particularly Cl(-) and K(+), and long-lasting responses are not completely understood...
May 10, 2017: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/28482217/ruthenium-ii-complexes-of-saccharin-with-dipyridoquinoxaline-and-dipyridophenazine-structures-biological-interactions-and-photoinduced-dna-damage-activity
#8
Priyaranjan Kumar, Srikanth Dasari, Ashis K Patra
Ruthenium complexes trans-[Ru(sac)2(dpq)2] (1) and trans-[Ru(sac)2(dppz)2] (2) where sac is artificial sweetener saccharin (o-sulfobenzimide; 1,2-benzothiazole-3(2H)-one1,1-dioxide (Hsac)), dpq = dipyrido[3,2-d:2',3'-f]quinoxaline and dppz = dipyrido[3,2-a:2',3'-c]phenazine have been synthesized and thoroughly characterized using various analytical and spectral techniques. Saccharin known to act as carbonic anhydrase IX (CA IX) inhibitor which is a biomarker for highly aggressive and proliferative tumor in hypoxic stress, so inhibition of CA IX is a potential strategy for anticancer chemotherapy...
May 3, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28473691/notochordal-and-nucleus-pulposus-marker-expression-is-maintained-by-sub-populations-of-adult-human-nucleus-pulposus-cells-through-aging-and-degeneration
#9
Stephen M Richardson, Francesca E Ludwinski, Kanna K Gnanalingham, Ross A Atkinson, Anthony J Freemont, Judith A Hoyland
The nucleus pulposus (NP) of the intervertebral disc (IVD) demonstrates substantial changes in cell and matrix composition with both ageing and degeneration. While recent transcriptomic profiling studies have helped define human NP cell phenotype, it remains unclear how expression of these markers is influenced by ageing or degeneration. Furthermore, cells of the NP are thought to derive from the notochord, although adult NP lacks identifiable notochordal (NC) cells. This study aimed to confirm expression of previously identified NP and NC marker genes in adult human NP cells from a range of ages and degenerate states...
May 4, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28467665/bryophyte-gas-exchange-dynamics-along-varying-hydration-status-reveal-a-significant-carbonyl-sulphide-cos-sink-in-the-dark-and-cos-source-in-the-light
#10
Teresa E Gimeno, Jérôme Ogée, Jessica Royles, Yves Gibon, Jason B West, Régis Burlett, Sam P Jones, Joana Sauze, Steven Wohl, Camille Benard, Bernard Genty, Lisa Wingate
Carbonyl sulphide (COS) is a potential tracer of gross primary productivity (GPP), assuming a unidirectional COS flux into the vegetation that scales with GPP. However, carbonic anhydrase (CA), the enzyme that hydrolyses COS, is expected to be light independent, and thus plants without stomata should continue to take up COS in the dark. We measured net CO2 (A(C) ) and COS (A(S) ) uptake rates from two astomatous bryophytes at different relative water contents (RWCs), COS concentrations, temperatures and light intensities...
May 3, 2017: New Phytologist
https://www.readbyqxmd.com/read/28453941/probing-molecular-interactions-between-human-carbonic-anhydrases-hcas-and-a-novel-class-of-benzenesulfonamides
#11
Elvira Bruno, Maria Rosa Buemi, Anna Di Fiore, Laura De Luca, Stefania Ferro, Andrea Angeli, Roberto Cirilli, Daniele Sadutto, Vincenzo Alterio, Simona Maria Monti, Claudiu T Supuran, Giuseppina De Simone, Rosaria Gitto
On the basis of X-ray crystallographic studies of the complex of hCA II with 4-(3,4-dihydro-1H-isoquinoline-2-carbonyl)benzenesulfonamide (3) (PDB code 4Z1J ), a novel series of 4-(1-aryl-3,4-dihydro-1H-isoquinolin-2-carbonyl)benzenesulfonamides (23-33) was designed. Specifically, our idea was to improve the selectivity toward druggable isoforms through the introduction of additional hydrophobic/hydrophilic functionalities. Among the synthesized and tested compounds, the (R,S)-4-(6,7-dihydroxy-1-phenyl-3,4-tetrahydroisoquinoline-1H-2-carbonyl)benzenesulfonamide (30) exhibited a remarkable inhibition for the brain-expressed hCA VII (Ki = 0...
May 9, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28445001/inhibition-properties-of-some-flavonoids-on-carbonic-anhydrase-i-and-ii-isoenzymes-purified-from-human-erythrocytes
#12
Zübeyir Huyut, Şükrü Beydemir, İlhami Gülçin
Carbonic anhydrases (CAs, E.C.4.2.1.1) play a critical role in many important physiological events and treatment of some diseases. Flavonoids or phenolic compounds have been discovered as novel CAs inhibitors instead of the traditional sulfonamides, with different binding to CAs, pro-drug activities, and new inhibition mechanisms. Here, we investigated the inhibition effects of some flavonoids including malvin, callistephin, oenin, pelargonin, silychristin, and 1-(4-methoxyphenyl)-2-methyl-3-nitro-1-H-indol-6-ol (ID-8) against hCA I and II, which purified from human erythrocytes by affinity column chromatography...
April 26, 2017: Journal of Biochemical and Molecular Toxicology
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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