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Carbonic anhydrase 3

Srinivas Angapelly, P V Sri Ramya, Rohini Sodhi, Andrea Angeli, Krishnan Rangan, Narayana Nagesh, Claudiu T Supuran, Mohammed Arifuddin
A practical and transition metal-free one-pot domino synthesis of diversified (1,3,4-oxadiazol-2-yl)anilines has been developed employing isatins and hydrazides as the starting materials, in the presence of molecular iodine. The prominent feature of this domino process involves consecutive condensation, hydrolytic ring cleavage, and an intramolecular decarboxylation, in a one-pot process that leads to the oxidative formation of a C-O bond. Fluorescence properties of some of the representative molecules obtained in this way were studied...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
Caoileann H Murphy, Mahalakshmi Shankaran, Tyler A Churchward-Venne, Cameron J Mitchell, Nathan M Kolar, Louise M Burke, John A Hawley, Amira Kassis, Leonidas G Karagounis, Kelvin Li, Chelsea King, Marc Hellerstein, Stuart M Phillips
We determined how the pattern of protein intake and resistance training (RT) influenced longer-term (2-wk) integrated myofibrillar protein synthesis (MyoPS) during energy restriction (ER). MyoPS and proteome kinetics were measured during 2-wk of ER alone and 2-wk of ER plus RT (ER + RT) in overweight/obese older men. Participants were randomized to consume dietary protein in a balanced (BAL: 25% daily protein/meal x 4 meals) or skewed (SKEW: 7:17:72:4% daily protein/meal) pattern (n = 10/group). Participants ingested D2 O during the consecutive 2-wk periods, and skeletal muscle biopsies and serum were obtained at the beginning and conclusion of ER and ER + RT...
March 12, 2018: Journal of Physiology
K Koruza, B Lafumat, Á Végvári, W Knecht, S Z Fisher
Deuterated proteins and other bio-derived molecules are important for NMR spectroscopy, neutron reflectometry, small angle neutron scattering, and neutron protein crystallography. In the current study we optimized expression media and cell culture conditions to produce high levels of 3 different deuterated human carbonic anhydrases (hCAs). The labeled hCAs were then characterized and tested for deuterium incorporation by mass spectrometry (MS), temperature stability, and propensity to crystallize. The results show that is possible to get very good yields (>10 mg of pure protein per liter of cell culture under deuterated conditions) and that protein solubility is unaffected at the crystallization concentrations tested...
March 7, 2018: Archives of Biochemistry and Biophysics
P Wang, J H Zeng, L Tang
Objective: To retrospectively investigate the medication structures and characteristics among the outpatients diagnosed with glaucoma at West China Hospital of Sichuan University in 2015. Methods: Based on retrospective study method, the data of glaucoma patients (6 236 people, and 13 693 person-times) who received medication at the outpatient department of West China Hospital in 2015 were collected from hospital information system, such data include date, doctor's advice date, doctor's advice ID, diagnosis, western medicine fee, Chinese medicine fee, etc...
March 11, 2018: [Zhonghua Yan Ke za Zhi] Chinese Journal of Ophthalmology
Anna Pellat, Chantal Dreyer, Camille Couffignal, Thomas Walter, Catherine Lombard-Bohas, Patricia Niccoli, Jean François Seitz, Olivia Hentic, Thierry André, Romain Coriat, Sandrine Faivre, Magaly Zappa, Philippe Ruszniewski, Nicolas Pote, Anne Couvelard, Eric Raymond
BACKGROUND/AIMS: Angiogenesis is extensively developed in well-differentiated pancreatic neuroendocrine tumours (PanNET) where sunitinib was shown to prolong progression-free survival, leading to nationwide approval. However, clinical experience in patients with grade 3 gastroenteropancreatic neuroendocrine neoplasms (GEPNEN-G3) remains limited. This prospective phase II trial evaluated potential predictive biomarkers of sunitinib activity in patients with advanced GEPNEN-G3. METHODS: Sunitinib was given at a dose of 37...
March 8, 2018: Neuroendocrinology
Ehsan Rahimy, Gui-Shuang Ying, Wei Pan, Jason Hsu
PURPOSE: To evaluate the effect of intraocular pressure-lowering medications on treatment outcomes in the Comparison of AMD Treatments Trials. METHODS: Secondary analysis of Comparison of AMD Treatments Trials data. Medication logs were reviewed for continuous 2-year use of agents that increased aqueous outflow (Group A: topical prostaglandins) or suppressed aqueous production (Group B: topical beta blockers and carbonic anhydrase inhibitors). Eyes were excluded if mixed-mechanism intraocular pressure-lowering agents or medications from more than one group were taken...
March 5, 2018: Retina
Sezen Karakus, Alan N Baer, Devika Agrawal, Merve Gurakar, Robert W Massof, Esen K Akpek
PURPOSE: To investigate the value of 3 novel autoantibodies [salivary protein 1 (SP1), carbonic anhydrase 6 (CA6), and parotid secretory protein (PSP)] in differentiating Sjögren's syndrome (SS)-related dry eye from non-SS dry eye. METHODS: Forty-six dry eye patients with SS (SS dry eye), 14 dry eye patients without SS (non-SS dry eye), and 25 controls were included. The 2012 American College of Rheumatology classification criteria were used for the diagnosis of SS...
April 2018: Cornea
Alessio Nocentini, Davide Moi, Gianfranco Balboni, Severo Salvadori, Valentina Onnis, Claudiu T Supuran
Herein we report the synthesis of a new series of aromatic sulfamates designed considering the sulfonamide COX-2 selective inhibitors celecoxib and valdecoxib as lead compounds. These latter were shown to possess important human carbonic anhydrase (CA, EC inhibitory properties, with the inhibition of the tumor-associated isoform hCA IX likely being co-responsible of the celecoxib anti-tumor effects. Bioisosteric substitution of the pyrazole or isoxazole rings from these drugs with the pyrazoline one was considered owing to the multiple biological activities ascribed to this latter heterocycle and paired with the replacement of the sulfonamide of celecoxib and valdecoxib with its equally potent bioisoster sulfamate...
February 23, 2018: Bioorganic Chemistry
Norihiko Masuda, Osamu Ogawa, Meyeon Park, Alvin Y Liu, Steve Goodison, Yunfeng Dai, Landon Kozai, Hideki Furuya, Yair Lotan, Charles J Rosser, Takashi Kobayashi
A 10-plex urine-based bladder cancer (BCa) diagnostic signature has the potential to non-invasively predict the presence of BCa in at-risk patients, as reported in various case-control studies. The present meta-analysis was performed to re-evaluate and demonstrate the robustness and consistency of the diagnostic utility of the 10-plex urine-based diagnostic assay. We re-analyzed primary data collected in five previously published case-control studies on the 10-plex diagnostic assay. Studies reported the sensitivity and specificity of ten urinary protein biomarkers for the detection of BCa, including interleukin 8, matrix metalloproteinases 9 and 10, angiogenin, apolipoprotein E, syndecan 1, alpha-1 antitrypsin, plasminogen activator inhibitor-1, carbonic anhydrase 9, and vascular endothelial growth factor A...
January 23, 2018: Oncotarget
Nabih Lolak, Suleyman Akocak, Silvia Bua, Murat Koca, Claudiu T Supuran
A series of novel 1,3-diaryltriazene-substituted sulfonamides was synthesized by reaction of diazonium salt of 4-amino benzenesulfonamide with substituted aromatic amines. The obtained 1,3-diaryltriazene-substituted sulfonamides were investigated as inhibitors of four selected human carbonic anhydrase (CA, EC isoforms (hCA I, hCA II, hCA VII and hCA IX) are involved in various diseases such as glaucoma, epilepsy, retinitis pigmentosa, cancer, obesity, etc. All these sulfonamides were found to be potent inhibitors of the cytosolic isoform hCA II with low nanomolar to sub-nanomolar Ki s in the range of 0...
February 15, 2018: Bioorganic Chemistry
Parham Taslimi, Cuneyt Caglayan, Vagif Farzaliyev, Oruj Nabiyev, Afsun Sujayev, Fikret Turkan, Ruya Kaya, İlhami Gulçin
During this investigation, N,N'-bis-azidomethylamines, N,N'-bis-cyanomethylamine, new alkoxymethylamine and chiral derivatives, which are considered to be a new generation of multifunctional compounds, were synthesized, functional properties were investigated, and anticholinergic and antidiabetic properties of those compounds were studied through the laboratory tests, and it was approved that they contain physiologically active compounds rather than analogues. Novel N-bis-cyanomethylamine and alkoxymethylamine derivatives were effective inhibitors of the α-glycosidase, cytosolic carbonic anhydrase I and II isoforms, butyrylcholinesterase (BChE), and acetylcholinesterase (AChE) with Ki values in the range of 0...
February 19, 2018: Journal of Biochemical and Molecular Toxicology
Fikret Türkan, Zübeyir Huyut, Parham Taslimi, İlhami Gülçin
In this paper, the in vivo effects of some antibiotics including cefazolin, cefuroxime, and cefoperazon, on the activity of the carbonic anhydrase enzyme (CA) in heart, brain, eye, liver, and kidney tissues of rats were evaluated. For this purpose, 16 different groups, which each containing six rats (n = 6), were formed (control group, cefazolin groups, cefuroxime groups, and cefoperazon groups). The rats were necropsied 60 min after the intraperitoneal injection of the chemicals into the rats. The CA activities were measured for each tissue using esterase activity methods...
February 19, 2018: Journal of Biochemical and Molecular Toxicology
Arjun L Khandare, Vakdevi Validandi, Naveen Boiroju
The present study aimed to determine the serum trace elements (copper (Cu), zinc (Zn), calcium (Ca), magnesium (Mg)) along with erythrocyte carbonic anhydrase (CA) activity and effect of intervention with safe drinking water for 5 years in the school children of fluorosis endemic area. For this purpose, three categories of villages were selected based on drinking water fluoride (F): Category I (control, F = 1.68 mg/L), category II (affected F = 3.77 mg/L), and category III (intervention village) where initial drinking water F was 4...
February 17, 2018: Biological Trace Element Research
Brandon Menke, Alex Walters, John F Payne
An 11-year-old boy presented for central vision blurring in each eye. Visual acuity was 20/80 and examination revealed spoke-wheel foveal schisis and peripheral elevated diaphanous inner retina in each eye. Spectral-domain optical coherence tomography showed inner-retinal, flat-topped cysts in each eye. Electrophysiologic testing was refused, but a clinical diagnosis of X-linked retinoschisis was made. Three months after topical dorzolamide (Trusopt; Santen Pharmaceutical, Osaka, Japan) was started, the macular cysts worsened significantly...
February 1, 2018: Ophthalmic Surgery, Lasers & Imaging Retina
Shams-Ul Mahmood, Aamer Saeed, Sivia Bua, Alessio Nocentini, Paola Gratteri, Claudiu T Supuran
A series of iminothiazolidinone-sulfonamide hybrids (2a-k) was synthesized by heterocyclization of sulfanilamide thioureas with methyl bromoacetate and characterized by spectroscopic techniques, mass and elemental analysis. The synthesized derivatives were screened against four relevant human (h) isoforms of carbonic anydrases (CAs, EC I, II, IV and IX. These enzymes are involved in a variety of diseases, including glaucoma, retinitis pigmentosa, epilepsy, arthritis, and tumors. Derivatives 2a-2k exhibited the best inhibitory activity against the cytosolyc hCA II (KIs are reaching the sub-nanomolar range, 0...
January 31, 2018: Bioorganic Chemistry
Alessio Nocentini, Davide Moi, Gianfranco Balboni, Valentina Onnis, Claudiu T Supuran
Herein we report the synthesis of a new series of aromatic sulfamates investigated for the inhibition of four human (h) isoforms of zinc enzyme carbonic anhydrase (CA, EC, hCA I, II, IV, and IX. The reported derivatives, obtained by a sulfamoylation reaction of the corresponding phenolic precursors, bear arylthiazolin-4-one moieties as spacers between the benzenesulfamate fragment which binds the zinc ion from the active site, and the tail of the inhibitor. Thiazolin-4-ones are biologically privileged scaffolds, endowed with versatile biological activity, such as an anti-proliferative action...
January 27, 2018: Bioorganic Chemistry
Alessandro Bonardi, Matteo Falsini, Daniela Catarzi, Flavia Varano, Lorenzo Di Cesare Mannelli, Barbara Tenci, Carla Ghelardini, Andrea Angeli, Claudiu T Supuran, Vittoria Colotta
Human carbonic anhydrases (hCAs, EC IX and XII are overexpressed in a wide variety of cancers and are considered available drug targets for anti-tumor therapy since their inhibition has been shown to reduce tumor growth and metastasis. A set of coumarin derivatives (1-10) and several 1-aryl and 2-aryl-substituted chromeno[4,3-c]pyrazol-4-ones (11-37) and pyrano[4,3-c]pyrazol-4-ones (38-39) were synthesized and tested against the tumor-associated hCAs IX and XII and the cytosolic isoforms hCAs I and II...
January 12, 2018: European Journal of Medicinal Chemistry
Michael Brannen, Kathleen M Gilmour
Rainbow trout (Oncorhynchus mykiss) exposed to acid-base challenges activate branchial mechanisms for the excretion of acid-base equivalents. Current models of branchial acid-base excretion in freshwater rainbow trout propose two main ionocyte types; the peanut lectin agglutinin-positive (PNA+) mitochondrion-rich cell or ionocyte is believed to secrete HCO3- in exchange for Cl-, whereas H+ secretion is thought to occur across PNA- ionocytes in exchange for Na+ Both HCO3- and H+ are supplied by intracellular hydration of CO2 catalyzed by cytosolic carbonic anhydrase (CAc)...
January 29, 2018: Journal of Experimental Biology
Otzem Chassid, Irena Epstein, Adi Sharabi-Nov, Joseph Pikkel
We describe the prevalence and treatment of glaucoma in a Muslim Arab population in Israel. Based on the medical records of 15 122 persons, the overall prevalence of glaucoma was 3.9%. Prevalence rates of primary open angle glaucoma (POAG) and primary angle-closure glaucoma (PACG) were 3.0% and 0.42%, respectively. Prevalence rates of women were 135% that of men considering all types of glaucoma, 143% for POAG, and 96% for PACG. Prostaglandin analogs and beta blockers, alone or combined with carbonic anhydrase inhibitors, were the preferred medications...
2018: International Journal of Ophthalmology
Daniela Vullo, Ronny Lehneck, Stefanie Pöggeler, Claudiu T Supuran
The two β-carbonic anhydrases (CAs, EC recently cloned and purified from the ascomycete fungus Sordaria macrospora, CAS1 and CAS2, were investigated for their inhibition with a panel of 39 aromatic, heterocyclic, and aliphatic sulfonamides and one sulfamate, many of which are clinically used agents. CAS1 was efficiently inhibited by tosylamide, 3-fluorosulfanilamide, and 3-chlorosulfanilamide (KIs in the range of 43.2-79.6 nM), whereas acetazolamide, methazolamide, topiramate, ethoxzolamide, dorzolamide, and brinzolamide were medium potency inhibitors (KIs in the range of 360-445 nM)...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
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