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Carbonic anhydrase 3

Halise Inci Gul, Ebru Mete, Parham Taslimi, Ilhami Gulcin, Claudiu T Supuran
4-(3-(4-Substituted-phenyl)-5-phenyl-4,5-dihydro-1H-pyrazol-1-yl) benzenesulfonamides (9-16) were successfully synthesized and their chemical structures were confirmed by (1)H NMR, (13)C NMR, and HRMS spectra. Carbonic anhydrase I and II inhibitory effects of the compounds were investigated. Ki values of the compounds were in the range of 316.7 ± 9.6-533.1 ± 187.8 nM towards hCA I and 412.5 ± 115.4-624.6 ± 168.2 nM towards hCA II isoenzymes. While Ki values of the reference compound Acetazolamide were 278...
October 24, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Halise Inci Gul, Ebru Mete, Sakip Emre Eren, Hiroshi Sakagami, Cem Yamali, Claudiu T Supuran
In this study, 4-[3-(4-hydroxyphenyl)-5-aryl-4,5-dihydro-pyrazol-1-yl]benzenesulfonamide (1-9) types compounds were synthesized and their chemical structures were confirmed by (1)H NMR, (13)C NMR and HRMS spectra. Cytotoxic and carbonic anhydrase (CA) inhibitory effects of the compounds were investigated. Cytotoxicity experiments pointed out that compound 4, (4-[5-(4-chlorophenyl)-3-(4-hydroxyphenyl)-4,5-dihydro-pyrazol-1-yl]benzenesulfonamide), exerting the highest tumor selectivity (TS) and potency selectivity expression (PSE) values, can be considered as a lead compound of this study in terms of development of novel anticancer agents...
October 23, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Jovana Trifunović, Vladan Borčić, Momir Mikov
Some biological properties of bile acids and their oxo derivatives have not been sufficiently investigated, although the interest for bile acids as signaling molecules is rising. The aim of this work was to evaluate physico-chemical parametar b (slope) that represents lipophilicity of the examined molecules and to investigate interactions of bile acids with carbonic anhydrase I, II, androgen receptor and CYP450s. 13 candidates were investigated using normal phase thin layer chromatography in two solvent systems...
October 14, 2016: Biomedical Chromatography: BMC
Mingchang Li, Wei Wang, Haojian Mai, Xinmu Zhang, Jian Wang, Yufeng Gao, Yuefei Wang, Gang Deng, Ling Gao, Shuanhu Zhou, Qianxue Chen, Xin Wang
Subarachnoid hemorrhage (SAH) results in significant nerve dysfunction, such as hemiplegia, mood disorders, cognitive and memory impairment. Currently, no clear measures can reduce brain nerve damage. The study of brain nerve protection after SAH is of great significance. We aim to evaluate the protective effects and the possible mechanism of methazolamide in C57BL/6J SAH animal model in vivo and in blood-induced primary cortical neuron (PCNs) cellular model of SAH in vitro. We demonstrate that methazolamide accelerates the recovery of neurological damage, effectively relieves cerebral edema, and improves cognitive function in SAH mice as well as offers neuroprotection in blood- or hemoglobin-treated PCNs and partially restores normal neuronal morphology...
October 12, 2016: Scientific Reports
Vaida Linkuvienė, Georg Krainer, Wen-Yih Chen, Daumantas Matulis
Isothermal titration calorimetry (ITC) is one of the most robust label- and immobilization-free techniques used to measure protein - small molecule interactions in drug design for the simultaneous determination of the binding affinity (ΔG) and the enthalpy (ΔH), both of which are important parameters for structure-thermodynamics correlations. It is important to evaluate the precision of the method and of various ITC instrument models by performing a single well-characterized reaction. The binding between carbonic anhydrase II and acetazolamide was measured by four ITC instruments - PEAQ-ITC, iTC200, VP-ITC, and MCS-ITC and the standard deviation of ΔG and ΔH was determined...
December 15, 2016: Analytical Biochemistry
Pia Viikilä, Antti J Kivelä, Harri Mustonen, Selja Koskensalo, Abdul Waheed, William S Sly, Jaromir Pastorek, Silvia Pastorekova, Seppo Parkkila, Caj Haglund
AIM: To investigate expression of four alpha-carbonic anhydrases (CAs) in colorectal carcinomas (CRC) and compare the results with patients' survival. METHODS: Colorectal carcinoma samples from 539 CRC patients and control tissues were arranged as tissue microarrays and analyzed with antibodies against CA II, CA VII, CA IX, and CA XII. Intensity and extent of staining were both scored from 0 to 3 in each sample. These enzyme expression levels were then correlated to patients' survival and clinicopathological parameters, which were tumor differentiation grade and stage, site of tumor, patients' age, and gender...
September 28, 2016: World Journal of Gastroenterology: WJG
Gap-Don Kim, Jin-Kyu Seo, Hyeon-Woong Yum, Jin-Yeon Jeong, Han-Sul Yang
The purpose of this study was to find discrimination markers for four major meat species such as beef, pork, chicken and duck. Myofibrillar and sarcoplasmic proteins isolated from each meat type were analyzed by one-dimensional gel electrophoresis and some proteins were identified through LC-MS/MS analysis. We confirmed that troponin I (TnI), enolase 3, l-lactate dehydrogenase (LDH) and triose-phosphate isomerase (TPI) could be useful markers for discrimination of mammals from poultry due to their different electrophoretic mobility...
February 15, 2017: Food Chemistry
Bruna Benso, Marcelo Franchin, Adna Prado Massarioli, Jonas Augusto Rizzato Paschoal, Severino Matias Alencar, Gilson Cesar Nobre Franco, Pedro Luiz Rosalen
Given their medical importance, natural products represent a tremendous source of drug discovery. The aim of this study was to investigate Malva sylvestris L. extract and fractions and their pharmacological activities followed by chemical identification. The aqueous fraction (AF) was identified as the bioactive fraction in the in vitro and in vivo assays. The AF controlled the neutrophil migration to the peritoneal cavity by 66%, inhibited the antiedematogenic activity by 58.8%, and controlled IL-1β cytokine expression by 54%...
2016: PloS One
Xiaoqi Lin
BACKGROUND: Clear cell papillary renal cell carcinoma (CCPRCC) shares some morphologic and immunohistochemical markers with clear cell RCC and papillary RCC. To the author's knowledge, its cytomorphology on fine-needle aspiration (FNA) or touch preparations (TPs) of core needle biopsy specimens has not been well delineated in the English language literature. METHODS: The FNA/TP cytomorphology of 7 retrieved cases was studied. RESULTS: The tumor cells were arranged in small nests (100%), 3-dimensional clusters (71%), papillary/tubular/acinar arrays (43%), and as single cells (57%)...
September 16, 2016: Cancer Cytopathology
Anoop Kumar, Arivarasu Natarajan Anbazhagan, Hayley P Coffing, Ishita Chatterjee, Shubha Priyamvada, Tarunmeet Gujral, Seema Saksena, Ravinder K Gill, Waddah A Alrefai, Alip Borthakur, Pradeep K Dudeja
Impaired absorption of electrolytes is a hallmark of diarrhea associated with inflammation or enteric infections. Intestinal epithelial luminal membrane NHE3 (Na(+)/H(+) exchanger 3) and DRA (Cl(-)/HCO3 (-) exchanger) play key roles in mediating electroneutral NaCl absorption. We have previously shown decreased NHE3 and DRA function in response to short-term infection with enteropathogenic E. coli (EPEC), a diarrheal pathogen. Recent studies have also shown substantial downregulation of DRA expression in diarrheal model of infection with Citrobacter rodentium, the mouse counterpart of EPEC...
September 15, 2016: American Journal of Physiology. Gastrointestinal and Liver Physiology
Rebecca C Lobo, Neil E Hubbard, Patrizia Damonte, Hidetoshi Mori, Zsófia Pénzváltó, Cindy Pham, Amanda L Koehne, Aiza C Go, Steve E Anderson, Peter M Cala, Alexander D Borowsky
Mechanisms for the progression of ductal carcinoma in situ (DCIS) to invasive breast carcinoma remain unclear. Previously we showed that the transition to invasiveness in the mammary intraepithelial neoplastic outgrowth (MINO) model of DCIS does not correlate with its serial acquisition of genetic mutations. We hypothesized instead that progression to invasiveness depends on a change in the microenvironment and that precancer cells might create a more tumor-permissive microenvironment secondary to changes in glucose uptake and metabolism...
2016: Frontiers in Cell and Developmental Biology
Cem Yamali, Halise Inci Gul, Hiroshi Sakagami, Claudiu T Supuran
Phenolic bis Mannich bases having the chemical structure of 1-[3,5-bis-aminomethyl-4-hydroxyphenyl]-3-(4-halogenophenyl)-2-propen-1-ones (1a-c, 2a-c, 3a-c) were synthesized (Numbers 1, 2, and 3 represent fluorine, chlorine, and bromine bearing compounds, respectively, while a, b, and c letters represent the compounds having piperidine, morpholine, and N-methyl piperazine) and their cytotoxic and carbonic anhydrase (CA, EC enzyme inhibitory effects were evaluated. Lead compounds should possess both marked cytotoxic potencies and selective toxicity for tumors...
September 4, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Lu Tang, Aijun Yao, Ming Yuan, Yetao Tang, Jian Liu, Xi Liu, Rongliang Qiu
Zinc (Zn) and cadmium (Cd) are two closely related chemical elements with very different biological roles in photosynthesis. Zinc plays unique biochemical functions in photosynthesis. Previous studies suggested that in some Zn/Cd hyperaccumulators, many steps in photosynthesis may be Cd tolerant or even Cd stimulated. Using RNA-seq data, we found not only that Cd and Zn both up-regulated the CA1 gene, which encodes a β class carbonic anhydrase (CA) in chloroplasts, but that a large number of other Zn up-regulated genes in the photosynthetic pathway were also significantly up-regulated by Cd in leaves of the Zn/Cd hyperaccumulator Sedum alfredii...
December 2016: Chemosphere
Abdur Rauf, Ghias Uddin, Muslam Raza, Seema Patel, Saud Bawazeer, Taibi Ben Hadda, Noor Jehan, Yahia Nasser Mabkhot, Ajmal Khan, Mohammad Mubarak
The dimeric napthoquione 5,8,4'-trihydroxy-1'-methoxy-6, 6'-dimethyl-7,3'-binaphtyl-1,4,5',8'-tetraone (1) was isolated from the chloroform fraction of Diospyros lotus extract. Compound 1 was screened for its inhibitory effects against four enzymes: urease, phosphodiesterase-I, carbonic anhydrase-II and α-chymotrypsin, and showed selective activity against urease enzyme with an IC50 value of 254.1 ± 3.82 μM as compared to the standard thiourea (IC50 = 21 ± 0.11 μM). Furthermore, in silico docking study was carried out to explain the molecular mechanism of compound 1 against the target receptor...
September 1, 2016: Natural Product Research
Kaan Kucukoglu, Fatih Oral, Tevfik Aydin, Cem Yamali, Oztekin Algul, Hiroshi Sakagami, Ilhami Gulcin, Claudiu T Supuran, Halise Inci Gul
A series of polymethoxylated-pyrazoline benzene sulfonamides were synthesized, investigated for their cytotoxic activities on tumor and non-tumor cell lines and inhibitory effects on carbonic anhydrase isoenzymes (hCA I and hCA II). Although tumor selectivity (TS) of the compounds were less than the reference compounds 5-Fluorouracil and Melphalan, trimethoxy derivatives 4, 5, and 6 were more selective than dimethoxy derivatives 2 and 3 as judged by the cytotoxicity assay with the cells both types originated from the gingival tissue...
August 31, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Claudiu T Supuran
Carbonic anhydrase IX (CA IX) is an enzyme overexpressed in many hypoxic tumors as a consequence of hypoxia inducible factor 1α (HIF-1α) transcription factor cascade. CA IX is a highly active catalyst for the conversion of CO2 to bicarbonate and protons, being involved in pH regulation, but also contributes to the acquisition of metastasic phenotypes and to chemoresistance with some widely used anticancer drugs. CA IX inhibition with small molecules or antibodies has profound antitumor/antimetastatic effects, and also depletes the number of cancer stem cells within the hypoxic niche, all factors crucial for new generation anticancer agents...
August 30, 2016: Expert Opinion on Therapeutic Patents
Imdat Aygul, Fatma Yaylaci Karahalil, Claudiu T Supuran
Polyphenols are important secondary products of plants with the potential to inhibit carbonic anhydrases. The aim of this study was to investigate the inhibition effects of various phenolic standards, honey, propolis, and pollen species on human carbonic anhydrase I and II. The inhibition values (IC50) of the phenolics (gallic acid, protocatechuic acid, quercetin, catechin, tannic acid, and chrysin) ranged from 0.009 to 0.32 μg/mL, tannic acid emerging as the best inhibitor. The inhibition values of three different types of honey, heather, rhododendron, and chestnut ranged between 2...
August 25, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Sian E Piret, Caroline M Gorvin, Anne Trinh, John Taylor, Stefano Lise, Jenny C Taylor, Peter R Ebeling, Rajesh V Thakker
The aim of this study was to identify the causative mutation in a family with an unusual presentation of autosomal dominant osteopetrosis (OPT), proximal renal tubular acidosis (RTA), renal stones, epilepsy, and blindness, a combination of features not previously reported. We undertook exome sequencing of one affected and one unaffected family member, followed by targeted analysis of known candidate genes to identify the causative mutation. This identified a missense mutation (c.643G>A; p.Gly215Arg) in the gene encoding the chloride/proton antiporter 7 (gene CLCN7, protein CLC-7), which was confirmed by amplification refractory mutation system (ARMS)-PCR, and to be present in the three available patients...
November 2016: American Journal of Medical Genetics. Part A
Javad Garousi, Hadis Honarvar, Ken G Andersson, Bogdan Mitran, Anna Orlova, Jos Buijs, John Löfblom, Fredrik Y Frejd, Vladimir Tolmachev
Overexpression of the enzyme carbonic anhydrase IX (CAIX) is documented for chronically hypoxic malignant tumors as well as for normoxic renal cell carcinoma. Radionuclide molecular imaging of CAIX would be useful for detection of hypoxic areas in malignant tumors, for patients' stratification of CAIX-targeted therapies and for discrimination of primary malignant and benign renal tumors. Earlier, we have reported feasibility of in vivo radionuclide based imaging of CAIX expressing tumors using Affibody molecules, small affinity proteins based on a non-immunoglobulin scaffold...
August 16, 2016: Molecular Pharmaceutics
Sian-Tai Liu, Jiun-Lin Horng, Po-Yen Chen, Pung-Pung Hwang, Li-Yih Lin
Ionocytes in the skin and gills of seawater (SW) teleosts are responsible for both salt and acid secretion. However, the mechanism through which ionocytes secrete acid is still unclear. Here, we hypothesized that apical Na(+)/H(+) exchangers (NHE2/3), carbonic anhydrase (CA2-like), and basolateral HCO3(-)/Cl(-) exchanger (AE1) are involved in acid secretion. In addition, the hypothesized involvement of basolateral AE1 suggested that acid secretion may be linked to Cl(-) secretion by ionocytes. The scanning ion-selective electrode technique (SIET) was used to measure H(+) and Cl(-) secretion by ionocytes in the skin of medaka larvae acclimated to SW...
2016: Scientific Reports
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