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carbonic anhydrase

Samuele Cazzamalli, Alberto Dal Corso, Fontaine Widmayer, Dario Neri
We present the first direct comparative evaluation of an antibody-drug conjugate and of a small molecule-drug conjugate for cancer therapy, using chemically-defined products which bind with high-affinity to carbonic anhydrase IX, a marker of tumor hypoxia and of renal cell carcinoma.
January 17, 2018: Journal of the American Chemical Society
Paresh Deshpande, Ashwin Dapkekar, Manoj Oak, Kishore Paknikar, Jyutika Rajwade
BACKGROUND: Wheat is the staple food for most of the world's population; however, it is a poor source of zinc. Foliar fertilization of zinc via zinc loaded chitosan nanocarriers (Zn-CNP) post-anthesis has proved to be a promising approach for grain zinc enhancement in durum wheat as evidenced in our earlier study. However, the molecular mechanism of uptake of zinc via Zn-CNP remains unclear. METHODS/PRINCIPLE FINDINGS: Foliar application of Zn-CNP was performed at post anthesis stages in two durum wheat cultivars (MACS 3125 and UC1114, containing the Gpc-B1 gene), and expression levels of several metal-related genes were analyzed during early senescence...
2018: PloS One
Umit Muhammet Kocyigit, Parham Taslimi, Fatih Gurses, Sinan Soylu, Sevgi Durna Dastan, İlhami Gulcin
The purpose of our study is to assist in understanding the effects of wireless electromagnetic waves on carbonic anhydrase (CA) and acetylcholinesterase (AChE) enzymes activities in the different tissues of the rats. For this purpose, two different groups each of which contains eight rats (n = 8) were formed as being control group and wireless electromagnetic wave-administered group. The rats were necropsied after 60 min from the injection of chemicals into the rats intraperitoneally. The different tissues of the rats were extracted...
January 17, 2018: Journal of Biochemical and Molecular Toxicology
Congcong Lin, Xue Zhang, Hubiao Chen, Zhaoxiang Bian, Ge Zhang, Muhammad Kashif Riaz, Deependra Tyagi, Ge Lin, Yanbo Zhang, Jinjin Wang, Aiping Lu, Zhijun Yang
The abilities of a drug delivery system to target and penetrate tumor masses are key factors in determining the system's chemotherapeutic efficacy. Here, we explored the utility of an anti-carbonic anhydrase IX (anti-CA IX) antibody and CPP33 dual-ligand modified triptolide-loaded liposomes (dl-TPL-lip) to simultaneously enhance the tumor-specific targeting and increase tumor cell penetration of TPL. In vitro, the dl-TPL-lip increased the cytotoxicity of TPL in CA IX-positive lung cancer cells, which showed tunable size (137...
November 2018: Drug Delivery
Iva Hoffmanová, Daniel Sánchez
Topical carbonic anhydrase inhibitors (CAI), used for treatment of glaucoma, are generally regarded as safe and unconnected with systemic side effects. We report an unusual case of fatigue, metabolic acidosis, and normocytic anaemia associated with ocular administration of the CAI, dorzolamide, in a patient with impaired renal function. In chronic kidney disease, where CAI elimination may be decreased, and patients prone to develop metabolic acidosis, systemic absorption of ocular administered CAI could lead to rare, but potentially serious adverse reaction, that are a consequence of inhibition of extraocular carbonic anhydrase isoenzymes...
January 14, 2018: British Journal of Clinical Pharmacology
Bibhuti Ranjan, Santhosh Pillai, Kugenthiren Permaul, Suren Singh
Cyanase detoxifies cyanate by transforming it to ammonia and carbon dioxide in a bicarbonate-dependent reaction, however, dependence on bicarbonate limits its utilization in large-scale applications. A novel strategy was therefore developed for overcoming this bottleneck by the combined application of cyanase (rTl-Cyn) and carbonic anhydrase (rTl-CA). The synergistic effect of rTl-Cyn and rTl-CA could reduce the dependence of bicarbonate by 80%, compared to using rTl-Cyn alone. Complete degradation of cyanate (4 mM) was achieved with buffered conditions and 85 ± 5% degradation with industrial wastewater sample, when 20 U of rTl-Cyn was applied...
December 29, 2017: Bioresource Technology
Abdur Rauf, Ghias Uddin, Bina S Siddiqui, Ajmal Khan, Umar Farooq, Farhan A Khan, Syed Majid Bukhari, Sher Bahadar Khan
Two new dimeric naphthoquinones, 5',8'-dihydroxy-6,6'-dimethyl-7,3'-binaphthyl-1,4,1',4'-tetraone (1; Di-naphthodiospyrol D) and 5',8'-dihydroxy-5,8-dimethoxy-6,6'-dimethyl-7,3'-binaphthyl-1,4,1',4'-tetraone (2; Di-naphthodiospyrol E), along with known naphthoquinones diospyrin (3) and 8-hydroxy diospyrin (4) were isolated from the chloroform fraction of extract of Diospyros lotus roots. Their structures were elucidated by advanced spectroscopic analyses, including HSQC, HMBC, NOESY, and J-resolved NMR experiments...
November 2017: Chinese Journal of Natural Medicines
Aikaterini Peperidou, Silvia Bua, Murat Bozdag, Dimitra Hadjipavlou-Litina, Claudiu T Supuran
A series of carboxamide derivatives of 6- and 7-substituted coumarins have been prepared by an original procedure starting from the corresponding 6- or 7-hydroxycoumarins which were alkylated with ethyl iodoacetate, and the obtained ester was converted to the corresponding carboxylic acids which were thereafter reacted with a series of aromatic/aliphatic/heterocyclic amines leading to the desired amides. The new derivatives were investigated as inhibitors of two enzymes, human carbonic anhydrases (hCAs) and soy bean lipoxygenase (LOX)...
January 12, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Ebru Akkemik, Baki Cicek, Yasemin Camadan, Umit Calisir, Zekai Onbasioglu
Carbonic anhydrases (CAs) play an important function in various physiological and pathological processes. Therefore, many researchers work in this field in order to design and synthesize new drugs. Both inhibitors and activators of CAs, which are associated with the diagnosis and treatment of many diseases, are very important. The emergence of the use of CA activators in the treatment of Alzheimer has led many scholars to work on this issue. In this study, CA activators and inhibitors are determined. The crown ethers compounds (1, 2, 3, 6, 7, 8, and 9) were found to cause activation on enzyme activities of hCA I and II...
January 12, 2018: Journal of Biochemical and Molecular Toxicology
Katarzyna Kowalik, Antoni Krzeski
Laryngopharyngeal reflux (LPR) is a common defect among laryngological and phoniatric patients. Although LPR is categorized as a superficial gastroesophageal reflux disease (GERD), differential diagnosis should treat these two diseases separately. LPR symptoms can be assessed in the interview using as a tool the reflux symptom index (RSI). In addition, changes in the larynx that occur during LPR might be seen during laryngoscopy and classified according to the reflux finding score (RFS). One of the main mucosal irritants in LPR is pepsin which digests proteins and impairs the functions of the upper respiratory tract cells by affecting carbonate anhydrase (CAIII) and the Sep 70 protein...
December 30, 2017: Otolaryngologia Polska
Eva Havránková, Jozef Csöllei, Daniela Vullo, Vladimír Garaj, Pavel Pazdera, Claudiu T Supuran
A new series of s-triazine derivatives incorporating sulfanilamide, homosulfanilamide, 4-aminoethyl-benzenesulfonamide and piperazine or aminoalcohol structural motifs is reported. Molecular docking was exploited to select compounds from virtual combinatorial library for synthesis and subsequent biological evaluation. The compounds were prepared by using step by step nucleophilic substitution of chlorine atoms from cyanuric chloride (2,4,6-trichloro-1,3,5-triazine). The compounds were tested as inhibitors of physiologically relevant carbonic anhydrase (CA, EC 4...
January 3, 2018: Bioorganic Chemistry
Serdar Burmaoglu, Ali O Yilmaz, Parham Taslimi, Oztekin Algul, Deryanur Kilic, Ilhami Gulcin
A series of novel phloroglucinol derivatives were designed, synthesized, characterized spectroscopically and tested for their inhibitory activity against selected metabolic enzymes, including α-glycosidase, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human carbonic anhydrase I and II (hCA I and II). These compounds displayed nanomolar inhibition levels and showed Ki values of 1.14-3.92 nM against AChE, 0.24-1.64 nM against BChE, 6.73-51.10 nM against α-glycosidase, 1.80-5.10 nM against hCA I, and 1...
January 11, 2018: Archiv der Pharmazie
Daniela Vullo, Leo Syrjänen, Marianne Kuuslahti, Seppo Parkkila, Claudiu T Supuran
An anion inhibition study of the β-class carbonic anhydrase, AgaCA, from the malaria mosquito Anopheles gambiae is reported. A series of simple as well as complex inorganic anions, and small molecules known to interact with CAs were included in the study. Bromide, iodide, bisulphite, perchlorate, perrhenate, perruthenate, and peroxydisulphate were ineffective AgaCA inhibitors, with KIs > 200 mM. Fluoride, chloride, cyanate, thiocyanate, cyanide, bicarbonate, carbonate, nitrite, nitrate, sulphate, stannate, selenate, tellurate, diphosphate, divanadate, tetraborate, selenocyanide, and trithiocarbonate showed KIs in the range of 1...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
Andrea Angeli, Sonia Del Prete, Sameh M Osman, Fatmah A S Alasmary, Zeid AlOthman, William A Donald, Clemente Capasso, Claudiu T Supuran
The activation of a β-class carbonic anhydrase (CAs, EC from Mycobacterium tuberculosis, encoded by the gene Rv3273 (mtCA 3), was investigated using a panel of natural and non-natural amino acids and amines. mtCA 3 was effectively activated by D-DOPA, L-Trp, dopamine and serotonin, with KAs ranging between 8.98 and 12.1 µM. L-His and D-Tyr showed medium potency activating effects, with KAs in the range of 17.6-18.2 µM, whereas other amines and amino acids were relatively ineffective activators, with KAs in the range of 28...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
Abdul M Baig, R Zohaib, S Tariq, H R Ahmad
AIM: This study intended to trace the evolution of acid-base buffers and water homeostasis in eukaryotes. Acanthamoeba castellanii  was selected as a model unicellular eukaryote for this purpose. Homologies of proteins involved in pH and water regulatory mechanisms at cellular levels were compared between humans and A. castellanii. MATERIALS & METHODS: Amino acid sequence homology, structural homology, 3D modeling and docking prediction were done to show the extent of similarities between carbonic anhydrase 1 (CA1), aquaporin (AQP), band-3 protein and H+ pump...
January 11, 2018: Future Microbiology
Andrea Angeli, Sonia Del Prete, William A Donald, Clemente Capasso, Claudiu T Supuran
The γ-class carbonic anhydrase (CAs, EC from the pathogenic bacterium Vibrio cholerae, VchCAγ, was investigated for its activation with a panel of natural and non-natural amino acids and amines. The enzyme was effectively activated by l-tryptophan, 1-(2-minoethyl)-piperazine and 4-(2-aminoethyl)-morpholine, in the low nanomolar range (KAs 8-71 nM). In contrast, l-/d-Phe, l-/d-DOPA, d-Trp, l-/d-Tyr, 4-amino-l-Phe, histamine, dopamine, serotonin, some pyridyl-alkylamines, as well as l-adrenaline were submicromolar activators (KAs between 0...
January 4, 2018: Bioorganic Chemistry
Adam Pecina, Jiri Brynda, Lukas Vrzal, Ramachandran Gnanasekaran, Magdalena Horejsi, Saltuk Eyrilmez, Jan Rezac, Martin Lepsik, Pavlina Rezacova, Pavel Hobza, Pavel Majer, Vaclav Veverka, Jindrich Fanfrlik
Accurate prediction of protein-ligand binding affinities is essential for hit-to-lead optimization and virtual screening. The reliability of scoring functions can be improved by implementing of quantum effects. Here, we demonstrate the ranking power of the semiempirical quantum mechanics (SQM)/implicit solvent (COSMO) scoring function using a challenging set of 10 inhibitors binding to carbonic anhydrase II via Zn2+ in the active site. This new dataset consists of the high-resolution (1.1 - 1.4 Å) crystal structures and experimentally determined Ki values...
January 8, 2018: Chemphyschem: a European Journal of Chemical Physics and Physical Chemistry
Abdul Chrachri, Brian M Hopkinson, Kevin Flynn, Colin Brownlee, Glen L Wheeler
Photosynthesis by marine diatoms plays a major role in the global carbon cycle, although the precise mechanisms of dissolved inorganic carbon (DIC) uptake remain unclear. A lack of direct measurements of carbonate chemistry at the cell surface has led to uncertainty over the underlying membrane transport processes and the role of external carbonic anhydrase (eCA). Here we identify rapid and substantial photosynthesis-driven increases in pH and [CO32-] primarily due to the activity of eCA at the cell surface of the large diatom Odontella sinensis using direct simultaneous microelectrode measurements of pH and CO32- along with modelling of cell surface inorganic carbonate chemistry...
January 8, 2018: Nature Communications
Iryna Antal, Martina Koneracka, Martina Kubovcikova, Vlasta Zavisova, Iryna Khmara, Dasa Lucanska, Lenka Jelenska, Ivana Vidlickova, Miriam Zatovicova, Silvia Pastorekova, Nikola Bugarova, Matej Micusik, Maria Omastova, Peter Kopcansky
Amino-modified magnetic nanoparticles were prepared by direct chemisorption of biocompatible d,l-lysine (DLL) on electrostatically stabilized magnetic nanoparticles with the aim to bind specific antibodies (Ab) able to detect cancer cells. The magnetic nanoparticles prepared by coprecipitation were stabilized in an acidic medium. A full optimization study of amino modification performed by UV/Vis spectroscopy and Dynamic Light Scattering measurement (DLS) confirmed an optimal DLL/Fe3O4 weight ratio of 2. The sample was subjected to complex characterizations using different techniques such as UV/Vis, FTIR and X-ray photoelectron spectroscopies (XPS) together with transmission electron microscopy and size/zeta potential measurements...
December 21, 2017: Colloids and Surfaces. B, Biointerfaces
Edita Čapkauskaitė, Audrius Zakšauskas, Virginijus Ruibys, Vaida Linkuvienė, Vaida Paketurytė, Marius Gedgaudas, Visvaldas Kairys, Daumantas Matulis
The similarity of human carbonic anhydrase (CA) active sites makes it difficult to design selective inhibitors for one or several CA isoforms that are drug targets. Here we synthesize a series of compounds that are based on 5-[2-(benzimidazol-1-yl)acetyl]-2-chloro-benzenesulfonamide (1a) which demonstrated picomolar binding affinity and significant selectivity for CA isoform five A (VA), and explain the structural influence of inhibitor functional groups to the binding affinity and selectivity. A series of chloro-substituted benzenesulfonamides bearing a heterocyclic tail, together with molecular docking, was used to build inhibitors that explore substituent influence on the binding affinity to the CA VA isoform...
December 24, 2017: Bioorganic & Medicinal Chemistry
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