• Structural aspects of isozyme selectivity in the binding of inhibitors to carbonic anhydrases II and IV. (proteopedia.org)
  • Carbonic anhydrase inhibitors: binding of an antiglaucoma glycosyl-sulfanilamide derivative to human isoform II and its consequences for the drug design of enzyme inhibitors incorporating sugar moieties. (expasy.org)
  • Carbonic anhydrase (CA) inhibitors are active over a number of CA isozymes. (guidetopharmacology.org)
  • The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. (guidetopharmacology.org)
  • 2013) Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety. (guidetopharmacology.org)
  • 2009) Carbonic anhydrase inhibitors. (guidetopharmacology.org)
  • Dual carbonic anhydrase--cyclooxygenase-2 inhibitors. (ageless.co.za)
  • I had a look at the hits on PDB, and a huge number are of inhibitors of CA. I searched for 'Carbonic Hydrase Inhibitors' and found a short piece on this topic on NCBI Bookshelf that starts: 'Carbonic anhydrase inhibitors are a medication used to manage and treat glaucoma, idiopathic intracranial hypertension, altitude sickness, congestive heart failure, and epilepsy, among other diseases. (stackexchange.com)
  • In this study we have examined the ability of a series of steroidal and non-steroidal sulphamates (originally developed as steroid sulphatase inhibitors) and related compounds to inhibit human CAII (hCAII) activity in vitro. (ox.ac.uk)
  • These studies and initial results with docking to the crystal structure of the extracellular domain of hCAXII indicate that the STS sulphamate ester inhibitors should also be interesting candidates to pursue as inhibitors of CA isozymes that are over-expressed in human tumours. (ox.ac.uk)
  • A series of sulfenimide derivatives (1a-i) were investigated as inhibitors of human (hCA-I, hCA-II) and bovine (bCA) carbonic anhydrase enzymes. (ogu.edu.tr)
  • Results of our study will make valuable contributions to carbonic anhydrase inhibition studies for further investigations since inhibitors of this enzyme are important molecules for medicinal chemistry. (ogu.edu.tr)
  • Comment: Carbonic anhydrase inhibitors (CAIs) and salicylates inhibit each other's renal tubular secretion, resulting in increased plasma levels. (medscape.com)
  • The protein encoded by this gene is one of several isozymes of carbonic anhydrase, which catalyzes reversible hydration of carbon dioxide. (nih.gov)
  • CA2 is one of several (at least 7) isozymes of carbonic anhydrase. (thermofisher.com)
  • Inhibitor (green) bound in the active site of carbonic anhydrase. (rcsb.org)
  • Dorzolamide HCl is a water-soluble, potent inhibitor of human carbonic anhydrase II and IV with Ki of 1.9 nM and 31 nM, respectively, used as anti-glaucoma agent. (abmole.com)
  • Acetazolamide is a carbonic anhydrase (CA) IX inhibitor with an IC50 of 30 nM. (abmole.com)
  • Dichlorphenamide is a sulfonamide and a carbonic anhydrase inhibitor of the meta-Disulfamoylbenzene class. (abmole.com)
  • Tioxolone is a metalloenzyme carbonic anhydrase I inhibitor with a Ki of 91 nM. (abmole.com)
  • U-104 is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with K i of 45.1 nM and 4.5 nM, respectively, very low inhibition for CA I and CA II. (abmole.com)
  • Methazolamide is a carbonic anhydrase inhibitor with K i of 50 nM, 14 nM and 36 nM for hCA I, hCA II and bCA IV isoforms, respectively. (abmole.com)
  • Ethoxzolamide is an inhibitor of the metalloenzyme carbonic anhydrase, which inhibits hCA I, hCA II, hCA IV, hCA VI and hCA VII with K i of 25 nM, 8 nM, 93 nM, 43 nM and 0.8 nM, respectively. (abmole.com)
  • hCAI/II-IN-6 is an orally active human carbonic anhydrase (CA) inhibitor. (abmole.com)
  • Sultiame is a carbonic anhydrase inhibitor, widely used as an antiepileptic agent. (abmole.com)
  • EMAC10101d is a potent and selective toward hCA II inhibitor, with a Ki of 8.1 nM. (abmole.com)
  • Benzenesulfonamide ia an inhibitor of carbonic anhydrases. (abmole.com)
  • The bromo derivative (1f) was found to be strongest inhibitor of all three enzymes with KI values of 0.023, 0.044 and 20.57 µM for hCA-I, hCA-II and bCA, respectively. (ogu.edu.tr)
  • Two transcript variants encoding different isoforms have been found for this gene. (nih.gov)
  • Inhibition of various human carbonic anhydrase isoforms (I, II, IX and XII) was tested with the 'cold', non-radiolabelled complexes, and compared with an acetazolamide standard (AZA). (bath.ac.uk)
  • hCAI/II-IN-6 selectively inhibits hCA II and hCA VII isoforms with Ki values of 220, 4.9, 6.5 and >50000 nM for hCA I, hCA II , hCA VII and hCA XII respectively. (abmole.com)
  • All derivatives except for the methyl derivative (1b) exhibited effective inhibitory action at low micromolar concentrations on human isoforms, but only four derivatives (1e, 1f, 1h, 1i) inhibited the bovine enzyme. (ogu.edu.tr)
  • Carbonic anhydrase catalyzes reversible hydration of carbon dioxide. (wikipedia.org)
  • Carbonic anhydrase, a zinc metalloenzyme, catalyzes the reversible hydration of carbon dioxide to bicarbonate. (rcsb.org)
  • In the CO 2 -hydration direction, the first step of catalysis is the conversion of CO 2 into HCO 3 − via the nucleophilic attack of a zinc-bound hydroxide. (iucr.org)
  • Carbonic anhydrase catalyzes cyanamide hydration to urea: is it mimicking the physiological reaction? (proteopedia.org)
  • Carbonic anhydrase 2 (CAII) supports tumor blood endothelial cell survival under lactic acidosis in the tumor microenvironment. (nih.gov)
  • Girentuximab (G250) is a chimeric monoclonal antibody that binds carbonic anhydrase IX (CAIX), a cell surface glycoprotein ubiquitously expressed in clear cell renal cell carcinoma (ccRCC). (abmole.com)
  • The following product was used in this experiment: Carbonic Anhydrase II Recombinant Rabbit Monoclonal Antibody (ARC1451) from Thermo Fisher Scientific, catalog # MA5-38188, RRID AB_2898105. (thermofisher.com)
  • Samples were incubated with Carbonic Anhydrase II Monoclonal antibody (Product # MA5-38188) using a dilution of 1:1,000, followed by HRP Goat Anti-Rabbit IgG (H+L) at a dilution of 1:10,000. (thermofisher.com)
  • Carbonic Anhydrase is a zinc-containing enzyme that catalyzes the reversible conversion of carbon dioxide to bicarbonate. (sigmaaldrich.com)
  • Carbonic anhydrases are metalloenzymes since most active sites contain zinc. (sigmaaldrich.com)
  • The second step involves the transfer of a proton from the zinc-bound water to bulk solvent, regenerating the zinc-bound hydroxide (equation 2, where B stands for a general base: either a water or a proton-shuttling residue). (iucr.org)
  • The carbonic anhydrases (or carbonate dehydratases) are classified as metalloenzyme for its zinc ion prosthetic group and form a family of enzymes that catalyze the rapid interconversion of carbon dioxide and water to bicarbonate and protons, a reversible reaction that takes part in maintaining acid-base balance in blood and other tissues. (assaygenie.com)
  • This seems surprising to me, as carbonic anhydrase is a zinc-containing enzyme which catalyses a really simple reaction, and doesn't seem to be part of any key signalling pathways. (stackexchange.com)
  • Product C7749, Bovine carbonic anhydrase II (CA II), has been widely used as a model protein in the investigation of the protein folding process. (sigmaaldrich.com)
  • However, here we show that the truncated protein identified by MAB8051 in cancer cell lines is carbonic anhydrase II (CA II), also implicated in tumour biology . (bvsalud.org)
  • Functionalization of the foldamers by a nanomolar ligand of human carbonic anhydrase II (HCA) ensured that they would be held in close proximity to the protein surface. (proteopedia.org)
  • Lyophilized proteins are stable for up to 12 months when stored at -20 to -80°C. Reconstituted protein solution can be stored at 4-8°C for 2-7 days. (assaygenie.com)
  • Lipid-specific oligomerization of the Marburg virus matrix protein VP40 is regulated by two distinct interfaces for virion assembly. (uci.edu)
  • Here we describe the 3.2 Å cryo-EM structure of human DEC-205, thereby illuminating the structure of the mannose receptor protein family. (uci.edu)
  • a 31 kDa protein band was determined which reacted with a rabbit polyclonal antibody specific for rat CA-II in Western blot analysis. (openrespiratorymedicinejournal.com)
  • The immunoreactive 31 kDa CA-II protein was detected and quantified by laser scanner densitometry using 125 I-rProtein A as a tracer. (openrespiratorymedicinejournal.com)
  • Why are there so many carbonic anhydrase structures in the Protein Data Bank? (stackexchange.com)
  • I've been looking through PDB - the Protein Data Bank - and I noticed that the protein with the most structures is human carbonic anhydrase II ( UniProt: P00918 ), with over a thousand X-ray structures. (stackexchange.com)
  • Endosialin is classified as a C-type lectin-like protein and shares both sequence and structural homology with thrombomodulin (CD141) and complement receptor C1qRp (CD93) [ 2 ]. (hindawi.com)
  • For a deeper look at carbonic anhydrase from a genomic perspective, please visit the Protein of the Month feature at the European Bioinformatics Institute. (rcsb.org)
  • For -lactalbu- min, only water molecules conserved in the human and baboon structures are shown (the structure of the bovine protein has not been reported). (lu.se)
  • ER protein determinations were performed using two-thirds of all breast cancers are ER at the time of diagnosis, the standard methods in the routine clinical laboratory (9). (lu.se)
  • Loss of carbonic anhydrase activity in bones impairs the ability of osteoclasts to promote bone resorption, leading to osteopetrosis. (wikipedia.org)
  • Although human osteopetrosis is a heterogeneous disorder encompassing different molecular lesions and a range of clinical features, all forms share a single pathogenic nexus in the osteoclast. (medscape.com)
  • The classification of osteopetrosis shown above is purely clinical and must be supplemented by the molecular insights gained from animal models (see Table 2, in Etiology). (medscape.com)
  • In this research, we determined the inhibition property of rosmarinic acid on carbonic anhydrase isoenzymes I and II (hCA I and II) puri ed from human erythrocytes by using Sepharose-4B a nity column chromatography. (gumushane.edu.tr)
  • hCA I and II isoenzymes were obtained with a yield of 57.9% and 67.2% and 76.5- and 509.3-fold puri cation of each isoenzyme, respectively. (gumushane.edu.tr)
  • In vitro inhibition of both hCA I and II isoenzymes by rosmarinic acid using CO2 -esterase activity gave Ki values of 86.0 M and 57.0 M, respectively. (gumushane.edu.tr)
  • Renal carbonic anhydrase allows the reabsorption of bicarbonate ions in the proximal tubule. (wikipedia.org)
  • Human SLC4A1/AE1 mutations cause either the erythroid disorders spherocytic haemolytic anaemia or ovalocytosis, or distal renal tubular acidosis. (tcdb.org)
  • Anmäl er till eftersitsen senast måndagen den 20/2 genom e-mail till anita.hoang ´at´ chem.lu.se. (lu.se)
  • and sodium-potassium ATPase transporter (ATP1A1), sodium-bicarbonate transporter (NBC), and carbonic anhydrase II (CA2) increased 5- to 10-fold. (unboundmedicine.com)
  • An enzyme present in red blood cells, carbonic anhydrase, aids in the conversion of carbon dioxide to carbonic acid and bicarbonate ions. (rcsb.org)
  • In both land and water plants, carbonic anhydrase plays a role in converting bicarbonate ions back to carbon dioxide for photosynthesis. (rcsb.org)
  • Seawater calcium reacts with the bicarbonate produced by carbonic anhydrase from the coral polyps, forming calcium carbonate. (rcsb.org)
  • Carbonic anhydrase is an enzyme that assists rapid inter-conversion of carbon dioxide and water into carbonic acid, protons and bicarbonate ions. (rcsb.org)
  • Since this enzyme produces and uses protons and bicarbonate ions, carbonic anhydrase plays a key role in the regulation of pH and fluid balance in different parts of our body. (rcsb.org)
  • Bovine carbonic anhydrase II (CA II) is a cytosolic, single-chain, approximately 29 kDa enzyme. (sigmaaldrich.com)
  • Here, a systematic approach to investigate the effect of an active-site-residue mutation on a model enzyme, human carbonic anhydrase II (CA II), is described. (iucr.org)
  • In this study, we describe the effect of a single amino-acid variation on a prototypical enzyme, human carbonic anhydrase II (CA II), by correlating its high-resolution reaction-intermediate structures with the measured kinetic parameters. (iucr.org)
  • Activation of isozymes I, II, IV, VA, VII, and XIV with l- and d-histidine and crystallographic analysis of their adducts with isoform II: engineering proton-transfer processes within the active site of an enzyme. (guidetopharmacology.org)
  • Although these reactions can occur even without the enzyme, carbonic anhydrase can increase the rate of these conversions up to a million fold. (rcsb.org)
  • This ancient enzyme has three distinct classes (called alpha, beta and gamma carbonic anhydrase). (rcsb.org)
  • Carbonic anhydrase from mammals belong to the alpha class, the plant enzymes belong to the beta class, while the enzyme from methane-producing archaea that grow in hot springs forms the gamma class. (rcsb.org)
  • 4lp6 is a 2 chain structure with sequence from Homo sapiens . (proteopedia.org)
  • Thyroxine modifies expressions of KSPG synthesis and carbonic anhydrase genes. (unboundmedicine.com)
  • Immunohistochemical localization of human carbonic anhydrase isoenzyme C.". Histochemistry. (wikipedia.org)
  • Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. (guidetopharmacology.org)
  • 2 However, patients who develop a syndrome of raised ICP triggered by certain medications or who are found to have cerebral transverse venous sinus stenoses (not thrombosis) are still conventionally classified as having 'IIH' ( figure 1 ). (bmj.com)
  • HIV, severe focused on mammals because of the frequency and sever- acute respiratory syndrome) suggest that targeted surveil- ity of previously reported mammal-borne zoonoses and lance efforts should focus on activities that bring humans because of the frequent close association between humans and wildlife in close contact ( 1,3 ). (cdc.gov)
  • Carbonic anhydrases are widely distributed in plant and animal tissues where they are involved in diverse physiological processes, such as photosynthesis, pH homeostasis, calcification, and bone resorption. (sigmaaldrich.com)
  • CAH2_HUMAN Essential for bone resorption and osteoclast differentiation (By similarity). (proteopedia.org)
  • Carbon Dioxide Sensing by Immune Cells Occurs through Carbonic Anhydrase 2-Dependent Changes in Intracellular pH. (nih.gov)
  • Figure 1-figure supplement 2 demonstrates that the operon beginning with acRAF indeed encodes a functional inorganic carbon transporter. (elifesciences.org)
  • Carbon dioxide diffuses out of cells and is transported in blood in a few different ways: less than 10% dissolves in the blood plasma, about 20% binds to hemoglobin, while the majority of it (70%) is converted to carbonic acid to be carried to the lungs. (rcsb.org)
  • As HCO 3 − can diffuse through the proteinaceous carboxysome shell but CO 2 cannot 5 , carbonic anhydrase generates high concentrations of CO 2 for carbon fixation by Rubisco 6 . (nature.com)
  • The reference range of the partial pressure of carbon dioxide (pCO 2 ) of arterial blood is 35-45 mm Hg. (medscape.com)
  • Proton Transfer in A THR200HIS Mutant of Human Carbonic Anhydrase II Proteins V. 61 239 2005 . (atomistry.com)
  • The carbonic anhydrasekl (CA) family consists of at least 11 enzymatically active members and a few inactive homologous proteins. (assaygenie.com)
  • In humans, the AE family (also called the SLC4 family) is composed of 10 paralogous members, among which are the proteins that perform Na + -independent Cl-HCO 3 - exchange (e.g. (tcdb.org)
  • Total RNA from tumors the expression of thousands of genes (3) to address complex questions was isolated using two successive rounds of Trizol. (lu.se)
  • Explore the normal functions of human genes and the health implications of genetic changes. (medlineplus.gov)
  • As it relies only on the well-founded assumption that catalysis with CO 2 and O 2 substrates are mutually exclusive, this mechanism should function for any rubisco. (elifesciences.org)
  • In addition to this mechanism, chemical carcinogenesis in experimental fashions may be divided into no less than three levels termed initiation, promotion, and development (Figure eleven [url=https://collegegate.org/lab/order-femara-online-no-rx/] menstruation every two weeks causes order 2.5mg femara visa[/url]. (ehd.org)
  • 2-7 This imperfect nomenclature will need to be revised as our understanding of the aetiology and pathophysiology of IIH improves. (bmj.com)
  • Mammalian carbonic anhydrases occur in about 10 slightly different forms depending upon the tissue or cellular compartment they are located in. (rcsb.org)
  • PDB entries 1ca2 , 1ddz and 1thj , shown here from top to bottom, are examples of the alpha, beta and gamma carbonic anhydrase enzymes, respectively. (rcsb.org)
  • While most carbonic anhydrase isozymes are soluble and secreted, some are bound to the membranes of specific epithelial cells. (rcsb.org)
  • Gastrointestinal absorption of soluble lead salts in adult humans can be high during fasting (40-50%), but is about 3-15% when ingested with food. (cdc.gov)
  • A single missense mutation allows AE1 to mediate both electrogenic SO 4 2- -Cl - exchange or electroneutral, H + -independent SO 4 2- -SO 4 2- exchange ( Alper 2006 ). (tcdb.org)
  • Here, we report previously undescribed structures of HCAII:CO(2) and HCAII:HCO(3)(-) complexes, together with a 3D molecular film of the enzymatic reaction observed successively in the same crystal after extended exposure to X-ray. (rcsb.org)
  • Furthermore, the CO 2 concentration inside the leaf is typically measured to be lower than ambient due to a balance of stomatal conductance and CO 2 fixation by rubisco itself ( Caemmerer and Evans, 1991 ). (elifesciences.org)
  • AIHA ERPG-2 (maximum airborne concentration below which it is believed that nearly all persons could be exposed for up to 1 hour without experiencing or developing irreversible or other serious health effects or symptoms that could impair their abilities to take protective action) = 25 ppm. (cdc.gov)
  • 3. Tanini D, Capperucci A, Supuran CT, Angeli A. (2019) Sulfur, selenium and tellurium containing amines act as effective carbonic anhydrase activators. (guidetopharmacology.org)
  • Primary structure of human carbonic anhydrase C." J. Biol. (wikipedia.org)
  • 1972) Nat New Biol 235:131-137], but a structure of an HCAII in complex with CO(2) or HCO(3)(-) has remained elusive. (rcsb.org)
  • Primary cutaneous signet-ring cell melanoma: a clinico-pathologic and immunohistochemical research of two circumstances Am J Dermatopathol. (ehd.org)
  • Fluorometholone acetate potently inhibits carbonic anhydrase (CA) with IC50s of 2.18 μM and 17.5 μM for hCA-I and hCA-II, respectively. (abmole.com)
  • More than 100 distinct human carbonic anhydrase II (HCAII) 3D structures have been generated in last 3 decades [Liljas A, et al. (rcsb.org)
  • Fig. 1 Crystal structures of human -lactal- bumin (PDB file 1HML), lysozyme (2LZT) and ribonuclease A (7RSA) showing potentially long-lived internal water molecules, disul- fide bonds (yellow), and the Ca2+ ion (green) in -lactalbumin. (lu.se)
  • Specific point mutations in human anion exchanger 1 (AE1) convert this electroneutral anion exchanger into a monovalent cation conductance. (tcdb.org)
  • Endosialin, also known as Tumor Endothelial Marker-1 (TEM-1) or CD248, was first described as a vascular endothelial cell surface antigen in human fetal fibroblasts [ 1 ]. (hindawi.com)
  • Studies have identified pericytes and reactive fibroblasts, two essential cell types required for tumor survival and growth, as the major sites of expression of endosialin. (hindawi.com)
  • D ) Rubiscos found in bacteria with a carboxysome CCM typically have relatively low CO 2 specificities (S C/O ≈ 50) and fast maximum carboxylation rates relative to other Form I rubiscos (k cat,C ≈ 10 s −1 ). (elifesciences.org)
  • In humans, three distinct clinical forms of the disease-infantile, intermediate, and adult onset-are identified based on age and clinical features. (medscape.com)
  • Using in vitro and cellular techniques, we present a mVP40 assembly model highlighting two distinct oligomerization interfaces: the (N-terminal domain (NTD) and C-terminal domain (CTD)) in mVP40. (uci.edu)
  • As such, Form II rubiscos do not perform well in ambient CO 2 and O 2 concentrations. (elifesciences.org)
  • Carbonic Anhydrase II bovine has been used as a control in native gel electrophoresis and X-ray absorption spectroscopy characterization of Thalassiosira weissflogii carbonic anhydrase 1. (sigmaaldrich.com)