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carbonic anhydrase

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https://www.readbyqxmd.com/read/29153590/heterocyclic-periphery-in-the-design-of-carbonic-anhydrase-inhibitors-1-2-4-oxadiazol-5-yl-benzenesulfonamides-as-potent-and-selective-inhibitors-of-cytosolic-hca-ii-and-membrane-bound-hca-ix-isoforms
#1
Mikhail Krasavin, Anton Shetnev, Tatyana Sharonova, Sergey Baykov, Tiziano Tuccinardi, Stanislav Kalinin, Andrea Angeli, Claudiu T Supuran
A series of novel aromatic primary sulfonamides decorated with diversely substituted 1,2,4-oxadiazole periphery groups has been prepared using a parallel chemistry approach. The compounds displayed a potent inhibition of cytosolic hCA II and membrane-bound hCA IX isoforms. Due to a different cellular localization of the two target enzymes, the compounds can be viewed as selective inhibition tools for either isoform, depending on the cellular permeability profile. The SAR findings revealed in this study has been well rationalized by docking simulation of the key compounds against the crystal structures of the relevant hCA isoforms...
October 16, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29152053/benzoxaboroles-as-efficient-inhibitors-of-the-%C3%AE-carbonic-anhydrases-from-pathogenic-fungi-activity-and-modeling-study
#2
Alessio Nocentini, Roberta Cadoni, Sonia Del Prete, Clemente Capasso, Pascal Dumy, Paola Gratteri, Claudiu T Supuran, Jean-Yves Winum
A series of 6-substituted benzoxaboroles were investigated as inhibitors of the β-class carbonic anhydrase from three pathogenic fungi (Cryptococcus neoformans, Candida glabrata, and Malassezia globosa). Independently from the nature of the substituents on the phenyl of the urea/thiourea group, all reported derivatives showed nanomolar inhibitory activities against Can2 and CgNce103 vs micromolar inhibition against MgCA. Selectivity over human CA I and CA II was noticed. The observed structure-activity relationship trends have been rationalized by modeling study of selected compounds into the active site of Can2 and MgCA...
November 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29151684/glaucoma-medication-preferences-among-glaucoma-specialists-in-mexico
#3
Gabriel Lazcano-Gomez, Daniela Alvarez-Ascencio, Cindy Haro-Zuno, Mauricio Turati-Acosta, Magdalena Garcia-Huerta, Jesus Jimenez-Arroyo, Rafael Castañeda-Diez, Armando Castillejos-Chevez, Roberto Gonzalez-Salinas, Francisca Dominguez-Dueñas, Jesus Jimenez-Roman
Aim: To determine the glaucoma specialists' preferences for the different brands of topical glaucoma medications available in Mexico. Materials and methods: A web-based survey was sent to 150 board-certified glaucoma specialists in Mexico, with 14 questions related to brand preferences for all glaucoma medications available in Mexico. Participants were asked to select each glaucoma medication class by brand and to state the factors leading to their choice. Results: Data from 111 (74%) glaucoma specialists were collected...
September 2017: Journal of Current Glaucoma Practice
https://www.readbyqxmd.com/read/29149534/novel-n-propylphthalimide-and-4-vinylbenzyl-substituted-benzimidazole-salts-synthesis-characterization-and-determination-of-their-metal-chelating-effects-and-inhibition-profiles-against-acetylcholinesterase-and-carbonic-anhydrase-enzymes
#4
Yakup Sarı, Aydın Aktaş, Parham Taslimi, Yetkin Gök, İlhami Gulçin
The novel N-propylphthalimide-substituted and 4-vinylbenzyl-substituted N-heterocyclic carbene (NHC) precursors were synthesized by N-substituted benzimidazolium with aryl halides. The novel N-propylphthalimide-substituted and 4-vinylbenzyl-substituted NHC precursors have been characterized by using (1) H NMR, (13) C NMR, FTIR spectroscopy, and elemental analysis techniques. They were tested for the inhibition of AChE and hCA enzymes and demonstrated efficient inhibition profiles with Ki values in the range of 351...
November 17, 2017: Journal of Biochemical and Molecular Toxicology
https://www.readbyqxmd.com/read/29147618/programmed-cell-death-ligands-expression-in-phaeochromocytomas-and-paragangliomas-relationship-with-the-hypoxic-response-immune-evasion-and-malignant-behavior
#5
David J Pinato, James R Black, Sebastian Trousil, Roberto E Dina, Pritesh Trivedi, Francesco A Mauri, Rohini Sharma
The hypoxic response underlies the pathogenesis and malignant behavior of PCC/PGL. Regulation of PD-1 receptor-ligand signaling, a therapeutically actionable driver of the anti-tumor immune response, is a hypoxic-driven trait across malignancies. We evaluated the prognostic role of PD ligands in association with biomarkers of hypoxia and angiogenesis in patients with PCC/PGL. Tissue microarrays sections including consecutive cases diagnosed between 1983-2011 were stained for PD-L1 and 2, hypoxia inducible factor 1a (Hif-1a), Carbonic Anhydrase IX (CaIX), Vascular Endothelial Growth Factor-A (VEGF-A)...
2017: Oncoimmunology
https://www.readbyqxmd.com/read/29146134/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
#6
Beata Żołnowska, Jarosław Sławiński, Krzysztof Szafrański, Andrea Angeli, Claudiu T Supuran, Anna Kawiak, Miłosz Wieczór, Joanna Zielińska, Tomasz Bączek, Sylwia Bartoszewska
A series of novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(6-substituted-4-chloro-1,3,5-triazin-2-ylamino)guanidine derivatives 9-20 have been synthesized by substitution of chlorine atom at the 1,3,5-triazine ring in compounds 5-8 with 3- or 4-aminobenzenesulfonamide and 4-(aminomethyl)benzenesulfonamide hydrochloride. All the synthesized compounds were evaluated for their inhibitory activity toward hCA I, II, IX and XII as well as anticancer activity against HeLa, HCT-116 and MCF-7 human tumor cell lines...
November 4, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29144028/efficacy-and-safety-of-different-regimens-for-primary-open-angle-glaucoma-or-ocular-hypertension-a-systematic-review-and-network-meta-analysis
#7
Fei Li, Wenbin Huang, Xiulan Zhang
PURPOSE: To assess the efficacy and safety of different regimens, including monotherapy and double therapy, for primary open-angle glaucoma (POAG) or ocular hypertension. METHODS: We searched PubMed, EMBASE and clinicaltrials.gov for studies that fit our inclusion criteria in this network meta-analysis. Randomized controlled trials that report data on efficacy and safety of medications for POAG or ocular hypertension are included. Data on intra-ocular pressure (IOP) lowering effect and incidence of adverse events including hyperaemia and ocular discomfort were extracted and used in mixed-comparison analysis...
November 16, 2017: Acta Ophthalmologica
https://www.readbyqxmd.com/read/29143485/synthesis-molecular-modeling-and-biological-evaluation-of-4-5-aryl-3-thiophen-2-yl-4-5-dihydro-1h-pyrazol-1-yl-benzenesulfonamides-towards-acetylcholinesterase-carbonic-anhydrase-i-and-ii-enzymes
#8
Cem Yamali, Halise Inci Gul, Abdulilah Ece, Parham Taslimi, Ilhami Gulcin
In the present study, 4-[5-aryl-3-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl] benzenesulfonamides were synthesized and inhibition effects on AChE, hCA I and hCA II were evaluated. Ki values of the compounds towards hCA I were in the range of 24.2±4.6-49.8±12.8 nM while they were in the range of 37.3±9.0-65.3±16.7 nM towards hCA II. Ki values of the Acetazolamide were 282.1±19.7 nM and 103.60±27.6 nM towards both isoenzymes, respectively. The compounds inhibited AChE with Ki in the range of 22.7±10.3-109...
November 16, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29139171/structural-insights-into-a-thermostable-variant-of-human-carbonic-anhydrase-ii
#9
Kelsey M Kean, Joseph J Porter, Ryan A Mehl, P Andrew Karplus
Carbonic anhydrase is an enzyme of interest for many biotechnological developments including carbon sequestration. These applications often require harsh conditions, so there is a need for the development of thermostable variants. One of the most thermostable human carbonic anhydrase II variants (HCAIIts) was patented in 2006. Here, we report the ultra-high resolution crystal structure of HCAIIts. The structural changes seen are consistent with each of the six mutations involved acting largely independently and variously resulting in increased H-bonding, improved packing, and reduced side chain entropy loss upon folding to yield the increased stability...
November 15, 2017: Protein Science: a Publication of the Protein Society
https://www.readbyqxmd.com/read/29138983/cloning-expression-analysis-and-enzyme-activity-assays-of-the-%C3%AE-carbonic-anhydrase-gene-from-chlamydomonas-sp-ice-l
#10
Changfeng Qu, Yingying He, Zhou Zheng, Meiling An, Lulu Li, Xixi Wang, Xiaodong He, Yibin Wang, Fangming Liu, Jinlai Miao
The α-carbonic anhydrase (α-CA) is a zinc ion-containing enzyme that catalyzes the hydration of carbon dioxide. In this paper, a full-length α-CA gene was cloned from Chlamydomonas sp. ICE-L using RT-PCR and RACE-PCR for bioinformatic analysis. The α-CA open reading frame obtained by PCR was cloned into a vector and transformed into Escherichia coli to generate α-CA-producing bacteria. The α-CA was highly expressed upon induction with isopropyl-β-d-thiogalactoside (IPTG) at a final concentration of 0...
November 14, 2017: Molecular Biotechnology
https://www.readbyqxmd.com/read/29137326/overexpression-of-carbonic-anhydrase-ix-induces-cell-motility-by-activating-matrix-metalloproteinase-9-in-human-oral-squamous-cell-carcinoma-cells
#11
Jia-Sin Yang, Chiao-Wen Lin, Yi-Hsien Hsieh, Ming-Hsien Chien, Chun-Yi Chuang, Shun-Fa Yang
Oral cancer is a solid malignant tumor that is prone to occur following hypoxia. There are no clear studies showing a link between hypoxia and oral carcinogenesis. Carbonic anhydrase IX (CAIX), which is a hypoxia-induced transmembrane protein, is highly expressed in various types of human cancer. However, the effects of CAIX on the metastasis of human oral cancer cells and the underlying molecular mechanisms have not been clarified. In this study, we observed that CAIX overexpression increased the migratory and invasive abilities of SCC-9 and SAS cells...
October 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/29137134/an-overview-of-the-bacterial-carbonic-anhydrases
#12
REVIEW
Claudiu T Supuran, Clemente Capasso
Bacteria encode carbonic anhydrases (CAs, EC 4.2.1.1) belonging to three different genetic families, the α-, β-, and γ-classes. By equilibrating CO₂ and bicarbonate, these metalloenzymes interfere with pH regulation and other crucial physiological processes of these organisms. The detailed investigations of many such enzymes from pathogenic and non-pathogenic bacteria afford the opportunity to design both novel therapeutic agents, as well as biomimetic processes, for example, for CO₂ capture. Investigation of bacterial CA inhibitors and activators may be relevant for finding antibiotics with a new mechanism of action...
November 11, 2017: Metabolites
https://www.readbyqxmd.com/read/29136525/improving-the-carbonic-anhydrase-inhibition-profile-of-the-sulfamoylphenyl-pharmacophore-by-attachment-of-carbohydrate-moieties
#13
Leonardo E Riafrecha, Silvia Bua, Claudiu T Supuran, Pedro A Colinas
One of the most successful approaches for designing carbonic anhydrase (CA, EC 4.2.1.1) inhibitors was denominated 'the sugar approach'. The sugar approach consists in attaching different carbohydrates to CA inhibiting pharmacophores for modulating the physicochemical properties of these pharmacological agents. In line with this approach, in this paper, we present a new class of C-glycosides incorporating the sulfamoylphenyl moiety. These compounds have been prepared by sulfamoylation of C-glycosyl phenols, which have been synthetized by aldol reaction of glycosyl ketones with the appropriate aromatic aldehydes...
November 2, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29134667/synthesis-and-carbonic-anhydrase-inhibition-of-tetrabromo-chalcone-derivatives
#14
Umit M Kocyigit, Yakup Budak, Fikret Eligüzel, Parham Taslimi, Deryanur Kılıç, İlhami Gulçin, Mustafa Ceylan
In the present study, human carbonic anhydrase (hCA) enzyme was purified and characterized from fresh blood human red cells by Sepharose-4B-l-tyrosine-sulfanilamide affinity gel chromatography. Secondly, a series of new tetrabromo chalcone derivatives containing 4,7-methanoisoindol-1,3-dione (2a-i) were synthesized from the addition of Br2 to related chalcone derivatives (1a-i). The structures of the new molecules (2a-i) were confirmed by means of (1) H NMR, (13) C NMR and elemental analysis. Finally, the inhibitory effects of 2a-i on CA activities were investigated using the esterase method under in vitro conditions...
November 14, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/29134362/selecting-patients-for-hyperthermia-combined-with-preoperative-chemoradiotherapy-for-locally-advanced-rectal-cancer
#15
Sang-Won Kim, Ji Woon Yea, Jae Hwang Kim, Mi Jin Gu, Min Kyu Kang
BACKGROUND: This study investigated the role of hyperthermia combined with preoperative concurrent chemoradiotherapy (CCRT) for locally advanced rectal cancer (LARC) according to hypoxic marker expression. METHODS: One hundred and nine LARC patients with tissue blocks available for immunohistochemical assessment of carbonic anhydrase 9 (CA9) expression were reviewed. CA9 expression was considered positive when the staining percentage of tumor cells was >25% (n = 31)...
November 13, 2017: International Journal of Clinical Oncology
https://www.readbyqxmd.com/read/29133450/resurrecting-ancestral-genes-in-bacteria-to-interpret-ancient-biosignatures
#16
Betul Kacar, Lionel Guy, Eric Smith, John Baross
Two datasets, the geologic record and the genetic content of extant organisms, provide complementary insights into the history of how key molecular components have shaped or driven global environmental and macroevolutionary trends. Changes in global physico-chemical modes over time are thought to be a consistent feature of this relationship between Earth and life, as life is thought to have been optimizing protein functions for the entirety of its approximately 3.8 billion years of history on the Earth. Organismal survival depends on how well critical genetic and metabolic components can adapt to their environments, reflecting an ability to optimize efficiently to changing conditions...
December 28, 2017: Philosophical Transactions. Series A, Mathematical, Physical, and Engineering Sciences
https://www.readbyqxmd.com/read/29132976/investigations-into-the-carbonic-anhydrase-inhibition-of-cos-releasing-donor-core-motifs
#17
Andrea K Steiger, Yu Zhao, Won Jin Choi, Alder Crammond, McKinna R Tillotson, Michael D Pluth
Carbonyl sulfide (COS) releasing scaffolds are gaining popularity as hydrogen sulfide (H2S) donors through exploitation of the carbonic anhydrase (CA)-mediated hydrolysis of COS to H2S. The majority of compounds in this emerging class of donors undergo triggerable decomposition (often referred to as self-immolation) to release COS, and a handful of different COS-releasing structures have been reported. One benefit of this donation strategy is that numerous caged COS-containing core motifs are possible and are poised for development into self-immolative COS/H2S donors...
November 10, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29131471/the-toxicological-effects-of-some-avermectins-on-goat-liver-carbonic-anhydrase-enzyme
#18
Cuneyt Caglayan, İlhami Gulcin
Avermectins are used worldwide as antiparasitic drugs in the field of veterinary medicine and as agricultural pesticides and insecticides. Carbonic anhydrase (CA, E.C. 4.2.1.1) is a zinc-containing metalloenzyme that catalyzes the reversible hydration of carbon dioxide (CO2 ) to yield protons (H(+) ) and bicarbonate (HCO3(-) ). In this study, some avermectins, including abamectin, doramectin, eprinomectin, and moxidectin, were investigated for in vitro inhibitory effects on the CA enzyme purified from goat liver, which was purified (125...
November 13, 2017: Journal of Biochemical and Molecular Toxicology
https://www.readbyqxmd.com/read/29131470/synthesis-of-some-novel-pyridine-compounds-containing-bis-1-2-4-triazole-thiosemicarbazide-moiety-and-investigation-of-their-antioxidant-properties-carbonic-anhydrase-and-acetylcholinesterase-enzymes-inhibition-profiles
#19
Nilufer Bulut, Umit M Kocyigit, Ibrahim H Gecibesler, Taner Dastan, Huseyin Karci, Parham Taslimi, Sevgi Durna Dastan, Ilhami Gulcin, Ahmet Cetin
Some novel derivatives of thiosemicarbazide and 1,2,4-triazole-3-thiol were synthesized and evaluated for their biological activities. The title compounds were prepared starting from readily available pyridine-2,5-dicarboxylic acid. The reaction carboxylic acid with absolute ethanol afforded the corresponding dimethyl pyridine-2,5-dicarboxylate (1). The reaction of dimethyl-2,5-pyridinedicarboxylate (1) with hydrazine hydrate good yielded pyridine-2,5-dicarbohydrazide (2). Refluxing compound 2 with alkyl/aryl isothiocyanate derivatives for 3-8 h afforded 1,4-disubstituted thiosemicarbazides (3a-e)...
November 13, 2017: Journal of Biochemical and Molecular Toxicology
https://www.readbyqxmd.com/read/29128547/associations-between-asymmetric-dimethylarginine-adma-nitrite-dependent-renal-carbonic-anhydrase-activity-and-plasma-testosterone-levels-in-hypogonadal-men
#20
Dimitrios Tsikas, Manfred Kinzel
BACKGROUND: Circulating inorganic nitrite (NO2(-)) is an abundant nitric oxide (NO) reservoir. Renal carbonic anhydrase (CA) mediates the absorption of urinary nitrite. The urinary nitrate-to-nitrite molar ratio UNOxR is a measure of nitrite-dependent renal CA activity. The CA family is also involved in the bioactivation of nitrite to S-nitrosothiols and NO. Thus, CA isoforms may combat atherosclerosis. METHODS: In plasma and urine of ten hypogonadal men we measured the major NO metabolites nitrite and nitrate, and the endogenous inhibitor of NO synthase (NOS) asymmetric dimethylarginine (ADMA) before and after a 24-weeks testosterone treatment to normalize plasma testosterone levels...
November 8, 2017: Hellenic Journal of Cardiology: HJC, Hellēnikē Kardiologikē Epitheōrēsē
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