Carbonic Anhydrase II: A cytosolic carbonic anhydrase isoenzyme found widely distributed in cells of almost all tissues. Deficiencies of carbonic anhydrase II produce a syndrome characterized by OSTEOPETROSIS, renal tubular acidosis (ACIDOSIS, RENAL TUBULAR) and cerebral calcification. EC 4.2.1.-Carbonic Anhydrases: A family of zinc-containing enzymes that catalyze the reversible hydration of carbon dioxide. They play an important role in the transport of CARBON DIOXIDE from the tissues to the LUNG. EC 4.2.1.1.Carbonic Anhydrase Inhibitors: A class of compounds that reduces the secretion of H+ ions by the proximal kidney tubule through inhibition of CARBONIC ANHYDRASES.Carbonic Anhydrase III: A cytosolic carbonic anhydrase isoenzyme primarily expressed in skeletal muscle (MUSCLES, SKELETAL). EC 4.2.1.-Ethoxzolamide: A carbonic anhydrase inhibitor used as diuretic and in glaucoma. It may cause hypokalemia.Acetazolamide: One of the CARBONIC ANHYDRASE INHIBITORS that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337)Carbonic Anhydrase I: A cytosolic carbonic anhydrase isoenzyme primarily expressed in ERYTHROCYTES, vascular endothelial cells, and the gastrointestinal mucosa. EC 4.2.1.-Carbonic Anhydrase IV: A membrane-bound carbonic anhydrase found in lung capillaries and kidney.Methazolamide: A carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma.Acidosis, Renal Tubular: A group of genetic disorders of the KIDNEY TUBULES characterized by the accumulation of metabolically produced acids with elevated plasma chloride, hyperchloremic metabolic ACIDOSIS. Defective renal acidification of URINE (proximal tubules) or low renal acid excretion (distal tubules) can lead to complications such as HYPOKALEMIA, hypercalcinuria with NEPHROLITHIASIS and NEPHROCALCINOSIS, and RICKETS.Osteopetrosis: Excessive formation of dense trabecular bone leading to pathological fractures; OSTEITIS; SPLENOMEGALY with infarct; ANEMIA; and extramedullary hemopoiesis (HEMATOPOIESIS, EXTRAMEDULLARY).Bicarbonates: Inorganic salts that contain the -HCO3 radical. They are an important factor in determining the pH of the blood and the concentration of bicarbonate ions is regulated by the kidney. Levels in the blood are an index of the alkali reserve or buffering capacity.Benzolamide: Selective renal carbonic anhydrase inhibitor. It may also be of use in certain cases of respiratory failure.Carbon Dioxide: A colorless, odorless gas that can be formed by the body and is necessary for the respiration cycle of plants and animals.Carbonic Acid: Carbonic acid (H2C03). The hypothetical acid of carbon dioxide and water. It exists only in the form of its salts (carbonates), acid salts (hydrogen carbonates), amines (carbamic acid), and acid chlorides (carbonyl chloride). (From Grant & Hackh's Chemical Dictionary, 5th ed)Isoenzymes: Structurally related forms of an enzyme. Each isoenzyme has the same mechanism and classification, but differs in its chemical, physical, or immunological characteristics.Hydrogen-Ion Concentration: The normality of a solution with respect to HYDROGEN ions; H+. It is related to acidity measurements in most cases by pH = log 1/2[1/(H+)], where (H+) is the hydrogen ion concentration in gram equivalents per liter of solution. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)Dansyl Compounds: Compounds that contain a 1-dimethylaminonaphthalene-5-sulfonyl group.Sodium-Bicarbonate Symporters: Proteins that cotransport sodium ions and bicarbonate ions across cellular membranes.Zinc: A metallic element of atomic number 30 and atomic weight 65.38. It is a necessary trace element in the diet, forming an essential part of many enzymes, and playing an important role in protein synthesis and in cell division. Zinc deficiency is associated with ANEMIA, short stature, HYPOGONADISM, impaired WOUND HEALING, and geophagia. It is known by the symbol Zn.Crystallography, X-Ray: The study of crystal structure using X-RAY DIFFRACTION techniques. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)Models, Molecular: Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.Histidine: An essential amino acid that is required for the production of HISTAMINE.Protons: Stable elementary particles having the smallest known positive charge, found in the nuclei of all elements. The proton mass is less than that of a neutron. A proton is the nucleus of the light hydrogen atom, i.e., the hydrogen ion.Kinetics: The rate dynamics in chemical or physical systems.Catalysis: The facilitation of a chemical reaction by material (catalyst) that is not consumed by the reaction.Catalytic Domain: The region of an enzyme that interacts with its substrate to cause the enzymatic reaction.Pancreatitis, Alcoholic: Acute or chronic INFLAMMATION of the PANCREAS due to excessive ALCOHOL DRINKING. Alcoholic pancreatitis usually presents as an acute episode but it is a chronic progressive disease in alcoholics.Protein Denaturation: Disruption of the non-covalent bonds and/or disulfide bonds responsible for maintaining the three-dimensional shape and activity of the native protein.Anion Exchange Protein 1, Erythrocyte: A major integral transmembrane protein of the ERYTHROCYTE MEMBRANE. It is the anion exchanger responsible for electroneutral transporting in CHLORIDE IONS in exchange of BICARBONATE IONS allowing CO2 uptake and transport from tissues to lungs by the red blood cells. Genetic mutations that result in a loss of the protein function have been associated with type 4 HEREDITARY SPHEROCYTOSIS.Protein Conformation: The characteristic 3-dimensional shape of a protein, including the secondary, supersecondary (motifs), tertiary (domains) and quaternary structure of the peptide chain. PROTEIN STRUCTURE, QUATERNARY describes the conformation assumed by multimeric proteins (aggregates of more than one polypeptide chain).Carbonic Anhydrase V: A carbonic anhydrase isoenzyme found in MITOCHONDRIA where it provides bicarbonate ions that are components in the urea cycle and in GLUCONEOGENESIS.Sulfonamides: A group of compounds that contain the structure SO2NH2.EsterasesAcroleinOncogene Proteins v-erbA: Transforming proteins encoded by erbA oncogenes from the avian erythroblastosis virus. They are truncated versions of c-erbA, the thyroid hormone receptor (RECEPTORS, THYROID HORMONE) that have retained both the DNA-binding and hormone-binding domains. Mutations in the hormone-binding domains abolish the transcriptional activation function. v-erbA acts as a dominant repressor of c-erbA, inducing transformation by disinhibiting proliferation.Water: A clear, odorless, tasteless liquid that is essential for most animal and plant life and is an excellent solvent for many substances. The chemical formula is hydrogen oxide (H2O). (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)Hydrogen Bonding: A low-energy attractive force between hydrogen and another element. It plays a major role in determining the properties of water, proteins, and other compounds.Erythrocytes: Red blood cells. Mature erythrocytes are non-nucleated, biconcave disks containing HEMOGLOBIN whose function is to transport OXYGEN.Binding Sites: The parts of a macromolecule that directly participate in its specific combination with another molecule.Protein Folding: Processes involved in the formation of TERTIARY PROTEIN STRUCTURE.Cattle: Domesticated bovine animals of the genus Bos, usually kept on a farm or ranch and used for the production of meat or dairy products or for heavy labor.Antiporters: Membrane transporters that co-transport two or more dissimilar molecules in the opposite direction across a membrane. Usually the transport of one ion or molecule is against its electrochemical gradient and is "powered" by the movement of another ion or molecule with its electrochemical gradient.Enzyme Stability: The extent to which an enzyme retains its structural conformation or its activity when subjected to storage, isolation, and purification or various other physical or chemical manipulations, including proteolytic enzymes and heat.Molecular Sequence Data: Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.Molecular Structure: The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.PubMed: A bibliographic database that includes MEDLINE as its primary subset. It is produced by the National Center for Biotechnology Information (NCBI), part of the NATIONAL LIBRARY OF MEDICINE. PubMed, which is searchable through NLM's Web site, also includes access to additional citations to selected life sciences journals not in MEDLINE, and links to other resources such as the full-text of articles at participating publishers' Web sites, NCBI's molecular biology databases, and PubMed Central.Periodicals as Topic: A publication issued at stated, more or less regular, intervals.Thermodynamics: A rigorously mathematical analysis of energy relationships (heat, work, temperature, and equilibrium). It describes systems whose states are determined by thermal parameters, such as temperature, in addition to mechanical and electromagnetic parameters. (From Hawley's Condensed Chemical Dictionary, 12th ed)ArchivesBiological Science Disciplines: All of the divisions of the natural sciences dealing with the various aspects of the phenomena of life and vital processes. The concept includes anatomy and physiology, biochemistry and biophysics, and the biology of animals, plants, and microorganisms. It should be differentiated from BIOLOGY, one of its subdivisions, concerned specifically with the origin and life processes of living organisms.

Calcium, carbonic anhydrase and gastric acid secretion. (1/207)

Previous data concerning the action of calcium (Ca) on gastric acid secretion (GAS) indicated that calcium ions increase GAS elicited by gastrin released through a vagal mechanism, and also by a direct effect on parietal cells. Our research showed that the stimulating effect of calcium on gastric acid secretion can be antagonized by verapamil administration, which reduces gastric acid secretion . In the present study we followed the effect induced by administration of calcium and Ca-chelating agents (disodium EDTA) on gastric acid secretion and on carbonic anhydrase (CA) activity. We selected two groups of healthy volunteers: Group I (n=21) received a single i.v. dose of CaCl2 (15 mg/kg b.w.), whereas Group II (n=22) received a single i.v. dose of disodium EDTA (5 mg/kg b.w.). We determined blood calcium before and after treatment, gastric acid secretion at 2 hours. erythrocyte CA II activity, and CA IV activity in membrane parietal cells, which were isolated from gastric mucosa obtained by endoscopic biopsy. Assessment of carbonic anhydrase activity was achieved by the stopped-flow method. In Group I calcium administration increased blood calcium, HCl output, CA II and CA IV activity as compared to initial values. In Group II, disodium EDTA reduced blood calcium, HCl output, CA II and CA IV activity as compared to initial values. The results demonstrated that increased blood calcium and GAS values after calcium administration correlated with the increase of erythrocyte CA II and parietal cell CA IV activity, while disodium EDTA induced a reversed process. Our results also show that cytosolic CA II and membrane CA IV values are sensitive to calcium changes and they directly depend on these levels. Our data suggest that intra- and extracellular pH changes induced by carbonic anhydrase might account for the modulation of the physiological and pathological secretory processes in the organism.  (+info)

A transport metabolon. Functional interaction of carbonic anhydrase II and chloride/bicarbonate exchangers. (2/207)

The cytoplasmic carboxyl-terminal domain of AE1, the plasma membrane chloride/bicarbonate exchanger of erythrocytes, contains a binding site for carbonic anhydrase II (CAII). To examine the physiological role of the AE1/CAII interaction, anion exchange activity of transfected HEK293 cells was monitored by following the changes in intracellular pH associated with AE1-mediated bicarbonate transport. AE1-mediated chloride/bicarbonate exchange was reduced 50-60% by inhibition of endogenous carbonic anhydrase with acetazolamide, which indicates that CAII activity is required for full anion transport activity. AE1 mutants, unable to bind CAII, had significantly lower transport activity than wild-type AE1 (10% of wild-type activity), suggesting that a direct interaction was required. To determine the effect of displacement of endogenous wild-type CAII from its binding site on AE1, AE1-transfected HEK293 cells were co-transfected with cDNA for a functionally inactive CAII mutant, V143Y. AE1 activity was maximally inhibited 61 +/- 4% in the presence of V143Y CAII. A similar effect of V143Y CAII was found for AE2 and AE3cardiac anion exchanger isoforms. We conclude that the binding of CAII to the AE1 carboxyl-terminus potentiates anion transport activity and allows for maximal transport. The interaction of CAII with AE1 forms a transport metabolon, a membrane protein complex involved in regulation of bicarbonate metabolism and transport.  (+info)

Estrogen regulation of ion transporter messenger RNA levels in mouse efferent ductules are mediated differentially through estrogen receptor (ER) alpha and ER beta. (3/207)

Earlier studies have shown that the efferent ductules (ED) of the male mouse are a target for estrogen. The loss of estrogen receptor (ER) function through either knockout technology (alpha ERKO mouse) or chemical interference (pure antagonist, ICI 182 780) results in a failure of a major function of the ED, the reabsorption of testicular fluids. The purpose of this study was to test the hypothesis that estrogen controls fluid (water) reabsorption in the ED by modulating ion transporters important for passive water movement through a leaky epithelium such as the ED. Northern blot analysis was used to detect the mRNA levels for key ion transporters in the following experimental groups: 1) wild-type (WT) control for the 14-day experiment, 2) ER alpha knockout (alpha ERKO) control for the 14-day experiment, 3) WT treated with ICI 182 780 (ICI) for 14 days, 4) alpha ERKO treated with ICI for 14 days, 5) WT control for the 35-day experiment, and 6) WT treated with ICI for 35 days. Estrogen differentially modulated the mRNA levels of key ion transporters. ER alpha mediated carbonic anhydrase II mRNA abundance, and there was a decrease in Na(+)/H(+) exchanger 3 mRNA levels in the alpha ERKO that appeared to be a cellular effect and not a direct estrogen effect. The loss of ER alpha control resulted in an increase in mRNA abundance for the catalytic subunit of Na(+)-K(+) ATPase alpha 1, whereas an increase in the mRNA abundance of the Cl(-)/HCO(3)(-) exchanger and the chloride channel cystic fibrosis transmembrane regulator was significantly ER beta mediated. Our results indicate for the first time that estrogen acting directly and indirectly through both ER alpha and ER beta probably modulates fluid reabsorption in the adult mouse ED by regulating the expression of ion transporters involved in the movement of Na(+) and Cl(-).  (+info)

Estrogen action and male fertility: roles of the sodium/hydrogen exchanger-3 and fluid reabsorption in reproductive tract function. (4/207)

Estrogen receptor alpha (ER alpha) is essential for male fertility. Its activity is responsible for maintaining epithelial cytoarchitecture in efferent ductules and the reabsorption of fluid for concentrating sperm in the head of the epididymis. These discoveries and others have helped to establish estrogen's bisexual role in reproductive importance. Reported here is the molecular mechanism to explain estrogen's role in fluid reabsorption in the male reproductive tract. It is shown that estrogen regulates expression of the Na(+)/H(+) exchanger-3 (NHE3) and the rate of (22)Na(+) transport, sensitive to an NHE3 inhibitor. Immunohistochemical staining for NHE3, carbonic anhydrase II (CAII), and aquaporin-I (AQP1) was decreased in ER alpha knockout (alpha ERKO) efferent ductules. Targeted gene-deficient mice were compared with alpha ERKO, and the NHE3 knockout and CAII-deficient mice showed alpha ERKO-like fluid accumulation, but only the NHE3 knockout and alpha ERKO mice were infertile. Northern blot analysis showed decreases in mRNA for NHE3 in alpha ERKO and antiestrogen-treated mice. The changes in AQP1 and CAII in alpha ERKO seemed to be secondary because of the disruption of apical cytoarchitecture. Ductal epithelial ultrastructure was abnormal only in alpha ERKO mice. Thus, in the male, estrogen regulates one of the most important epithelial ion transporters and maintains epithelial morphological differentiation in efferent ductules of the male, independent of its regulation of Na(+) transport. Finally, these data raise the possibility of targeting ER alpha in developing a contraceptive for the male.  (+info)

Crystal structure of human carbonic anhydrase II complexed with an anti-convulsant sugar sulphamate. (5/207)

The fructose-based sugar sulphamate RWJ-37497, a potent analogue of the widely used anti-epileptic drug topiramate, possesses anti-convulsant and carbonic anhydrase-inhibitory activities. We have studied the binding interactions of RWJ-37497 in the active site of human carbonic anhydrase II by X-ray crystallography. The atomic positions of the enzyme inhibitor complex were refined at a resolution of 2.1 A (1 A=0.1 nm) to the final crystallographic R and R(free) values of 0.18 and 0.23, respectively. The inhibitor co-ordinates to the active-site zinc ion through its oxygen atom and the ionized nitrogen atom of the sulphamate group by replacing the metal-bound water molecules, although the sulphamoyl oxygen atom provides a rather lengthy co-ordination. The 4,5-cyclic sulphate group is positioned in a hydrophobic pocket of the active site, making contacts with the residues Phe-131, Leu-198, Pro-201 and Pro-202. Since the ligand was found to be intact, concerns about RWJ-37947 irreversibly alkylating the enzyme through its 4,5-cyclic sulphate group were dispelled.  (+info)

Combinatorial computational method gives new picomolar ligands for a known enzyme. (6/207)

Combinatorial small molecule growth algorithm was used to design inhibitors for human carbonic anhydrase II. Two enantiomeric candidate molecules were predicted to bind with high potency (with R isomer binding stronger than S), but in two distinct conformations. The experiments verified that computational predictions concerning the binding affinities and the binding modes were correct for both isomers. The designed R isomer is the best-known inhibitor (K(d) approximately 30 pM) of human carbonic anhydrase II.  (+info)

In vivo repression of an erythroid-specific gene by distinct corepressor complexes. (7/207)

To assess the mechanisms of repression of the erythroid-specific carbonic anhydrase II (CAII) locus we used chromatin immunoprecipitation and show that an NCoR-histone deacetylase (HDAC)3 complex is recruited by the nuclear receptor v-ErbA to the intronic HS2 enhancer turning it into a potent silencer. Furthermore we demonstrate that efficient CAII silencing requires binding of a MeCP2-targeted HDAC-containing corepressor complex to the hypermethylated CpG-island at the promoter. Activation of transcription by either AZAdC or thyroid hormone results in loss of one of the two corepressor complexes. Thyroid hormone further replaces the enhancer-bound NCoR-corepressor complex by the TRAP220 coactivator. Treatment with the HDAC inhibitor trichostatin A (TSA) causes activation of CAII transcription and histone H3 and H4 hyperacetylation at the enhancer, apparently without affecting binding of the two corepressor complexes. Unexpectedly, histone H3 and H4 at the fully repressed promoter are already hyperacetylated despite the close apposition of the MeCP2-targeted HDAC complex. Acetylation of histone H4, but not H3, at the promoter is moderately increased following TSA treatment. Our data suggest that the hyperacetylated but repressed CAII promoter is (partially) remodeled and primed for activation in v-ErbA-transformed cells.  (+info)

Induction of oligodendrocyte-like properties in a primitive hypothalamic cell line by cholesterol, an eye derived growth factor and brain extract. (8/207)

A serum-free medium has been devised which permits proliferation of the mouse primitive nervous cell line F7. When cholesterol, eye-derived growth factor and brain extract are added in this medium for 48 h, 80-90% of oligodendrocyte-like cells are generated. These cells have diminished substrate adhesion. They acquire the capacity to synthesize carbonic anhydrase II and myelin basic protein, two specific proteins of oligodendrocytes. These observations suggest that F7 clonal cell line, which has been previously shown to be a neurophysin cell precursor, is also a precursor for oligodendrocytes, and represents a bipotent stem cell line for both neuronal and glial cell lineages.  (+info)

Most loss-of-function diseases are caused by aberrant folding of important proteins. These proteins often misfold due to inherited mutations. The rare disease marble brain disease (MBD) also known as carbonic anhydrase II deficiency syndrome (CADS) can manifest in carriers of point mutations in the human carbonic anhydrase II (HCA II) gene. We have over the past 10-15 years studied the folding, misfolding and aggregation of the enzyme human carbonic anhydrase II. In summary our HCA II folding studies have shown that the protein folds via an intermediate of molten-globule type, which lacks enzyme activity and the molten globule state of HCA II is prone to aggregation. One mutation associated with MBD entails the His107Tyr (H107Y) substitution. We have demonstrated that the H107Y mutation is a remarkably destabilizing mutation influencing the folding behavior of HCA II. A mutational survey of position H107 and a neighboring conserved position E117 has been performed entailing the mutants H107A, ...
Aryl sulfonamides are a widely used drug class for the inhibition of carbonic anhydrases. In the context of our program of photochromic pharmacophores we were interested in the exploration of azobenzene-containing sulfonamides to block the catalytic activity of human carbonic anhydrase II (hCAII). Herein, we report the synthesis and in vitro evaluation of a small library of nine photochromic sulfonamides towards hCAII. All molecules are azobenzene-4-sulfonamides, which are substituted by different functional groups in the 4 -position and were characterized by X-ray crystallography. We aimed to investigate the influence of electrondonating or electron-withdrawing substituents on the inhibitory constant Ki. With the aid of an hCAII crystal structure bound to one of the synthesized azobenzenes, we found that the electronic structure does not strongly affect inhibition. Taken together, all compounds are strong blockers of hCAII with K-i = 25-65 nM that are potentially photochromic and thus combine ...
Most loss-of-function diseases are caused by aberrant folding of important proteins. These proteins often misfold due to inherited mutations. The rare disease marble brain disease (MBD) also known as carbonic anhydrase II deficiency syndrome (CADS) can manifest in carriers of point mutations in the human carbonic anhydrase II (HCA II) gene. We have over the past 10-15 years studied the folding, misfolding and aggregation of the enzyme human carbonic anhydrase II. In summary our HCA II folding studies have shown that the protein folds via an intermediate of molten-globule type, which lacks enzyme activity and the molten globule state of HCA II is prone to aggregation. One mutation associated with MBD entails the His107Tyr (H107Y) substitution. We have demonstrated that the H107Y mutation is a remarkably destabilizing mutation influencing the folding behavior of HCA II. A mutational survey of position H107 and a neighboring conserved position E117 has been performed entailing the mutants H107A, ...
cansSAR 3D Structure of 3DC3 | USE OF CARBONIC ANHYDRASE II, IX ACTIVE-SITE MIMIC, FOR THE PURPOSE OF SCREENING INHIBITORS FOR POSSIBLE ANTI-CANCER PROPERTIES | 3DC3_A | Carbonic anhydrase 2 - Also known as CAH2_HUMAN, CA2. Essential for bone resorption and osteoclast differentiation (By similarity). Reversible hydration of carbon dioxide. Can hydrate cyanamide to urea. Involved in the regulation of fluid secretion into the anterior chamber of the eye. Contributes to intracellular pH regulation in the duodenal upper villous epithelium during proton-coupled peptide absorption. Stimulates the chloride-bicarbonate exchange activity of SLC26A6. Interacts with SLC4A4. Interaction with SLC4A7 regulates SLC4A7 transporter activity. Interacts with SLC26A6 isoform 4 (via C-terminus cytoplasmic domain).
Mono- and Stereopictres of 5.0 Angstrom coordination sphere of Zinc atom in PDB 1z9y: Carbonic Anhydrase II in Complex With Furosemide As Sulfonamide Inhibitor
The X-ray crystal structure of the complex between human carbonic anhydrase II and the inhibitor 1,2,4-triazole has been refined at 1.9 A resolution to a final R-factor of 0.153. Triazole is an analogue of the competitive inhibitor imidazole, but the crystal structure shows a different type of binding to the enzyme. 1,2,4-Triazole is directly bound to the zinc(II) ion through the nitrogen in position 4, replacing the native water/hydroxyl (Wat263) in a distorted four-co-ordinated complex. The interaction of the inhibitor with the active site is completed by two hydrogen bonds to O gamma of Thr200 and to the amide nitrogen atom of Thr199 through the two adjacent N-1 and N-2 atoms. The binding site of triazole overlaps the proposed binding sites for the substrates, explaining the observed competitive behaviour of the inhibitor towards CO2/HCO3- under equilibrium conditions. Crystal structure of the complex between human carbonic anhydrase II and the aromatic inhibitor 1,2,4-triazole.,Mangani S, ...
12CA: Altering the mouth of a hydrophobic pocket. Structure and kinetics of human carbonic anhydrase II mutants at residue Val-121.
In the catalysis of the hydration of carbon dioxide and dehydration of bicarbonate by human carbonic anhydrase II (HCA II), a histidine residue (His64) shuttles protons between the zinc-bound solvent molecule and the bulk solution. To evaluate the effect of the position of the shuttle histidine and …
In the catalysis of the hydration of carbon dioxide and dehydration of bicarbonate by human carbonic anhydrase II (HCA II), a histidine residue (His64) shuttles protons between the zinc-bound solvent molecule and the bulk solution. To evaluate the effect of the position of the shuttle histidine and pH on proton shuttling, we have examined the catalysis and crystal structures of wild-type HCA II and two double mutants: H64A/N62H and H64A/N67H HCA II. His62 and His67 both have their side chains extending into the active-site cavity with distances from the zinc approximately equivalent to that of His64. Crystal structures were determined at pH 5.1-10.0, and the catalysis of the exchange of (18)O between CO(2) and water was assessed by mass spectrometry. Efficient proton shuttle exceeding a rate of 10(5) s(-)(1) was observed for histidine at positions 64 and 67; in contrast, relatively inefficient proton transfer at a rate near 10(3) s(-)(1) was observed for His62. The observation, in the crystal ...
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SWISS-MODEL Template Library (SMTL) entry for 1t9n.1. Effect of Shuttle Location and pH Environment on H+ Transfer in Human Carbonic Anhydrase II
BioAssay record AID 644085 submitted by ChEMBL: Inhibition of human carbonic anhydrase 2 using 4-nitrophenylacetate as substrate after 3 mins using spectrophotometry by Lineweaver-Burk plot analysis.
The HE6 receptor is expressed at high levels within the efferent ductules and the initial segment of the epididymis (32, 34), regions of the reproductive tract which are well characterized as being responsible for the absorption of ,90% of the fluid produced by the testis (4). The concentration of sperm delivered to the ductus epididymis is determined by the net fluid reabsorption across the efferent duct epithelium (4, 20). Considering the abnormal accumulation of spermatozoa within the efferent ductules observed in HE6 knockout mice, a role for this receptor in the regulation of fluid balance is suggested.. Fluid reabsorption within the efferent ductules is primarily a passive process that occurs in parallel with the establishment of an Na+ gradient across the nonciliated cells of the epithelium (17). The hydration of CO2 by carbonic anhydrase II within the nonciliated cells results in the production of H+ and HCO3−. H+ is exchanged for luminal Na+ by the apically located sodium-hydrogen ...
2h4n: Histidine --| carboxamide ligand substitutions in the zinc binding site of carbonic anhydrase II alter metal coordination geometry but retain catalytic activity.
Immunohistochemical staining of multinucleated giant bone-resorbing cells. The cells were stained green for (a) carbonic anhydrase II and (b) vitronectin recept
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This study focused on the synthesis and characterization of hydrazide ligands and their respective Pd(II) complexes and used high throughput screening to determine their α-glucosidase and carbonic anhydrase II enzyme inhibition activities. The physical, analytical (elemental analyses for C, H, N and Pd) and spectral (FT-IR, 1H NMR, 13C NMR, EI-mass) techniques utilized during characterization revealed the formation of square planar, neutral and 1:2 Pd(II)-hydrazide complexes with the general formula [PdL2Cl2]. In these Pd(II) complexes, the hydrazide ligands are monodentate; the terminal nitrogen is the donor atom. The uncoordinated hydrazide ligands were inactive against both α-glucosidase and carbonic anhydrase II enzymes; however, the respective Pd(II)-hydrazide complexes were approximately 300 times more potent α-glucosidase inhibitors than the standard compound, 1-deoxynojirimycin (DNJ). Some of the Pd(II) complexes also demonstrated potential carbonic anhydrase (CA) inhibition ...
The high expression of CA-II in saliva of ruminating animals may be interpreted as an adaptation to maintain a suitable environment for ruminal microbes that are essential for the digestion of tough-structured, fibrous grass diets (3, 6). This would get strong support from the expression of the identical enzyme in Colobus monkeys, known to be the only foregut-fermenting primates, as well as in termites, the hindgut of which is an insect analogue to the bovine rumen. Providing the evidence of a connection between salivary CA concentration and changing ruminal or stomach pH in fore-stomach fermenters will enable us to easily and non-invasively detect and diagnose developing acidosis in a zoo environment before it becomes serious or lethal. Thereby, the overall performance and breeding success of Colobus monkeys or zoo ruminants could be improved.. Studies following the idea and techniques presented here may help to increase our knowledge of the important role that pH regulation plays in the ...
OAK RIDGE, Tenn., Feb. 12, 2018 - New insights from neutron analysis of glaucoma drugs and their enzyme target may help scientists design drugs that more effectively target aggressive cancers. A team of researchers led by the Department of Energys Oak Ridge National Laboratory used neutron macromolecular crystallography to investigate the different states of three glaucoma drugs as they interact with the targeted enzyme, human carbonic anhydrase II (hCA II).. "Our goal was to observe differences in the presentation of three clinically used glaucoma drugs while they are bound to the hCA II enzyme," said Andrey Kovalevsky, an instrument scientist at ORNL and a senior co-author of the study. "By looking at how well these drugs target hCA II in protonated, neutral and deprotonated states, we hoped to obtain insights that would make it possible to improve these medicines so they can better target enzymes linked to cancer.". Protonation refers to the presence, addition or loss of a proton, which ...
Brinzolamide is a highly specific, non-competitive, reversible carbonic anhydrase inhibitor. Carbonic anhydrase (CA) is an enzyme found in many tissues of the body including the eye. It catalyzes the reversible reaction involving the hydration of carbon dioxide and the dehydration of carbonic acid. In humans, carbonic anhydrase exists as a number of isoenzymes, the most active being carbonic anhydrase II (CA-II). Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport. The result is a reduction in intraocular pressure. Brinzolamide is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.
The IUPHAR/BPS Guide to Pharmacology. carbonic anhydrase 9 - Carbonic anhydrases. Detailed annotation on the structure, function, physiology, pharmacology and clinical relevance of drug targets.
Monocarboxylate transporter-5 (MCT5 or SLC16A4; sometimes referred to as MCT4). Lactate transport via the MCT5 is non enzymatically stimulated by carbonic anhydrase II (Becker et al., 2010). MCTs require an ancillary 1TMS glycoprotein, either Embigin (Q6PCB8; TC# 8.A.23.1.2) or basigin (P35613; TC# 8.A.23.1.1) for plasma membrane localization (Ovens et al., 2010). Upregulated in some cancers and maintains the metabolic phenotype of these cancer cells by mediating lactate efflux together with a proton, promoting pH homeostasis (Baltazar et al. 2014). Also transports the chemotheraputic agent, 3-bromopyruvate (Baltazar et al. 2014 ...
3mzc: Selective hydrophobic pocket binding observed within the carbonic anhydrase II active site accommodate different 4-substituted-ureido-benzenesulfonamides and correlate to inhibitor potency.
Carbonic anhydrases (CAs) are a large family of zinc metalloenzymes that catalyze the reversible hydration of carbon dioxide. They participate in a variety of biological processes, including respiration, calcification, acid-base balance, bone resorption, and the formation of aqueous humor, cerebrospinal fluid, saliva, and gastric acid. They show extensive diversity in tissue distribution and in their subcellular localization. CA IX is a transmembrane protein and is one of only two tumor-associated carbonic anhydrase isoenzymes known. It is expressed in all clear-cell renal cell carcinoma, but is not detected in normal kidney or most other normal tissues. It may be involved in cell proliferation and transformation. This gene was mapped to 17q21.2 by fluorescence in situ hybridization, however, radiation hybrid mapping localized it to 9p13-p12. [provided by RefSeq, Jun 2014 ...
Carbonic anhydrase 12, 0.1 ml. Carbonic anhydrases (CAs) are a large family of zinc metalloenzymes that catalyze the reversible hydration of carbon dioxide.
Zn(2+)-dependent carbonic anhydrases (CA) catalyse the reversible hydration of carbon dioxide to bicarbonate and participate in diverse physiological processes, hence having manifold therapeutic potentials. Among the 15 human CAs with wide-ranging sub-cellular localisation and kinetic properties, CA VI is the only secretory isoform. The 1.9Å crystal structure of the human CA VI catalytic domain reveals a prototypical mammalian CA fold, and a novel dimeric arrangement as compared to previously-reported CA structures. The active site cavity contains a cluster of non-conserved residues that may be involved in ligand binding and have significant implications for developing the next-generation of isoform-specific inhibitors.
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Occasional coexistence of pancreatitis with other autoimmune diseases suggests that there may be common target antigens in the pancreas and other exocrine organs, such as the salivary glands, biliary tract, and renal tubules. Several autoantibodies such as antinuclear antibody (ANA), antilactoferrin (LF) antibody (ALF), anticarbonic anhydrase II (CA-II) antibody (ACA-II), and rheumatoid factor (RF) were frequently detected in patients with AIP.12,13 CA-II and LF are distributed in the cells of several exocrine organs, including the pancreas, salivary glands, biliary duct, and distal renal tubules.12 The high prevalence of these antibodies suggests that CA-II and LF may be candidates for the target antigens in AIP. However, it was found that these autoantibodies are not necessarily specific for AIP.12 Although the majority of diabetic patients with associated AIP show type 2 diabetes mellitus, a few AIP patients with type 1A diabetes mellitus have autoantibodies against glutamic acid ...
RESEARCH TRIANGLE PARK, N.C., Jan. 26, 2017-- Metabolon, Inc., the global leader in metabolomics, announced changes today to its executive team. Prior to joining Metabolon, he was the Managing Director of Klaipeda Health, a healthcare and life sciences advisory company. He has held a variety of commercial, medical, scientific, informatics and technology leadership...
US Patent 8,131,473. Data analysis methods for locating entities of interest within large, multivariable datasets. Inventors: Marie Coffin, Keith Allen, Brian Bullard, Alan Higgins. Assignee: Metabolon
We post blogs on all things metabolomics - from the latest publications to precision medicine. Visit the page to view recent posts from Metabolon.
We post blogs on all things metabolomics - from the latest publications to precision medicine. Visit the page to view recent posts from Metabolon.
Carbon dioxide sequestration activity was compared and evaluated using bovine carbonic anhydrase (BCA), and a water soluble protein extract derived from hemocytes from diseased shell (HDS). Para-nitro
B. Żołnowska, J. Sławiński, K. Szafrański, A. Angeli, C. T. Supuran, A. Kawiak, M. Wieczór, J. Zielińska, T. Bączek, S. Bartoszewska. Novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(1,3,5-triazin-2-ylamino)guanidine derivatives: Inhibition of human carbonic anhydrase cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII, anticancer activity, and molecular modeling studies. Eur. J. Med. Chem. 2018, 143, 1931-1941. ...
SWISS-MODEL Template Library (SMTL) entry for 3hlj.1. Crystal structure of human carbonic anhydrase isozyme II with 3-methylthiobenzimidazo[1,2-c][1,2,3]thiadiazol-7-sulfonamide
We present a fast (,,1 s per profile) inversion code for solar Ca II lines. The code uses an archive of spectra that are synthesized prior to the inversion under the assumption of local thermodynamic equilibrium (LTE). We show that it can be successfully applied to spectrograph data or more sparsely sampled spectra from two-dimensional spectrometers. From a comparison to a non-LTE inversion of the same set of spectra, we derive a first-order non-LTE correction to the temperature stratifications derived in the LTE approach. The correction factor is close to unity up to log τ ∼ -3 and increases to values of 2.5 and 4 at log τ = -6 in the quiet Sun and the umbra, respectively. ...
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Synthesis, characterization, thermal stability and pyrolysis of some alkaline earth picolinates M(C H NO ) ⋅nH O (where M = Mg(II), Ca(II), Sr(II) and Ba(II ...
To further assess our results, we performed a literature review of the genes reported by at least seven studies in the cancer versus normal comparison to determine if any have been shown to have diagnostic and/or prognostic utility in colorectal cancer. The most consistently reported differentially expressed gene in our meta-analysis was carbonic anhydrase II (CA2), which was reported as down-regulated in 11 studies. Along with carbonic anhydrase I, CA2 has been shown to have prognostic significance where the expression of both enzymes was related to the metastatic aggressiveness of colorectal cancer (23). Similarly, the potential diagnostic utility of CA2 was shown in a study in which the average level of fecal CA2 in colorectal cancer patients was shown to be significantly greater than those in the control group (24). Immunohistochemistry has been done on colorectal tumor and healthy mucosa tissue to monitor the protein levels of four carbonic anhydrases, among them CA2 (25). That study showed ...
This study tests the hypothesis that the increase in blood PCO2 and associated respiratory acidosis after exhaustive exercise play an important role in stimulating ventilation during post-exercise recovery in fish. Injection of bovine carbonic anhydrase (10 mg kg-1) into the bloodstream of rainbow trout caused a persistent 40 % increase in the HCO3- dehydration capacity of the blood. The treatment was designed to increase CO2 excretion and therefore to reduce PCO2 build-up and acidosis after exercise. Aerobic and anaerobic swimming performance were not affected by carbonic anhydrase, and there were only very minor effects on arterial blood acid­base status in resting fish. However, carbonic anhydrase attenuated post-exercise increases in PaCO2 and decreases in pHa by about 50 % without altering arterial O2 variables, red cell swelling or the intracellular pH of the brain or muscle tissues. The effects on arterial pH (pHa) resulted largely from alleviation of the increase in PaCO2. In ...
Carbonic anhydrase III (CAIII) is a member of a multigene family (at least six separate genes are known) that encodes carbonic anhydrase isozymes. These carbonic anhydrases are a class of metalloenzymes that catalyze the reversible hydration of carbon dioxide and are differentially expressed in a number of cell types. The expression of the CA3 gene is strictly tissue specific and present at high levels in skeletal muscle and much lower levels in cardiac and smooth muscle. A proportion of carriers of Duchenne muscle dystrophy have a higher CA3 level than normal. The gene spans 10.3 kb and contains seven exons and six introns. [provided by RefSeq, Oct 2008 ...
ESCUDERO-ALMANZA, Dalila Jacqueline et al. Carbonic Anhydrase and Zinc in Plant Physiology. Chilean J. Agric. Res. [online]. 2012, vol.72, n.1, pp.140-146. ISSN 0718-5839. http://dx.doi.org/10.4067/S0718-58392012000100022.. Carbonic anhydrase (CA) (EC: 2.4.1.1) catalyzes the rapid conversion of carbon dioxide plus water into a proton and the bicarbonate ion (HCO3-) that can be found in prokaryotes and higher organisms; it is represented by four different families. Carbonic anhydrase is a metalloenzyme that requires Zn as a cofactor and is involved in diverse biological processes including pH regulation, CO2 transfer, ionic exchange, respiration, CO2 photosynthetic fixation, and stomatal closure. Therefore, the review includes relevant aspects about CA morphology, oligomerization, and structural differences in the active site. On the other hand, we consider the general characteristics of Zn, its geometry, reactions, and physiology. We then consider the CA catalysis mechanism that is carried out ...
Uppsala University, Teknisk-naturvetenskapliga vetenskapsområdet, Faculty of Science and Technology, Biology, Department of Cell and Molecular Biology. ...
Find quality suppliers and manufacturers of 1694-06-0(Benzenesulfonamide,N-(aminocarbonyl)-4-methyl-) for price inquiry. where to buy 1694-06-0(Benzenesulfonamide,N-(aminocarbonyl)-4-methyl-).Also offer free database of 1694-06-0(Benzenesulfonamide,N-(aminocarbonyl)-4-methyl-) including MSDS sheet(poisoning, toxicity, hazards and safety),chemical properties,Formula, density and structure, solution etc.
Benzenesulfonamide 98-10-2 NMR spectrum, Benzenesulfonamide H-NMR spectral analysis, Benzenesulfonamide C-NMR spectral analysis ect.
One of the four discrete isoenzymes of carbonic anhydrase hitherto characterized, CA III, has the lowest turnover rate and the greatest resistance to inhibition by sulphonamides. Streptozotocin-induced diabetes mellitus resulted in a reduction in acetazolamide-resistant activity of carbonic anhydrase in the liver, but not in tonic skeletal muscle, of adult male rats. The hepatic activity declined with apparent first-order kinetics [calculated rate constant (k) 0.089 day-1] to a minimum of approx. 6% of control values; the reduction in activity was moderated by administration of insulin. ...
Human carbonic anhydrase 8 (CA-VIII) is an acatalytic isoform of the α -CA family. Though the protein cannot hydrate CO2, CA-VIII is essential for calcium (Ca2+) homeostasis within the body, and achieves this by allosterically inhibiting the binding of inositol 1,4,5-triphosphate (IP3) to the IP3 receptor type 1 (ITPR1) protein. However, the mechanism of interaction of CA-VIII to ITPR1 is not well understood. In addition, functional defects to CA-VIII due to non-synonymous single nucleotide polymorphisms (nsSNVs) result in Ca2+ dysregulation and the development of the phenotypes such as cerebellar ataxia, mental retardation and disequilibrium syndrome 3 (CAMRQ3). The pathogenesis of CAMRQ3 is also not well understood. The structure and function of CA-VIII was characterised, and pathogenesis of CAMRQ3 investigated. Structural and functional characterisation of CA-VIII was conducted through SiteMap and CPORT to identify potential binding site residues. The effects of four pathogenic nsSNVs,
Carbonic Anhydrase IX/CA9 Antibody Pairs available through Novus Biologicals. Browse our Carbonic Anhydrase IX/CA9 Antibody Pair catalog backed by our Guarantee+.
Carbonic Anhydrase IX/CA9 Antibody Pairs available through Novus Biologicals. Browse our Carbonic Anhydrase IX/CA9 Antibody Pair catalog backed by our Guarantee+.
We report the cloning, purification and characterization of the full domain of carbonic anhydrase (CA, EC 4.2.1.1) from Plasmodium falciparum, which incorporates 358 amino acid residues (from 181 to 538, in the sequence of this 600 amino acid long protein), called PfCAdom. The enzyme, which belongs to the η-CA class showed the following kinetic parameters: kcat of 3.8×10(5)s(-1) and kcat/Km of 7.2×10(7)M(-1)×s(-1), being 13.3 times more effective as a catalyst compared to the truncated form PfCA. PfCAdom is more effective than the human (h) isoform hCA I, being around 50% less effective compared to hCA II, one of the most catalytically efficient enzymes known so far. Intriguingly, the sulfonamides CA inhibitors generally showed much weaker inhibitory activity against PfCAdom compared to PfCA, prompting us to hypothesize that the 69 amino acid residues insertion present in the active site of this η-CA is crucial for the active site architecture. The best sulfonamide inhibitors for PfCAdom ...
FUNCTIONS OF CARBONIC ANHYDRASES. The presence of carbonic anhydrases in all living organisms probably originates because the components of the catalyzed reaction are involved in almost all metabolic processes. We suppose that the main reason for the abundance of CAs in nature is the ubiquitous involvement of bicarbonate buffers in aqueous media and then in the cytoplasm at every stage of evolution; these enzymes acceleration achieving appropriate pH, which is important for homeostasis of every living cell. The role of carbonic anhydrases in accelerating the conversion of inorganic forms of carbon was probably not their initial main function, but now it is established that these enzymes are critical regulators of the exchange of these forms in many metabolic processes.. Functions of Carbonic Anhydrases in Animals. Although the main purpose of this review is to consider the available experimental data and ideas concerning the role of CAs in higher plants, we should present, at least briefly, ...
Glaucoma is a serious disease associated with increased intraocular pressure which often leads to blindness. One of the ways to treat glaucoma is to reduce aqueous humour secretion in the ciliary body of the eye by suppressing (inhibiting) activity of special enzymes - carbonic anhydrases. Russian scientists from RUDN University have designed new compounds that can effectively reduce intraocular pressure by isoform selective inhibiting human carbonic anhydrase. The results of the study were published in the prestigious Bioorganic Chemistry journal.
Anti-human Carbonic Anhydrase IX/CA9 antibody,Rabbit MAb. Applications for ELISA,IHC-P, fully validated. Quality guaranteed. Buy elite antibodies at up to 60% cost saving.
Anti-human Carbonic Anhydrase IX/CA9 antibody,Rabbit MAb. Applications for ELISA,FCM, fully validated. Quality guaranteed. Buy elite antibodies at up to 60% cost saving.
Ectopic calcification as very well as fatty and fibrotic tissues accumulation occurs in skeletal muscle during the disease development of Duchenne buff dystrophy (DMD), a degenerative muscle disorder caused by mutations in the dystrophin gene. the nmMSCs become turned on during the disease development in dKO rodents, exhibiting elevated growth and difference possibilities (adipogenesis, osteogenesis and fibrogenesis). We discovered that after co-culturing the dKO-nmMSCs with dKO-MPCs also, the myogenic difference potential of the dKO-MPCs was decreased. This impact was discovered to end up being possibly mediated by the release of secreted frizzled-related proteins 1 by the dKO-nmMSCs. We posit that the speedy incidence of fibrosis as a result, ectopic calcification and fats deposition, in dKO rodents, is certainly not really just attributable to the speedy exhaustion of the MPC pool, but is certainly also the effect of nmMSC account activation. Outcomes from this research recommend that methods ...
Reactome is pathway database which provides intuitive bioinformatics tools for the visualisation, interpretation and analysis of pathway knowledge.
N-(Aminoiminomethyl)benzenesulfonamide/AFI4392374 can be provided in Alfa Chemistry. We are dedicated to provide our customers the best products and services.
en] Acidosis, Renal Tubular/chemically induced/enzymology ; Anticonvulsants/adverse effects/therapeutic use ; Carbonic Anhydrases/metabolism ; Female ; Fructose/adverse effects/analogs & derivatives/therapeutic use ; Humans ; Kidney/drug effects/enzymology/pathology ; Middle Aged ; Migraine Disorders/drug therapy ; Models, ...
Reactome is pathway database which provides intuitive bioinformatics tools for the visualisation, interpretation and analysis of pathway knowledge.
The enzyme catalyzes the reversible hydration of gaseous CO(2) to carbonic acid, which spontaneously converts to hydrogencarbonate under neutral pH. -!- It is widespread and found in archaea, bacteria, and eukaryotes. -!- Three distinct classes exist, and appear to have evolved independently ...
L-arginine, Disease, Patients, Arginine, Nitric Oxide, Carbonic Anhydrase, Isoforms, Inhibition, Sulfonamides, Active Site, Heart, and Concentrations
Carbonic anhydrases are abundant in mammalian tissues, plants and bacteria. The several distinct classes of this enzyme (α, β, γ etc.) share little similarity in terms of structure and sequence, but they all perform the same function of catalyzing the hydration of carbon dioxide and the dehydration of bicarbonate [3]. Carbonic anhydrase B is one of the two major forms of carbonic anhydrase in human red blood cell (the other form is CA C). Like other members of the CA family, its main function is assisting the important chemical reaction that occurs in the blood. CO2 + H2O ,-----, HCO3- + H+. The above reaction is very slow in the absence of the enzyme. Hence, by assisting the inter-conversion between carbon dioxide and bicarbonate, Carbonic anhydrase B helps to maintain acid-base balance in blood, and transport carbon dioxide out of blood. Note that the carbonic acid (H2CO3) and hydrogen carbonate ions (HCO3-) is an important buffer system in the body. They equilibrate in the blood plasma to ...
Novelty, in brief, is represented by the intended elaboration of carborane, heteroborane and metallaborane compounds as active-site inhibitors of CA isoenzymes. All currently used inhibitors anhydrase inhibitors contain a sulfonamide or a sulfamate moiety connected to so called ring structure which is usually a 5- or 6-membered aromatic ring or conjugated ring system containing nitrogen, oxygen, and/or sulfur heteroatoms. The ring structure bears characteristics or functionality which modulates the affinity toward certain CA isoform. The use of three-dimensional boron cluster is a novel approach in development of isoform-specific CA inhibitors. Selected sulfamides incorporating cluster with inhibitory effects toward CAs (IC50 values in low micromolar and submicromolar range, some of the inhibitors being more than 50-times more selective toward the tumor specific CAIX than for CAII abundantly present in normal tissues ...
Carbonic anhydrase IX (CAIX) is generally expressed in individual tumors and serves as a marker for hypoxia. Breasts. Am.J.Pathol. 2001;158:1011C1019. [PMC free of charge content] [PubMed] [10] Sowter HM, Raval R, Moore J, Ratcliffe PJ, Harris AL. Predominant Function of Hypoxia-Inducible Transcription Aspect Ednra (Hif)-1 Hif-2 in Legislation from the Transcriptional Response to Hypoxia. Cancers Res. 2003;63:6130C6134. [PubMed] [11] Chiche J, Ilc K, Laferriere J, Trottier E, Dayan F, Mazure NM, Brahimi-Horn MC, Pouyssegur J. Cyclopamine Hypoxia-Inducible Carbonic Anhydrase XII and IX Promote Tumor Cell Growth by Counteracting Acidosis coming from the Regulation from the Intracellular pH. Cancer tumor Res. 2009;69:358C368. [PubMed] [12] Swinson DEB, Jones JL, Richardson D, Wykoff C, Turley H, Pastorek J, Taub N, Harris AL, OBryne KJ. Carbonic Anhydrase IX Appearance, a Book Surrogate Marker of Tumor Hypoxia, Is normally Associated with an unhealthy Prognosis in Non-Small-Cell Lung Cancers. ...
Hyperventilation is a difficult diagnosis to make clinically and that is why having an objective test of hyperventilation is so useful. People who hyperventilate deplete their levels of red cell carbonic anhydrase and the ratio between the activity and the protein gives us a good indication of whether or not hyperventilation is a problem. Hyperventilation is also difficult to treat and so this test tells us how much effort we have to put in to correcting this. Essentially, there is a two-pronged approach - firstly biochemical and secondly physical: Biochemically, red cell carbonic anhydrase is a zinc dependent enzyme and will be depleted simply by zinc deficiency. Furthermore, a low red cell carbonic anhydrase drives hyperventilation and so this is another example of one of the many vicious cycles seen in patients with chronic fatigue. Zinc is best absorbed at night and I recommend taking 30mg last thing at night on an empty stomach. This should be in addition to zinc taken in my physiological ...
beta-Lactam antibiotics are a broad class of antibiotics, consisting of all antibiotic agents that contain a beta-lactam ring in their molecular structures. Synthesis of beta-lactam analogs, which are containing dichloride atoms and N-methyl, N-aromatic rings, was achieved by Schiff bases and dichloroketene compounds. All the synthesized imines and beta-lactam analogs were tested against two physiologically relevant carbonic anhydrase isozymes (hCA I and II) and acetylcholinesterase (AChE). They demponstrated effective inhibitory profiles with K-i values in ranging of 3.22-11.18 nM against hCA I, 3.74-10.41 nM against hCA II, and 0.50-1.57 nM against AChE. On the other hand, acetazolamide and dorzolamide clinically used as CA inhibitors, showed K-i value of 170.34 and 129.26nM against hCA I, and 115.43 and 135.67 nM against hCA II, respectively. Also, tacrine used as standard AChE inhibitor showed Ki value of 5.70 nM against AChE ...
Carbonic anhydrase (CA; EC 4.2.1.1) is a zinc containing enzyme which catalyzes a reversible reaction to form bicarbonate from carbon dioxide and water [1, 2]. By facilitating the interconversion between CO2 and bicarbonate in vivo, CA activity was proposed to be required to ensure adequate level of CO2or HCO3- as the substrates for other enzymes [3]. Therefore, CAs have been found to play an essential role in a series of fundamental biological processes such as photosynthesis, respiration, pH homeostasis and ion transport [4]. Based on the origins and structural features, CAs are divided into six classes, termed α, β, γ, δ, ε and ζ, respectively [5]. The α-CAs were found in mammals, algae and prokaryotes to facilitate the exchange of CO2 in the respiratory cycle. The β-CAs were characterized in higher plants, algae and prokaryotes, and those in higher plants have been reported to play a critical role during photosynthesis [6]. The γ-class was first identified in the thermophilic ...
Recombinant Carbonic Anhydrase VII (CA7) Protein. Species: Rat (Rattus). Source: Escherichia coli (E. coli). Order product ABIN6302725.
The IUPHAR/BPS Guide to Pharmacology. carbonic anhydrase 12 - 4.2.1.1 Carbonate dehydratases. Detailed annotation on the structure, function, physiology, pharmacology and clinical relevance of drug targets.
N-(1H-Imidazole-5-ylmethyl)-N-[4-[4-(benzylcarbamoyl)piperazino]phenyl]benzenesulfonamide | C28H30N6O3S | CID 44282638 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
Structure, properties, spectra, suppliers and links for: 4-Methyl-N-[4-(trimethylsilyl)-3-butyn-1-yl]-N-[(trimethylsilyl)ethynyl]benzenesulfonamide.
... ,These 2-D standards consist of seven reduced, denatured proteins (equine myoglobin, soybean trypsin inhibitor, bovine carbonic anhydrase, rabbit muscle GAPDH, bovine muscle actin, BSA, and hen egg white conalbumin) with pIs ranging from 4.5 to 8.5 and molecular weights ranging from 17,500 to 76,000,biological,biology supply,biology supplies,biology product
Residents of the Rivière-des-Prairies-Pointe-aux-Trembles-Montreal-East borough are being told to boil their water for five minutes before consuming it after E.Coli bacteria was detected in the water network.. The area south of Sherbrooke St. and east of de la Rousselière Blvd. to the edge of the island and the St. Lawrence River.. A public health official says the strain of E. coli found in the water supply near the eastern tip of Montreal is not harmful to humans. Seven people died and about 23-hundred people fell ill in Walkerton, Ontario after another strain of E. coli found its way into the towns water system two years ago. Residents will be advised when the matter is resolved, a process that could take a few days, the city said.. ...
Question 10: This is the reaction that integrates CO2 into ________ sugars during photosynthesis, and can use only the CO2 form of carbon, not carbonic acid or bicarbonate. ...
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Quinoline derivatives have diverse biological activities including anticancer activity. On the other hand, many sulfonamide derivatives exhibited good cytotoxic activity. Hybrids of both moieties may present novel anticancer agents. Chloroquinoline incorporating a biologically active benzene-sulfonamide moieties 5-21 and diarylsulfone derivatives 22 and 23 were prepared using (E)-1-(4-((E)-7-chloro-1-methylquinolin-4(1H)-ylideneamino)phenyl)-3-(dimethyl-amino)prop-2-en-1-one 4 as strategic starting material. The structure of the newly synthesized compounds were confirmed by elemental analyses and spectral data. Compound 4 was confirmed by X-ray crystallographic analysis. The prepared compounds were evaluated for their anticancer activity against Lung, HeLa, Colorectal and breast cancer cell lines. Compounds 2, 4, 7, 11, 14 and 17 showed better or comparable activity to 2′, 7′-dichlorofluorescein (DCF) as reference drug. Molecular docking of the active compounds on the active site of PI3K enzyme was
One of the major tasks of the renal proximal tubule (PT) is to secrete acid into the tubule lumen, thereby reabsorbing approximately 80% of the filtered bicarbonate (HCO3(-)), as well as generating "new HCO3(-)" for regulating blood pH. In the tubular lumen, filtered HCO3(-) combines with H(+) in a reaction catalyzed by CA IV. The CO2 thus produced rapidly diffuses into the tubular cells and is combined with water to produce intracellular H(+) and HCO3(-), catalyzed by soluble cytoplasmic CA II. HCO3(-) is then cotransported with Na(+) into blood via the NBC-1. The intracellular H(+) produced by CA II is secreted into the tubular lumen predominantly via the NHE-3. The PT creates the "new HCO3(-)" by taking glutamine and metabolizing it to two molecules each of NH4(+) and HCO3(-). The NH4(+) is excreted into the tubular lumen, and the HCO3(-) , which is "new HCO3(-) ," is returned to the blood, where it replaces the HCO3(-) lost earlier in the titration of nonvolatile acids ...
Creative Biolabs provides Lenti-Carbonic anhydrase IX (CA9) CAR (scFv-CD3ζ, G36) Viral Particle product for Biopharmaceutical research,preclinical and clinical trials.
... Systematic (IUPAC) name 4-amino-N-(2,6-dimethylpyrimidin-4-yl)benzenesulfonamide Identifiers CAS number 515-64-0 ATC code J01EB01
... Systematic (IUPAC) name 4-amino-N-(4-methoxypyrimidin-5-yl)benzenesulfonamide Identifiers CAS number  ? ATC code J01ED02 PubChem
TYTU : Synthesis, QSAR studies, and metabolic stability of novel 2-alkylthio-4-chloro-N-(5-oxo-4,5-dihydro-1,2,4-triazin-3-yl)benzenesulfonamide derivatives as potential anticancer and apoptosis-inducing agents ...
Cryptococcus neoformans, a fungal pathogen of humans, causes fatal meningitis in immunocompromised patients. Its virulence is mainly determined by the elaboration of a polysaccharide capsule surrounding its cell wall. During its life, C. neoformans is confronted with and responds to dramatic variations in CO2 concentrations; one important morphological change triggered by the shift from its natural habitat (0.033% CO2) to infected hosts (5% CO2) is the induction of capsule biosynthesis. In cells, CO2 is hydrated to bicarbonate in a spontaneous reaction that is accelerated by carbonic anhydrases. Here we show that C. neoformans contains two beta-class carbonic anhydrases, Can1 and Can2. We further demonstrate that CAN2, but not CAN1, is abundantly expressed and essential for the growth of C. neoformans in its natural environment, where CO2 concentrations are limiting. Structural studies reveal that Can2 forms a homodimer in solution. Our data reveal Can2 to be the main carbonic anhydrase and ...
The cuticle of the freshwater crayfish, Procambarus clarkii (Girard, 1852), has several extracellular, cuticular isozymes for carbonic anhydrase (CA) which were isolated and purified via affinity chromatography. To denature proteins not entombed in cuticle calcite the ground cuticle was washed twice with both a 0.5% SDS and 1.5% sodium hypochlorite solution prior to CA isolation. Total water soluble protein (WSP) was 133 ± 68 (SD) mg/100 g (6) cuticle, whereas affinity column bound protein, CA, was 191 ± 108 (SD) μg/100 g (6) cuticle. CA was 0.144% WSP. EDTA dissolved the calcium carbonate and freed the CA along with the other WSP. The CA fraction was positive to bovine CA II antibodies (ELIZA and Western Blot) and had low CA enzyme activity. The estimated molecular weights using PAGE showed one isozyme with a molecular weight of 29 kDa, which is similar to that in vertebrates, and two larger isozymes (53 and 66 kDa). All four isozymes were detected in only one sample, whereas the two larger isozymes
Carbonic anhydrase (CA) from erythrocytes of the pink salmon, Onchorhyncus gorbushka, was purified using chloroform-ethanol extraction and Sephadex G-75 gel filtration. A single, high specific-activity CA isozyme having a molecular weight of 29,000 was found. The enzyme sedimented as a ...read more ...
BACKGROUND: Carbonic anhydrase IX (CA9) is reportedly overexpressed in several types of carcinomas, but little is known about the expression pattern of CA9 in osteosarcoma. We aimed to assess the prevalence of CA9 expression and its prognostic implications in osteosarcoma patients. METHODS: We compared immunohistochemical expression of CA9 between conventional, high-grade and low-grade, central osteosarcomas. Specimens were obtained before chemotherapy and stained with anti-human CA9 antibody. We also evaluated the histologic grade, presence of metastasis, and patient prognosis. RESULTS: Among 38 samples of conventional high-grade osteosarcoma, 22 (57.9%) tumors displayed CA9 overexpression. Twenty-five cases of low-grade central osteosarcomas were all negative (p < 0.0001). CA9 expression was significantly associated with the presence of metastasis (p = 0.0010). The overall survival rate was significantly reduced with increased CA9 expression (p = 0.0012), higher histologic grade (p < 0.0001), ...
Carbonic anhydrase 12 is an enzyme that in humans is encoded by the CA12 gene. Carbonic anhydrases (CAs) are a large family of zinc metalloenzymes that catalyze the reversible hydration of carbon dioxide. They participate in a variety of biological processes, including respiration, calcification, acid-base balance, bone resorption, and the formation of aqueous humor, cerebrospinal fluid, saliva, and gastric acid. This gene product is a type I membrane protein that is highly expressed in normal tissues, such as kidney, colon and pancreas, and has been found to be overexpressed in 10% of clear cell renal carcinomas. Two transcript variants encoding different isoforms have been identified for this gene. Loss of function mutations in the CAXII gene result in defects in fluids and carbonate secretions in the following diseases: 1) Cystic fibrosis-like syndrome with normal cystic fibrosis transmembrane conductance regulator (CFTR) protein levels 2) Pancreatitis 3) Sjögrens syndrome 4) Xerostomia or ...
Title: EUROPAC 2 trial to investigate the efficacy of ANTOX (vers) 1.2 and MGCT (Magnesiocard) for the treatment of hereditary pancreatitis and idiopathic chronic pancreatitis. Study drug: ANTOX (vers) 1.2 MGCT (Magnesiocard). Intended indication: Hereditary pancreatitis and idiopathic chronic pancreatitis. Study design: A multi-centre, double blind, and placebo-controlled, randomised, parallel group study. Patient population: Patients with hereditary pancreatitis or idiopathic chronic pancreatitis. Number of patients: Total of 240 patients in three equal groups. Proposed number of initial centres: two (Greifswald, Germany and Liverpool, UK).. Duration of dosing: 12 months. Treatment groups:. Group one: Two ANTOX (vers) 1.2 tablets, three times daily, Antioxidant treatment: Daily: 300 µg organic selenium, 54000 IU beta carotene = 18 mg, 750 mg vitamin C, 540 IU of vitamin E = 240 mg, 2700 mg methionine.. Group two: Two Magnesium-L-Aspartate-hydrochloride (MGCT) (Magnesiocard  2,5 mmol ...
The plant hormone salicylic acid (SA) is required for defense responses. NON EXPRESSER OF PATHOGENESIS RELATED 1 (NPR1) and NON RECOGNITION OF BTH-4 (NRB4) are required for the response to SA in Arabidopsis (Arabidopsis thaliana). Here, we isolated several interactors of NRB4 using yeast two-hybrid assays. Two of these interactors, βCA1 and βCA2, are β-carbonic anhydrase family proteins. Since double mutant βca1 βca2 plants did not show any obvious phenotype, we investigated other βCAs and found that NRB4 also interacts with βCA3 and βCA4. Moreover, several βCAs interacted with NPR1 in yeast, including one that interacted in a SA-dependent manner. This interaction was abolished in loss-of-function alleles of NPR1. Interactions between βCAs and both NRB4 and NPR1 were also detected in planta, with evidence for a triple interaction, NRB4-βCA1-NPR1. The quintuple mutant βca1 βca2 βca3 βca4 βca6 showed partial insensitivity to SA. These findings suggest that one of the functions of carbonic
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Ectopic calcification (EC), which is the pathological deposition of calcium and phosphate in extra-skeletal tissues, may be associated with hypercalcaemic and hyperphosphataemic disorders, or it may occur in the absence of metabolic abnormalities. In addition, EC may be inherited as part of several monogenic disorders and studies of these have provided valuable insights into the metabolic pathways regulating mineral metabolism. For example, studies of tumoural calcinosis, a disorder characterised by hyperphosphataemia and progressive EC, have revealed mutations of fibroblast growth factor 23 (FGF23), polypeptide N-acetyl galactosaminyltransferase 3 (GALNT3) and klotho (KL), which are all part of a phosphate-regulating pathway. However, such studies in humans are limited by the lack of available large families with EC, and to facilitate such studies we assessed the progeny of mice treated with the chemical mutagen N-ethyl-N-nitrosourea (ENU) for EC. This identified two mutants with autosomal recessive
Sigma-Aldrich offers abstracts and full-text articles by [Vaida Morkūnaitė, Joana Gylytė, Asta Zubrienė, Lina Baranauskienė, Miglė Kišonaitė, Vilma Michailovienė, Vaida Juozapaitienė, Matthew J Todd, Daumantas Matulis].
Looking for Carbonic anhydrase iv? Find out information about Carbonic anhydrase iv. An enzyme which aids carbon dioxide transport and release by catalyzing the synthesis, and the dehydration, of carbonic acid from, and to, carbon dioxide... Explanation of Carbonic anhydrase iv
The inhibition of a newly cloned human carbonic anhydrase (CA, EC 4.2.1.1), isozyme VII (hCA VII), has been investigated with a series of aromatic and heterocyclic sulfonamides, including some of the clinically used derivatives (acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide and benzolamide), as well as the sulfamate antiepileptic drug topiramate. Inhibition data for the the other physiologically relevant cytosolic isoforms hCA I, hCA II and mCA XIII are also provided for comparison. hCA VII shows a high catalytic activity for the CO(2) hydration reaction, with a k(cat) of 9.5 x 10(5)s(-1) and k(cat)/K(m) of 8.3 x 10(7)M(-1)s(-1) at pH7.5 and 20 degrees C. A very interesting inhibition profile against hCA VII with this series of 32 sulfonamides/sulfamates was observed. hCA VII shows high affinity for all the investigated compounds, with inhibition constants in the range of 0.45-210 nM. Topiramate, ethoxzolamide and benzolamide showed subnanomolar hCA ...
Background: Carbonic anhydrase is found in the blood of all vertebrate and thus playing a fundamental role in the maintenance of acid-base homeostasis. Erythrocytes are intrinsically prone to oxidative stress because of their exposure to high oxygen tension. Aim: The study aimed to investigate the changes of erythrocytes anti-oxidative enzymes in STZ induced diabetic rats and to determine the antioxidant potential of Cadaba farinosa leaves. Results: The result of the present study showed that inhibition of carbonic anhydrase result in significant decrease in both erythrocyte and plasma catalase activity, whereas erythrocyte and plasma superoxide dismutase activity increased. Conclusion: Carbonic anhydrase inhibition may alter the activity of anti-oxidative enzymes in vivo ...
Looking for online definition of carbonic anhydrase inhibitor d's in the Medical Dictionary? carbonic anhydrase inhibitor d's explanation free. What is carbonic anhydrase inhibitor d's? Meaning of carbonic anhydrase inhibitor d's medical term. What does carbonic anhydrase inhibitor d's mean?
Methazolamide (Generic: Neptazane) was approved by the FDA on August 28, 1996 and is manufactured by Wyeth-Ayerst. Methazolamide is prescribed to treat glaucoma, certain kinds of tremors, and mountain or altitude sickness. Methazolamide is a carbonic anhydrase inhibitor. Carbonic anhydrase is a protein in the body, and Methazolamide reduces its activity. In treating glaucoma, Methazolamide reduces the actions of carbonic anhydrase and the amount of fluid produced in the eyes, which also reduces pressure.. There have been instances of people taking Methazolamide developing Stevens Johnson Syndrome (SJS), a rare skin disease. Stevens Johnson Syndrome can cause rash, skin peeling, and sores on the mucous membranes. Stevens Johnson Syndrome is an immune-complex mediated hypersensitivity disorder that may be caused by many drugs, viral infections, and malignancies. SJS patients are often treated in burn centers due to their open wounds and risk of infection. SJS can be fatal. Many drugs that cause ...
Lutwak-Mann C, Adams CE (April 1957). "Carbonic anhydrase in the female reproductive tract. II. Endometrial carbonic anhydrase ... to possess similar potency to progesterone and hydroxyprogesterone caproate in the rabbit endometrial carbonic anhydrase test, ... 8S,9S,10R,13S,14S,17S)-17-Acetyl-10,13-dimethyl-2,7,8,9,11,12,14,15,16,17-decahydro-1H-cyclopenta[a]phenanthren-3-yl] acetate ... CC(=O)[[email protected]]1CC[[email protected]@H]2[[email protected]@]1(CC[[email protected]]3[[email protected]]2CC=C4[[email protected]@]3(CCC(=C4)OC(=O)C)C)C ...
The cause of the rapid widespread acceptance of Celebrex and Vioxx by physicians was the publication of two large trials, the ... Two of the metabolites of COX-2, prostaglandin A2 (PGA2) and A1 (PGA1), when present in high quantities bind to p53 in the ... it was discovered that prostaglandins could indeed be separated into two general classes which could loosely be regarded as " ... while prostaglandins whose synthesis involves the cyclooxygenase-II enzyme, or COX-2, are responsible for inflammation and pain ...
"Differential expression of cytoplasmic carbonic anhydrases, CA I and II, and membrane-associated isozymes, CA IX and XII, in ... "Entrez Gene: CA9 carbonic anhydrase IX".. *^ Kirkpatrick JP, Rabbani ZN, Bentley RC, Hardee ME, Karol S, Meyer J, Oosterwijk E ... Carbonic anhydrase 9 (CA9/CAIX) is an enzyme that in humans is encoded by the CA9 gene.[5][6][7] ... Nishimori I, Onishi S (2001). "Carbonic anhydrase isozymes in the human pancreas". Digestive and Liver Disease. 33 (1): 68-74. ...
Sato S, Zhu XL, Sly WS (1990). "Carbonic anhydrase isozymes IV and II in urinary membranes from carbonic anhydrase II-deficient ... "Human carbonic anhydrases and carbonic anhydrase deficiencies". Annu. Rev. Biochem. 64 (1): 375-401. doi:10.1146/annurev.bi. ... Roth DE, Venta PJ, Tashian RE, Sly WS (1992). "Molecular basis of human carbonic anhydrase II deficiency". Proc. Natl. Acad. ... Sly also identified the first inherited deficiency of a human carbonic anhydrase, CA II, and defined the biochemical and ...
Exhibits a Drug Disposition Profile in Healthy Volunteers Compatible With High Affinity to Carbonic Anhydrase-I/II: Preliminary ... It inhibits the enzymes carbonic anhydrase and COX-2. A study in healthy volunteers showed drug effects on urinary ... Hirankarn, S.; Barrett, J.S.; Alamuddin, N.; Fitzgerald, G. A.; Skarke, C. (2013). "GCG100649, A Novel Cyclooxygenase-2 ...
Functional interaction of carbonic anhydrase II and chloride/bicarbonate exchangers". J. Biol. Chem. 276 (51): 47886-94. doi: ... Vince JW, Reithmeier RA (October 1998). "Carbonic anhydrase II binds to the carboxyl terminus of human band 3, the erythrocyte ... Vince JW, Reithmeier RA (May 2000). "Identification of the carbonic anhydrase II binding site in the Cl(-)/HCO(3)(-) anion ... anion exchanger binding site to the amino-terminal region of carbonic anhydrase II". Biochemistry. 39 (44): 13344-9. doi: ...
... is a carbonic anhydrase inhibitor (specifically, carbonic anhydrase II). Carbonic anhydrase is found primarily in ... the most active of which is carbonic anhydrase II (CA-II). Use for the treatment of open-angle glaucoma and raised intraocular ... and thus exhibits carbonic anhydrase inhibitory activity (largely carbonic anhydrase-I, when in the presence of Brinzolamide) ... Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases aqueous humor secretion and thus lowers the ...
Functional interaction of carbonic anhydrase II and chloride/bicarbonate exchangers". J. Biol. Chem. 276 (51): 47886-94. doi: ... Extracellular loop 4 of the human AE1 Cl-/HCO3- exchanger binds carbonic anhydrase IV". J. Biol. Chem. 277 (28): 25239-46. doi: ... exchanger and carbonic anhydrase XIV interaction". Am. J. Physiol., Cell Physiol. 297 (5): C1091-102. doi:10.1152/ajpcell. ... Alvarez BV, Fujinaga J, Casey JR (2002). "Molecular basis for angiotensin II-induced increase of chloride/bicarbonate exchange ...
Functional interaction of carbonic anhydrase II and chloride/bicarbonate exchangers". The Journal of Biological Chemistry. 276 ... binds carbonic anhydrase II (CAII) forming a "transport metabolon" as CAII binding activates AE1 transport activity about 10 ... At least two genes encode these symporters in any one mammal. A 10 TMS model has been presented, but this model conflicts with ... Two others (AE4, SLC4A9 and BTR1, SLC4A11) are not characterized. Most, though not all, are inhibited by 4,4'- ...
Carbonic anhydrase. *CO dehydrogenase [18]. *Cytochrome c peroxidase. *Fumarase. *Superoxide dismutase. *Triosephosphate ... 62 (2): 154-9. doi:10.1021/j150560a005.. *^ a b c Eigen, Manfred; Hammes, Gordon G. (2006). "Elementary Steps in Enzyme ... 8 (2): 46. doi:10.1016/0968-0004(83)90382-1.. *^ Zhou, Guozhi; Wong, Ming-Tat; Zhou, Guo-Qiang (1983). "Diffusion-controlled ... In 1972, it was observed that in the dehydration of H2CO3 catalyzed by carbonic anhydrase, the second-order rate constant ...
Carbonic anhydrase inhibitors: binding of indanesulfonamides to the human isoform II. ... Indane-5-sulfonamide is a carbonic anhydrase inhibitor. ...
Fathallah DM, Bejaoui M, Lepaslier D, Chater K, Sly WS, Dellagi K (1997). "Carbonic anhydrase II (CA II) deficiency in ... July 1985). "Carbonic anhydrase II deficiency in 12 families with the autosomal recessive syndrome of osteopetrosis with renal ... Combined dRTA and pRTA is also observed as the result of inherited carbonic anhydrase II deficiency. Mutations in the gene ... Shah GN, Bonapace G, Hu PY, Strisciuglio P, Sly WS (September 2004). "Carbonic anhydrase II deficiency syndrome (osteopetrosis ...
... has been shown to interact with carbonic anhydrase II and CHP. It is also the target of the ... Li X, Alvarez B, Casey JR, Reithmeier RA, Fliegel L (September 2002). "Carbonic anhydrase II binds to and enhances activity of ... 275 (2 Pt 1): C431-9. PMID 9688597. Wakabayashi S, Pang T, Su X, Shigekawa M (2000). "A novel topology model of the human Na ... 56 (2): 271-80. doi:10.1016/0092-8674(89)90901-X. PMID 2536298. Mattei MG, Sardet C, Franchi A, Pouysségur J (1988). "The human ...
2005). "Molecular mechanism of kNBC1-carbonic anhydrase II interaction in proximal tubule cells". J. Physiol. 559 (Pt 1): 55-65 ... Asp988 and kNBC1-carbonic anhydrase II binding". J. Physiol. 544 (Pt 3): 679-85. doi:10.1113/jphysiol.2002.029777. PMC 2290621 ... 2003). "Direct extracellular interaction between carbonic anhydrase IV and the human NBC1 sodium/bicarbonate co-transporter". ... 57 (2): 371-84. doi:10.1046/j.1523-1755.2000.00857.x. PMID 10652014. Choi I, Romero MF, Khandoudi N, et al. (1999). "Cloning ...
"The functional and physical relationship between the DRA bicarbonate transporter and carbonic anhydrase II". American Journal ... Sandal NN, Marcker KA (January 1994). "Similarities between a soybean nodulin, Neurospora crassa sulphate permease II and a ... "Identification of seven novel mutations including the first two genomic rearrangements in SLC26A3 mutated in congenital ... 3.0.CO;2-A. PMID 9554749. Antalis TM, Reeder JA, Gotley DC, Byeon MK, Walsh MD, Henderson KW, Papas TS, Schweinfest CW (August ...
... cotransporter by carbonic anhydrase II and PKA". Am. J. Physiol., Cell Physiol. 286 (6): C1423-33. doi:10.1152/ajpcell. ... 246 (2): 535-8. doi:10.1006/bbrc.1998.8658. PMID 9610397. Pushkin A, Abuladze N, Lee I, et al. (1999). "Mapping of the human ... 277 (6 Pt 2): F974-81. PMID 10600945. Park M, Ko SB, Choi JY, et al. (2003). "The cystic fibrosis transmembrane conductance ... 57 (2): 321-2. doi:10.1006/geno.1999.5781. PMID 10198178. Pushkin A, Abuladze N, Lee I, et al. (1999). "Cloning, tissue ...
... cotransporter by carbonic anhydrase II and PKA". Am. J. Physiol., Cell Physiol. 286 (6): C1423-33. doi:10.1152/ajpcell. ... Grichtchenko II, Choi I, Zhong X, Bray-Ward P, Russell JM, Boron WF (May 2001). "Cloning, characterization, and chromosomal ... 276 (6 Pt 2): F903-13. PMID 10362779. Pushkin A, Abuladze N, Lee I, Newman D, Hwang J, Kurtz I (1999). "Cloning, tissue ... 283 (2): G473-80. doi:10.1152/ajpgi.00421.2001. PMID 12121896. Amlal H, Burnham CE, Soleimani M (1999). "Characterization of ...
Vince JW, Reithmeier RA (2000). "Identification of the Carbonic Anhydrase II Binding Site in the Cl−/HCO3− Anion Exchanger AE1 ... Bonaldo MF, Lennon G, Soares MB (1997). "Normalization and subtraction: two approaches to facilitate gene discovery". Genome ... Anion exchange protein 2 (AE2) is a membrane transport protein that in humans is encoded by the SLC4A2 gene. AE2 is ... Huang QR, Li Q, Chen YH, Li L, Liu LL, Lei SH, Chen HP, Peng WJ, He M (June 2010). "Involvement of anion exchanger-2 in ...
Parr JS, Khalifah RG (1992). "Inhibition of carbonic anhydrases I and II by N-unsubstituted carbamate esters". J Biol Chem. 267 ... The mechanism of action of methocarbamol is currently unknown, but may involve the inhibition of carbonic anhydrase. The muscle ... followed by Phase II conjugation. All the major metabolites are unhydrolyzed carbamates. Methocarbamol is marketed under ... 122 (2): 239-246. PMID 13514612. Crankshaw DP, Raper C (1968). "Some studies on peripheral actions of mephenesin, methocarbamol ...
Poulsen, S.-A.; Bornaghi, L. F. (May 2006). "Fragment-based drug discovery of carbonic anhydrase II inhibitors by dynamic ... II. Nickel(II) Complexes of Some Novel Tetradentate Ligands". Journal of the American Chemical Society. 84 (9): 1762-1763. doi: ... Metal Ion Control in the Synthesis of Planar Nickel(II) Complexes of α-Diketo-bis-mercaptoimines". Journal of the American ... Valade, A.; Urban, D.; Beau, J.-M. (Jan-Feb 2007). "Two galatosyltransferases' selection of different binders from the same ...
... make it unlikely that it has carbonic anhydrase activity. It shares properties in common with two other acatalytic CA isoforms ... Carbonic anhydrase-related protein 11 is an enzyme that in humans is encoded by the CA11 gene. Carbonic anhydrases (CAs) are a ... Check date values in: ,year= / ,date= mismatch (help) "Entrez Gene: CA11 carbonic anhydrase XI". Liao W, Xiao Q, Tchikov V, ... Bellingham J, Gregory-Evans K, Gregory-Evans CY (1998). "Sequence and tissue expression of a novel human carbonic anhydrase- ...
Some of these fused proteins have SulP homologues fused to carbonic anhydrase homologues (TC# 2.A.53.8.1). These are also ... where two subunits do not function independently. The dimeric structure probably represents the native state of SulP ... Felce, Jeremy; Saier, Milton H. (2004-01-01). "Carbonic anhydrases fused to anion transporters of the SulP family: evidence for ... SLC26A3 (2.A.53.2.3) and SLC26A6 (2.A.53.2.7 and 2.A.53.2.8) can function as carriers or channels, depending on the transported ...
... is a carbonic anhydrase inhibitor, hence causing the accumulation of carbonic acid. Carbonic anhydrase is an ... Other carbonic anhydrase inhibitors - potential for additive inhibitory effects on carbonic anhydrase and hence potential for ... The enzyme carbonic anhydrase is found here, allowing the reabsorption of bicarbonate, sodium, and chloride. By inhibiting this ... Larsen, D. "Carbonic Anhydrase 2". UC Davis Chemwiki. University of California. Retrieved 10 April 2014. "Archived copy" (PDF ...
... and kinetic characterization of active-site histidine as a proton shuttle in catalysis by human carbonic anhydrase II". ... An example of an enzyme that contains a cofactor is carbonic anhydrase, which is shown in the ribbon diagram above with a zinc ...
One gene is carbonic anhydrase II (CAII), which, when mutated, causes osteopetrosis with renal tubular acidosis(type 3) {Sly, ... "Carbonic anhydrase II deficiency identified as the primary defect in the autosomal recessive syndrome of osteopetrosis with ... A stoichiometry of two protons translocated for each ATP hydrolyzed has been proposed by (Johnson, 1982). In addition to the ... It has been shown how the V-ATPase structure of the ancestral form consisting of two different proteins evolves into the fungi ...
The differences in tissue distribution suggest that the two mitochondrial carbonic anhydrases evolved to assume different ... Carbonic anhydrase 5B, mitochondrial is an enzyme that in humans is encoded by the CA5B gene. Carbonic anhydrases (CAs) are a ... Sly WS, Hu PY (1995). "Human carbonic anhydrases and carbonic anhydrase deficiencies". Annu. Rev. Biochem. 64: 375-401. doi: ... "Entrez Gene: CA5B carbonic anhydrase VB, mitochondrial". Human CA5B genome location and CA5B gene details page in the UCSC ...
carbonic anhydrase (chloride shift). *oxyhemoglobin. *respiratory quotient. *arterial blood gas. *diffusion capacity (DLCO) ...
An enzyme, carbonic anhydrase, located within the carboxysome releases CO2 from the dissolved hydrocarbonate ions (HCO−. 3). ... Two water molecules are oxidized by four successive charge-separation reactions by photosystem II to yield a molecule of ... whose electrons come from electron transport through photosystem II. Photosystem II, as the first step of the Z-scheme, ... Photosynthesis occurs in two stages. In the first stage, light-dependent reactions or light reactions capture the energy of ...
... In: Beilstein Journal of Organic Chemistry, Vol. 11: pp. 1129-1135 ... Aryl sulfonamides are a widely used drug class for the inhibition of carbonic anhydrases. In the context of our program of ... in the exploration of azobenzene-containing sulfonamides to block the catalytic activity of human carbonic anhydrase II (hCAII ...
Kinetically Selective Inhibitors of Human Carbonic Anhydrase Isozymes I, II, VII, IX, XII, and XIII.. Talibov VO1, Linkuvienė V ... To get a better understanding of the possibility of developing selective carbonic anhydrase (CA) inhibitors, interactions ... Carbonic Anhydrase Inhibitors/chemical synthesis. *Carbonic Anhydrase Inhibitors/chemistry. *Carbonic Anhydrase Inhibitors/ ... between 17 benzenesulphonamide ligands and 6 human CAs (full-length CA I, II, VII, and XIII and catalytic domains of CA IX and ...
Carbonic Anhydrase Isozyme II human, ≥80%, powder, ≥3,000 W-A units/mg protein pricing ... Human carbonic anhydrase (CA) I and II are cytosolic proteins, where their expression disorders can cause diseases such as ... Intrinsic thermodynamics of sulfonamide inhibitor binding to human carbonic anhydrases I and II.. [Vaida Morkūnaitė, Joana ... Intrinsic thermodynamic binding parameters to CA I and II were determined for such widely studied drugs as acetazolamide, ...
... can manifest in carriers of point mutations in the human carbonic anhydrase II (HCA II) gene. We have over the past 10-15 years ... is caused by autosomal recessive mutations in the human carbonic anhydrase II (HCA II) gene. Here we report a small-molecule ... misfolding and aggregation of the enzyme human carbonic anhydrase II. In summary our HCA II folding studies have shown that the ... Small-Molecule Suppression of Misfolding of Mutated Human Carbonic Anhydrase II Linked to Marble Brain Disease. Almstedt, Karin ...
Carbonic anhydrase I/II hydrates carbon dioxide (Canis familiaris) Carbonic anhydrase I/II hydrates carbon dioxide (Danio rerio ... Carbonic anhydrase I/II hydrates carbon dioxide (Rattus norvegicus) Carbonic anhydrase I/II hydrates carbon dioxide (Sus scrofa ... Carbonic anhydrase I/II hydrates carbon dioxide (Bos taurus) Carbonic anhydrase I/II hydrates carbon dioxide (Caenorhabditis ... Carbonic anhydrase I/II hydrates carbon dioxide (Mus musculus) Carbonic anhydrase I/II hydrates carbon dioxide (Plasmodium ...
Carbonic Anhydrase II in Complex With Furosemide As Sulfonamide Inhibitor ... The binding sites of Zinc atom in the structure of Carbonic Anhydrase II in Complex With Furosemide As Sulfonamide Inhibitor ( ... Zinc in the structure of Carbonic Anhydrase II in Complex With Furosemide As Sulfonamide Inhibitor (pdb 1z9y). ... Zinc binding site 2 out of 2 in 1z9y. Click to enlarge. Click to enlarge. Mono- and Stereo- picture of 5.0 Angstrom ...
Carbonic anhydrase 2 - Also known as CAH2_HUMAN, CA2. Essential for bone resorption and osteoclast differentiation (By ... USE OF CARBONIC ANHYDRASE II, IX ACTIVE-SITE MIMIC, FOR THE PURPOSE OF SCREENING INHIBITORS FOR POSSIBLE ANTI-CANCER PROPERTIES ...
Carbonic Anhydrase II (CAII) deficiency osteopetrosis variant. *Creatinine clearance ≤ 40ml/min/1.73m^2 or RTA ... Cyclosporin A 1.5 mg/kg/day iv from -2, then 3 mg/kg/day iv (from +7 in PBSCT and +11 in BMT or UCBT) then 9 mg/kg/day po ... 10 mg/m^2 iv day +1 then 6 mg/m^ iv day +3 and +6 (Not for UCBT) ...
... can manifest in carriers of point mutations in the human carbonic anhydrase II (HCA II) gene. We have over the past 10-15 years ... can manifest in carriers of point mutations in the human carbonic anhydrase II (HCA II) gene. One mutation associated with MBS ... misfolding and aggregation of the enzyme human carbonic anhydrase II. In summary our HCA II folding studies have shown that the ... The rare disease marble brain disease (MBD) also known as carbonic anhydrase II deficiency syndrome (CADS) ...
Find out information about Carbonic anhydrase iv. An enzyme which aids carbon dioxide transport and release by catalyzing the ... synthesis, and the dehydration, of carbonic acid from, and to, carbon dioxide... Explanation of Carbonic anhydrase iv ... Related to Carbonic anhydrase iv: Carbonic anhydrase inhibitor, Carbonic anhydrase ii, carbonic anhydrase IX ... Carbonic Anhydrase. (redirected from Carbonic anhydrase iv). Also found in: Dictionary, Medical. ...
We sought to determine whether carbonic anhydrase inhibition with acetazolamide would prevent CO2-mediated inhibition of LPS- ... We sought to determine whether carbonic anhydrase inhibition with acetazolamide would prevent CO2-mediated inhibition of LPS- ... We sought to determine whether carbonic anhydrase inhibition with acetazolamide would prevent CO2-mediated inhibition of LPS- ... We sought to determine whether carbonic anhydrase inhibition with acetazolamide would prevent CO2-mediated inhibition of LPS- ...
The two agents differ in their anticonvulsant effect in mice ; antagonism by reserpine is insurmountable by carbonic anhydrase ... THE ANTICONVULSANT ACTION OF CARBON DIOXIDE: INTERACTION WITH RESERPINE AND INHIBITORS OF CARBONIC ANHYDRASE. WILLIAM D. GRAY ... THE ANTICONVULSANT ACTION OF CARBON DIOXIDE: INTERACTION WITH RESERPINE AND INHIBITORS OF CARBONIC ANHYDRASE. WILLIAM D. GRAY ... THE ANTICONVULSANT ACTION OF CARBON DIOXIDE: INTERACTION WITH RESERPINE AND INHIBITORS OF CARBONIC ANHYDRASE. WILLIAM D. GRAY ...
Carbonic anhydrase B is one of the two major forms of carbonic anhydrase in human red blood cell (the other form is CA C). Like ... Structure of human erythrocyte Carbonic anhydrase B. Like all other forms of carbonic anhydrase, CA B. consists of protein and ... Biological importance of human erythrocyte Carbonic anhydrase B. Carbonic anhydrases are abundant in mammalian tissues, plants ... Human erythrocyte Carbonic anhydrase (CA) B is a type of α-CA that is present in the blood [2]. This paper discusses the ...
Carbonic anhydrase IX expression in renal neoplasms: Correlation with tumor type and grade. American Journal of Clinical ... Carbonic anhydrase IX expression in renal neoplasms : Correlation with tumor type and grade. In: American Journal of Clinical ... Carbonic anhydrase IX expression in renal neoplasms : Correlation with tumor type and grade. / Genega, Elizabeth M.; ... abstract = "Carbonic anhydrase IX (CAIX), a hypoxia-induced protein, is expressed in some renal tumors. We evaluated its ...
... is caused by mutations in the gene coding for carbonic anhydrase II, CA2. CA2 catalyzes the formation of protons in the ... Typically 2 to 4 weeks from receipt of a sample in the laboratory. All cases involving ongoing pregnancies will be expedited. ... Osteoclast-poor forms of autosomal recessive osteopetrosis, types 2 and 7 respectively, are caused by mutations in either the ...
... is caused by mutations in the gene coding for carbonic anhydrase II, CA2. CA2 catalyzes the formation of protons in the ... Typically 2 to 4 weeks from receipt of a sample in the laboratory. All cases involving ongoing pregnancies will be expedited. ... Fibroblasts: 2 confluent T-25 flasks. *Saliva: only samples collected in Oragene DNA Self-Collection Kit or Oragene Saliva ... Osteoclast-poor forms of autosomal recessive osteopetrosis, types 2 and 7 respectively, are caused by mutations in either the ...
PubMed] [14] Pastorekova S, Zavadova Z, Kostal M, Babusikova O, Zavada J. A Book Quasi-viral Agent, MaTu, is normally a Two- ... Carbonic anhydrase IX (CAIX) is generally expressed in individual tumors and. Carbonic anhydrase IX (CAIX) is generally ... Carbonic Anhydrase IX Appearance, a Book Surrogate Marker of Tumor Hypoxia, Is normally Associated with an unhealthy Prognosis ... Immunohistochemistry of Carbonic Anhydrase Isozyme IX (MN/CA IX) in Individual Gut Reveals Polarized Appearance in Epithelial ...
Please note if your account is within the State of California two of these pieces of identification will be required.. VWR will ... Carbonic Anhydrase III Overexpression Lysate (Adult Normal), Novus Biologicals (NBL1-08616). Carbonic Anhydrase III ... 2. Publish, post, upload, distribute or disseminate any inappropriate, profane, defamatory, infringing, obscene, indecent or ... 2) terminate any users access to all or part of the Web Site. However, the Company can neither review all material before it ...
Type II),Causes of PRTA, Clinical Features and Symptoms of PRTA, Diagnosis and treatment of PRTA,Prognosis of PRTA ... Carbonic anhydrase enzyme is inhibited, defective or there is associated Fanconi syndrome.Proximal Renal Tubular Acidosis (Type ... Type II RTA is less common than Type I RTA. Type II most often occurs during infancy and may go away by itself. ... Type II), Proximal RTA Type II, proximal tubule, Sjogren syndrome, Symptoms of PRTA, Treatment for PRTA ...
Expression of another hypoxia inducible CA isoform, CAXII, was upregulated in 3D but not two-dimensional culture in response to ... including carbonic anhydrase IX (CAIX), in response to bevacizumab treatment in xenografts. CAIX expression correlates with ... Carbonic Anhydrase IX, Carbonic Anhydrases, Cell Line, Tumor, Cell Proliferation, Female, Gene Knockdown Techniques, ... Carbonic anhydrase IX promotes tumor growth and necrosis in vivo and inhibition enhances anti-VEGF therapy. ...
Carbonic anhydrase inhibition selectively prevents amyloid β neurovascular mitochondrial toxicity. Aging Cell. 2018 Aug 1;17(4 ... Carbonic anhydrase inhibition selectively prevents amyloid β neurovascular mitochondrial toxicity. In: Aging Cell. 2018 ; Vol. ... Solesio, ME, Peixoto, PM, Debure, L, Madamba, SM, de Leon, MJ, Wisniewski, T, Pavlov, E & Fossati, S 2018, Carbonic anhydrase ... Carbonic anhydrase inhibition selectively prevents amyloid β neurovascular mitochondrial toxicity. María E. Solesio, Pablo M. ...
Methazolamides inhibitory action on carbonic anhydrase decreases the secretion of aqueous humor and results in a decrease in ... The onset of the decrease in intraocular pressure generally occurs within two to four hours, has a peak effect in six to eight ... Methazolamide is a potent inhibitor of carbonic anhydrase.. Methazolamide is well absorbed from the gastrointestinal tract. ... coma and death have been reported with concomitant use of high-dose aspirin and carbonic anhydrase inhibitors (see WARNINGS). ...
... with RTA is associated with carbonic anhydrase type 2 (CA2) mutations. No mutations were detected in CA2 or any other genes ... CLC-7 mutations are known to cause autosomal dominant OPT type 2, also called Albers-Schonberg disease, which is characterized ... with RTA is associated with carbonic anhydrase type 2 (CA2) mutations. No mutations were detected in CA2 or any other genes ... CLC-7 mutations are known to cause autosomal dominant OPT type 2, also called Albers-Schonberg disease, which is characterized ...
Belongs to a class of drugs called carbonic anhydrase inhibitors.. Brand Name(s): Neptazane. There may be other brand names for ... You should not use two doses at the same time.. How to Store and Dispose of This Medicine: *Store at room temperature, away ...
The carbonic anhydrase inhibitors act by a noncompetitive, reversible inhibition of the enzyme carbonic anhydrase. This reduces ... This medication, a type of carbonic anhydrase inhibitor, works by lowering pressure in the eye, called aintraocular pressure, ... coma and death have been reported with concomitant use of high-dose aspirin and carbonic anhydrase inhibitors. Precautions: ... If a dose is missed, give it as soon as you remember but do not give 2 doses at once. Only give Methazolamide Tablets to the ...
  • To get a better understanding of the possibility of developing selective carbonic anhydrase (CA) inhibitors, interactions between 17 benzenesulphonamide ligands and 6 human CAs (full-length CA I, II, VII, and XIII and catalytic domains of CA IX and XII) were characterized using surface plasmon resonance and fluorescent-based thermal shift assays. (nih.gov)
  • Antiangiogenic therapy induces hypoxia and we observed increased expression of hypoxia-regulated genes, including carbonic anhydrase IX (CAIX), in response to bevacizumab treatment in xenografts. (ox.ac.uk)
  • Expression of another hypoxia inducible CA isoform, CAXII, was upregulated in 3D but not two-dimensional culture in response to CAIX knockdown. (ox.ac.uk)
  • We previously showed that incubation in carbon dioxide (CO 2 ), but not air or helium (He), markedly decreased macrophage intracellular pH (pH i ) and resulted in reversible inhibition of lipopolysaccharide- (LPS) stimulated tumor necrosis factor (TNF) and interleukin-1 release. (elsevier.com)
  • Both MTZ and ATZ prevented mitochondrial membrane depolarization and H 2 O 2 generation, with no effects on intracellular pH or ATP production. (elsevier.com)
  • Therefore, the zinc ion has a distorted tetrahedral coordination [2]. (libretexts.org)
  • In fact, it is zinc-aquo complex (rather than zinc ion alone) that needs to be present in the active site for the catalytic functionality of the enzyme [2]. (libretexts.org)
  • Note that the carbonic acid (H 2 CO 3 ) and hydrogen carbonate ions (HCO 3 - ) is an important buffer system in the body. (libretexts.org)
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