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Carbonic anhydrase 3

Cem Yamali, Halise Inci Gul, Abdulilah Ece, Parham Taslimi, Ilhami Gulcin
In the present study, 4-[5-aryl-3-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl] benzenesulfonamides were synthesized and inhibition effects on AChE, hCA I and hCA II were evaluated. Ki values of the compounds towards hCA I were in the range of 24.2±4.6-49.8±12.8 nM while they were in the range of 37.3±9.0-65.3±16.7 nM towards hCA II. Ki values of the Acetazolamide were 282.1±19.7 nM and 103.60±27.6 nM towards both isoenzymes, respectively. The compounds inhibited AChE with Ki in the range of 22.7±10.3-109...
November 16, 2017: Chemical Biology & Drug Design
Umit M Kocyigit, Yakup Budak, Fikret Eligüzel, Parham Taslimi, Deryanur Kılıç, İlhami Gulçin, Mustafa Ceylan
In the present study, human carbonic anhydrase (hCA) enzyme was purified and characterized from fresh blood human red cells by Sepharose-4B-l-tyrosine-sulfanilamide affinity gel chromatography. Secondly, a series of new tetrabromo chalcone derivatives containing 4,7-methanoisoindol-1,3-dione (2a-i) were synthesized from the addition of Br2 to related chalcone derivatives (1a-i). The structures of the new molecules (2a-i) were confirmed by means of (1) H NMR, (13) C NMR and elemental analysis. Finally, the inhibitory effects of 2a-i on CA activities were investigated using the esterase method under in vitro conditions...
November 14, 2017: Archiv der Pharmazie
Betul Kacar, Lionel Guy, Eric Smith, John Baross
Two datasets, the geologic record and the genetic content of extant organisms, provide complementary insights into the history of how key molecular components have shaped or driven global environmental and macroevolutionary trends. Changes in global physico-chemical modes over time are thought to be a consistent feature of this relationship between Earth and life, as life is thought to have been optimizing protein functions for the entirety of its approximately 3.8 billion years of history on the Earth. Organismal survival depends on how well critical genetic and metabolic components can adapt to their environments, reflecting an ability to optimize efficiently to changing conditions...
December 28, 2017: Philosophical Transactions. Series A, Mathematical, Physical, and Engineering Sciences
Nilufer Bulut, Umit M Kocyigit, Ibrahim H Gecibesler, Taner Dastan, Huseyin Karci, Parham Taslimi, Sevgi Durna Dastan, Ilhami Gulcin, Ahmet Cetin
Some novel derivatives of thiosemicarbazide and 1,2,4-triazole-3-thiol were synthesized and evaluated for their biological activities. The title compounds were prepared starting from readily available pyridine-2,5-dicarboxylic acid. The reaction carboxylic acid with absolute ethanol afforded the corresponding dimethyl pyridine-2,5-dicarboxylate (1). The reaction of dimethyl-2,5-pyridinedicarboxylate (1) with hydrazine hydrate good yielded pyridine-2,5-dicarbohydrazide (2). Refluxing compound 2 with alkyl/aryl isothiocyanate derivatives for 3-8 h afforded 1,4-disubstituted thiosemicarbazides (3a-e)...
November 13, 2017: Journal of Biochemical and Molecular Toxicology
Daniela Vullo, Sonia Del Prete, Sameh M Osman, Fatmah A S Alasmary, Zeid AlOthman, William A Donald, Clemente Capasso, Claudiu T Supuran
The β-class carbonic anhydrase (CA, EC from the pathogenic bacterium Burkholderia pseudomallei, BpsCAβ, that is responsible for the tropical disease melioidosis was investigated for its activation with natural and non-natural amino acids and amines. Previously, the γ-CA from this bacterium has been investigated with the same library of 19 amines/amino acids, which show very potent activating effects on both enzymes. The most effective BpsCAβ activators were L- and D-DOPA, L- and D-Trp, L-Tyr, 4-amino-L-Phe, histamine, dopamine, serotonin, 2-pyridyl-methylamine, 1-(2-aminoethyl)-piperazine and L-adrenaline with KAs of 0...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
M Connolly, J Shand, M Kinnin, I Menown, M J Kurth, J Lamont, D Mc Eneaney
OBJECTIVES: To assess the prognostic value of biomarkers of myocardial injury following elective percutaneous coronary intervention (PCI). BACKGROUND: Type 4a myocardial infarction (MI) occurs when myocardial injury is combined with either symptoms suggestive of myocardial ischaemia, new left bundle branch block, angiographic loss of patency of a major artery or imaging suggestive of new loss of myocardium. Myocardial injury is defined as a rise of > 5 x 99th upper reference limit (URL) of 14ng/L (i...
October 10, 2017: QJM: Monthly Journal of the Association of Physicians
Mohammad Aasif Dar, Wahiduzzaman, Asimul Islam, Md Imtaiyaz Hassan, Faizan Ahmad
Owing to the urine concentrating mechanism of kidney cells, urea concentration is very high (3.0-5.0M) in mammalian kidneys which may denature many kidney proteins. Methylamines are known to counteract the deleterious effects of urea on structure, stability and function of proteins at 2:1 molar ratio of urea to methylamines. It is known that mammalian kidney cells also contain stabilizing osmolytes, non-methylamines (myo-inositol and sorbitol). A question arises: Do these non-methylmine osmolytes have ability to counteract the deleterious effects of urea on kidney proteins? To answer this question, we took two kidney proteins, namely, sheep serum albumin and Human carbonic anhydrase II...
October 10, 2017: International Journal of Biological Macromolecules
Eun-Gyung Mun, Hee-Sook Sohn, Mi-Sun Kim, Youn-Soo Cha
BACKGROUND/OBJECTIVES: Although Korean fermented foods contain large amounts of salt, which is known to exacerbate health problems, these foods still have beneficial effects such as anti-hypertension, anti-cancer, and anti-colitis properties. We hypothesized that ganjang may have different effects on blood pressure compared to same concentrations of salt. MATERIALS/METHODS: Sprague-Dawley rats were divided into control (CT), NaCl (NC), and ganjang (GJ) groups and orally administered with 8% NaCl concentration for 9 weeks...
October 2017: Nutrition Research and Practice
N N Rudenko, D V Vetoshkina, T P Fedorchuk, B N Ivanov
Changes in expression levels of genes encoding carbonic anhydrases α-CA1, α-CA2, α-CA4, β-CA1, β-CA2, β-CA3, β-CA4, β-CA5, and β-CA6 in Arabidopsis thaliana leaves after light increase from 80 to 400 µmol PAR quanta·m(-2)·s(-1) were investigated under short day (8 h) and long day (16 h) photoperiods. The expression of two forms of the gene, At3g01500.2 and At3g01500.3, encoding the most abundant carbonic anhydrase of leaves, β-CA1, situated in chloroplast stroma, was found. The content of At3g01500...
September 2017: Biochemistry. Biokhimii︠a︡
Maj Rabjerg
Kidney cancer (Renal Cell Carcinoma (RCC)) is one of the most deadly malignancies due to frequent late diagnosis and poor treatment options. Histologically, RCC embraces a wide variety of different subtypes with the clear cell variant (ccRCC) being the most common, accounting for 75-90% of all RCCs. At present, the surveillance protocols for follow-up of RCC patients after radical nephrectomy are based on the American Joint Committee on Cancers (AJCC) pathological tumor-node-metastasis (TNM) classification system...
October 2017: Danish Medical Journal
Sylvie Berthier, Josiane Arnaud, Pierre Champelovier, Edwige Col, Catherine Garrel, Cécile Cottet, Jean Boutonnat, François Laporte, Patrice Faure, Florence Hazane-Puch
Glioblastoma (GBM) is the most common type of primary tumor of the central nervous system with a poor prognosis, needing the development of new therapeutic drugs. Few studies focused on sodium selenite (SS) effects in cancer cells cultured as multicellular tumor spheroids (MCTS or 3D) closer to in vivo tumor. We investigated SS anticancer effects in three human GBM cell lines cultured in 3D: LN229, U87 (O(6)-methyguanine-DNA-methyltransferase (MGMT) negative) and T98G (MGMT positive). SS absorption was evaluated and the cytotoxicity of SS and temozolomide (TMZ), the standard drug used against GBM, were compared...
December 2017: Journal of Trace Elements in Medicine and Biology
P V Sri Ramya, Srinivas Angapelly, Andrea Angeli, Chander Singh Digwal, Mohammed Arifuddin, Bathini Nagendra Babu, Claudiu T Supuran, Ahmed Kamal
A series of curcumin inspired sulfonamide derivatives was prepared from various chalcones and 4-sulfamoyl benzaldehyde via Claisen-Schmidt condensation. All new compounds were assayed as inhibitors of four human isoforms of the metalloenzyme carbonic anhydrase (hCA, EC isoforms hCA I, II, IX and XII. Interesting inhibitory activities were observed against all these isoforms. hCA I, an isoform involved in several eye diseases was inhibited moderately with KIs in the range of 191.8-904.2 nM, hCA II, an antiglaucoma drug target was highly inhibited by the new sulfonamides, with KIs in the range of 0...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
Joanna Matysiak, Alicja Skrzypek, Paweł Tarasiuk, Mariusz Mojzych
The QSAR models for a set of pyrazolo[4,3-e][1,2,4]triazines incorporating benzenesulfonamide moiety combined directly with the heterocyclic ring or by NH linkage were generated. The inhibitory potency of compounds against human carbonic anhydrase isoforms IX and XII and antiproliferative activity against human MCF-7 cells were used as the dependent variables. The Codessa pro software was used for the descriptors calculation and the Best Multi-Linear Regression (BMLR) algorithm was employed to build the QSAR models...
September 21, 2017: Computational Biology and Chemistry
Lianhua Zhu, Yanli Guo, Luofu Wang, Xiaozhou Fan, Xingyu Xiong, Kejing Fang, Dan Xu
BACKGROUND: Ultrasound molecular imaging is a novel diagnostic approach for tumors, whose key link is the construction of targeted ultrasound contrast agents. However, available targeted ultrasound contrast agents for molecular imaging of tumors are only achieving imaging in blood pool or one type tumor. No targeted ultrasound contrast agents have realized targeted ultrasound molecular imaging of tumor parenchymal cells in a variety of solid tumors so far. Carbonic anhydrase IX (CAIX) is highly expressed on cell membranes of various malignant solid tumors, so it's a good target for ultrasound molecular imaging...
September 29, 2017: Journal of Nanobiotechnology
Alba Sánchez-Mascuñano, Cristina Masuet-Aumatell, Sergio Morchón-Ramos, Josep M Ramon
OBJECTIVES: The aim of this study is to analyse the relationship between smoking and altitude mountain sickness in a cohort of travellers to 2500 metres above sea level (masl) or higher. SETTING: Travel Health Clinic at the Hospital Universitari de Bellvitge, in Barcelona, Spain. PARTICIPANTS: A total of 302 adults seeking medical advice at the travel clinic, between July 2012 and August 2014, before travelling to 2500 masl or above, who agreed to participate in the study and to be contacted after the trip were included...
September 24, 2017: BMJ Open
Srinivas Angapelly, P V Sri Ramya, Andrea Angeli, Claudiu T Supuran, Mohammed Arifuddin
A series of sulfocoumarin-, coumarin-, and 4-sulfamoylphenyl-bearing indazole-3-carboxamide hybrids were synthesized and investigated as inhibitors of the human carbonic anhydrase (hCA, EC isoforms I and II (cytosolic isozymes), as well as hCA IX and XII (transmembrane, tumor-associated enzymes). Compounds 6 a-g (amide derivatives) and 7 a-h (triazoles) act as "prodrugs", and their hydrolysis products are the de facto CA inhibitors. These compounds displayed sub-micromolar to high-nanomolar inhibitory activity against hCA isoforms IX and XII, which were recently validated as antitumor drug targets...
October 9, 2017: ChemMedChem
Ailian Du, Shiqian Huang, Xiaonan Zhao, Kuan Feng, Shuangyan Zhang, Jiefang Huang, Xiang Miao, Fulvio Baggi, Rennolds S Ostrom, Yanyun Zhang, Xiangjun Chen, Congfeng Xu
Myasthenia gravis is an autoimmune disorder of the neuromuscular junction manifested as fatigable muscle weakness, which is typically caused by pathogenic autoantibodies against postsynaptic CHRN/AChR (cholinergic receptor nicotinic) in the endplate of skeletal muscle. Our previous studies have identified CA3 (carbonic anhydrase 3) as a specific protein insufficient in skeletal muscle from myasthenia gravis patients. In this study, we investigated the underlying mechanism of how CA3 insufficiency might contribute to myasthenia gravis...
September 21, 2017: Autophagy
Marthe Aimée Tchuente Tchuenmogne, Thierry Ngouana Kammalac, Sebastian Gohlke, Rufin Marie Toghueo Kouipou, Abdulselam Aslan, Muslum Kuzu, Veysel Comakli, Ramazan Demirdag, Silvère Augustin Ngouela, Etienne Tsamo, Norbert Sewald, Bruno Ndjakou Lenta, Fabrice Fekam Boyom
Background: Pathogenic yeasts resistance to current drugs emphasizes the need for new, safe, and cost-effective drugs. Also, new inhibitors are needed to control the effects of enzymes that are implicated in metabolic dysfunctions such as cancer, obesity, and epilepsy. Methods: The anti-yeast extract from Terminalia mantaly (Combretaceae) was fractionated and the structures of the isolated compounds established by means of spectroscopic analysis and comparison with literature data. Activity was assessed against Candida albicans, C...
January 24, 2017: Medicines (Basel, Switzerland)
Jennifer L Bryant, Roben G Gieling, Suzanne L Meredith, Tiffany-Jayne Allen, Leanne Walker, Brian A Telfer, Claudiu T Supuran, Kaye J Williams, Anne White
Small cell lung cancer (SCLC) has an extremely poor prognosis and methods of improving chemotherapeutic intervention are much sought after. A promising approach lies in inhibiting the tumour-associated enzyme, carbonic anhydrase IX (CA IX), which supports tumour cell survival. The aim of this study was to assess the potential of CA IX inhibition using 4-(3'-(3″,5″-dimethylphenyl)ureido)phenyl sulfamate (S4), for the treatment of human SCLC alone and in combination with cisplatin chemotherapy. Treating SCLC cell lines (DMS 79 and COR-L24) with 100 µM S4 reduced viability in vitro and enhanced cell death when combined with 7 µM cisplatin, most prominently under hypoxic conditions (0...
September 14, 2017: International Journal of Cancer. Journal International du Cancer
Sanjith Aaron, Anupriya Arthur, A T Prabakhar, Pavitra Mannam, N K Shyamkumar, Sunithi Mani, Vivek Mathew, Jeyanthi Peter, Ajith Sivadasan, Anika Alexander, M Karthik, Rohith Ninan Benjamin, Mathew Alexander
Visual impairment can complicate cerebral venous thrombosis (CVT). Here, we describe the various pathophysiological mechanisms and treatments available. A retrospective chart review of all patients treated for CVT in a large quaternary teaching hospital was done, and cases with visual impairment due to CVT were identified. The various mechanisms causing visual impairment in CVT were (1) raised intracranial pressure (ICP) caused by venous thrombosis without venous infarcts resulting in a benign intracranial hypertension-like presentation of CVT, (2) venous infarcts involving the occipital cortex, (3) raised ICP following the development of a secondary dural arteriovenous (AV) fistula, and (4) arterial occipital infarcts due to posterior cerebral artery compression secondary to herniation in large venous infarcts...
July 2017: Annals of Indian Academy of Neurology
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