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Carbonic anhydrase 3

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https://www.readbyqxmd.com/read/28940980/sulfocoumarin-coumarin-4-sulfamoylphenyl-bearing-indazole-3-carboxamide-hybrids-synthesis-and-selective-inhibition-of-tumor-associated-carbonic-anhydrase-isozymes-ix-and-xii
#1
Srinivas Angapelly, P V Sri Ramya, Andrea Angeli, Claudiu T Supuran, Mohammed Arifuddin
A series of sulfocoumarin-, coumarin-, and 4-sulfamoylphenyl-bearing indazole-3-carboxamide hybrids were synthesized and investigated as inhibitors of the human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms I and II (cytosolic isozymes), as well as hCA IX and XII (transmembrane, tumor-associated enzymes). Compounds 6 a-g (amide derivatives) and 7 a-h (triazoles) act as "prodrugs", and their hydrolysis products are the de facto CA inhibitors. These compounds displayed sub-micromolar to high-nanomolar inhibitory activity against hCA isoforms IX and XII, which were recently validated as antitumor drug targets...
September 2, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28933591/suppression-of-chrn-endocytosis-by-carbonic-anhydrase-car3-in-the-pathogenesis-of-myasthenia-gravis
#2
Ailian Du, Shiqian Huang, Xiaonan Zhao, Kuan Feng, Shuangyan Zhang, Jiefang Huang, Xiang Miao, Fulvio Baggi, Rennolds S Ostrom, Yanyun Zhang, Xiangjun Chen, Congfeng Xu
Myasthenia gravis is an autoimmune disorder of the neuromuscular junction manifested as fatigable muscle weakness, which is typically caused by pathogenic autoantibodies against postsynaptic CHRN/AChR (cholinergic receptor nicotinic) in the endplate of skeletal muscle. Our previous studies have identified CA3 (carbonic anhydrase 3) as a specific protein insufficient in skeletal muscle from myasthenia gravis patients. In this study, we investigated the underlying mechanism of how CA3 insufficiency might contribute to myasthenia gravis...
September 21, 2017: Autophagy
https://www.readbyqxmd.com/read/28930221/compounds-from-terminalia-mantaly-l-combretaceae-stem-bark-exhibit-potent-inhibition-against-some-pathogenic-yeasts-and-enzymes-of-metabolic-significance
#3
Marthe Aimée Tchuente Tchuenmogne, Thierry Ngouana Kammalac, Sebastian Gohlke, Rufin Marie Toghueo Kouipou, Abdulselam Aslan, Muslum Kuzu, Veysel Comakli, Ramazan Demirdag, Silvère Augustin Ngouela, Etienne Tsamo, Norbert Sewald, Bruno Ndjakou Lenta, Fabrice Fekam Boyom
Background: Pathogenic yeasts resistance to current drugs emphasizes the need for new, safe, and cost-effective drugs. Also, new inhibitors are needed to control the effects of enzymes that are implicated in metabolic dysfunctions such as cancer, obesity, and epilepsy. Methods: The anti-yeast extract from Terminalia mantaly (Combretaceae) was fractionated and the structures of the isolated compounds established by means of spectroscopic analysis and comparison with literature data. Activity was assessed against Candida albicans, C...
January 24, 2017: Medicines (Basel, Switzerland)
https://www.readbyqxmd.com/read/28905987/novel-carbonic-anhydrase-ix-targeted-therapy-enhances-the-anti-tumour-effects-of-cisplatin-in-small-cell-lung-cancer
#4
Jennifer L Bryant, Roben G Gieling, Suzanne L Meredith, Tiffany-Jayne Allen, Leanne Walker, Brian A Telfer, Claudiu T Supuran, Kaye J Williams, Anne White
Small cell lung cancer (SCLC) has an extremely poor prognosis and methods of improving chemotherapeutic intervention are much sought after. A promising approach lies in inhibiting the tumour-associated enzyme, carbonic anhydrase IX (CA IX), which supports tumour cell survival. The aim of this study was to assess the potential of CA IX inhibition using 4-(3'-(3″,5″-dimethylphenyl)ureido)phenyl sulfamate (S4), for the treatment of human SCLC alone and in combination with cisplatin chemotherapy. Treating SCLC cell lines (DMS 79 and COR-L24) with 100µM S4 reduced viability in vitro and enhanced cell death when combined with 7µM cisplatin, most prominently under hypoxic conditions (0...
September 14, 2017: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/28904465/spectrum-of-visual-impairment-in-cerebral-venous-thrombosis-importance-of-tailoring-therapies-based-on-pathophysiology
#5
Sanjith Aaron, Anupriya Arthur, A T Prabakhar, Pavitra Mannam, N K Shyamkumar, Sunithi Mani, Vivek Mathew, Jeyanthi Peter, Ajith Sivadasan, Anika Alexander, M Karthik, Rohith Ninan Benjamin, Mathew Alexander
Visual impairment can complicate cerebral venous thrombosis (CVT). Here, we describe the various pathophysiological mechanisms and treatments available. A retrospective chart review of all patients treated for CVT in a large quaternary teaching hospital was done, and cases with visual impairment due to CVT were identified. The various mechanisms causing visual impairment in CVT were (1) raised intracranial pressure (ICP) caused by venous thrombosis without venous infarcts resulting in a benign intracranial hypertension-like presentation of CVT, (2) venous infarcts involving the occipital cortex, (3) raised ICP following the development of a secondary dural arteriovenous (AV) fistula, and (4) arterial occipital infarcts due to posterior cerebral artery compression secondary to herniation in large venous infarcts...
July 2017: Annals of Indian Academy of Neurology
https://www.readbyqxmd.com/read/28902458/the-impact-of-some-natural-phenolic-compounds-on-carbonic-anhydrase-acetylcholinesterase-butyrylcholinesterase-and-%C3%AE-glycosidase-enzymes-an-antidiabetic-anticholinergic-and-antiepileptic-study
#6
Parham Taslimi, Cuneyt Caglayan, İlhami Gulcin
Natural products from food and plant sources have been used for medicinal usage for ages. Also, natural products with therapeutic significance are compounds derived from animals, plants, or any microorganism. In this study, chrysin, carvacrol, hesperidin, zingerone, and naringin as natural phenols showed excellent inhibitory effects against human (h) carbonic anhydrase (CA) isoforms I and II (hCA I and II), α-glucosidase (α-Gly), acetylcholinesterase (AChE), and butyrylcholinesterase (BChE). These phenolic compounds were tested for the inhibition of α-glycosidase, hCA I, hCA II, AChE, and BChE enzymes and demonstrated efficient inhibition profiles with Ki values in the range of 3...
September 13, 2017: Journal of Biochemical and Molecular Toxicology
https://www.readbyqxmd.com/read/28902455/synthesis-of-2-amino-3-cyanopyridine-derivatives-and-investigation-of-their-carbonic-anhydrase-inhibition-effects
#7
Aliye Altundas, Berna Gül, Murat Çankaya, Ali Atasever, İlhami Gülçin
The conversion of carbon dioxide (CO2 ) and bicarbonate (HCO3(-) ) to each other is very important for living metabolism. Carbonic anhydrase (CA, E.C.4.2.1.1), a metalloenzyme familly, catalyzes the interconversion of these ions (CO2 and HCO3(-) ) and are very common in living organisms. In this study, a series of novel 2-amino-3-cyanopyridines supported with some functional groups was synthesized and tested as potential inhibition effects against both cytosolic human CA I and II isoenzymes (hCA I and II) using by Sepharose-4B-l-tyrosine-sulfanilamide affinity chromatography...
September 13, 2017: Journal of Biochemical and Molecular Toxicology
https://www.readbyqxmd.com/read/28902167/optimization-and-comparison-of-synthetic-procedures-for-a-group-of-triazinyl-substituted-benzene-sulfonamide-conjugates-with-amino-acids
#8
Dominika Krajčiová, Daniel Pecher, Vladimír Garaj, Peter Mikuš
Sulfonamides incorporating 1,3,5-triazine moieties can selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII, and XIV over cytosolic isoforms I and II. In the present work, a highly effective synthetic procedure was proposed for this group of potent cancerostatic drugs and compared with previously used methods. The synthesis of triazinyl-substituted benzene-sulfonamide conjugates with amino acids can be easily carried out using sodium carbonate-based water solution as a synthetic medium instead of N,N-Diisopropylethylamine/Dimethylformamide...
September 13, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28891338/synthesis-and-biological-evaluation-of-benzenesulphonamide-bearing-1-4-5-trisubstituted-1-2-3-triazoles-possessing-human-carbonic-anhydrase-i-ii-iv-and-ix-inhibitory-activity
#9
Rajiv Kumar, Vikas Sharma, Silvia Bua, Claudiu T Supuran, Pawan K Sharma
A library of benzenesulphonamides incorporating 1,2,3-triazole rings functionalised with ester, carboxylic acid, carboxamide, carboxyhydrazide, and hydroxymethyl moieties were synthesised. The carbonic anhydrase (CAs, EC 4.2.1.1) inhibitory activity of the new compounds was assessed against four human (h) isoforms, hCA I, hCA II, hCA IV, and hCA IX. Among them, hCA II and IV are anti-glaucoma drug targets, being involved in aqueous humour secretion within the eye. hCA I was inhibited with Ki's ranging between 8...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28887000/development-of-sulfonamides-incorporating-phenylacrylamido-functionalities-as-carbonic-anhydrase-isoforms-i-ii-ix-and-xii-inhibitors
#10
Srinivas Angapelly, P V Sri Ramya, Andrea Angeli, Sonia Del Prete, Clemente Capasso, Mohammed Arifuddin, Claudiu T Supuran
A series of novel sulfonamides incorporating phenylacrylamido functionalities were synthesized and investigated for the inhibition of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1). The physiologically and pharmacologically relevant human (h) isoforms hCA I and II (cytosolic isozymes), as well as the transmembrane tumor-associated hCA IX and XII were included in the study. These compounds showed low nanomolar or sub-nanomolar inhibition constants against hCA II (KIs in the range of 0.50-50.5nM), hCA IX (KIs of 1...
September 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28869329/a-multiple-stimulus-responsive-biomimetic-assembly-based-on-polyisocyanopeptide-and-conjugated-polymer
#11
Fanfan Meng, Chengfen Xing, Hongbo Yuan, Yibing Fan, Ran Chai, Yong Zhan
An assembly has been fabricated and indicated as a multiple-stimulus responsive biomimetic hybrid polymer architecture. It was constructed by the hydrophobic interactions between the conjugated polyfluorene containing 2,1,3-benzothia-diazole units (PFBT) and the tri(ethylene glycol)-functionalized polyisocyanopeptide (3OEG-PIC). The introduction of PFBT to the polyisocyanopeptide (PIC) network allows for the incorporation of multiple-stimulus responsiveness including temperature, CO2, carbonic anhydrase and nonlinear mechanics, which mimics the natural processes and interactions...
September 4, 2017: Chemistry, An Asian Journal
https://www.readbyqxmd.com/read/28866249/the-synthesis-of-novel-sulfamides-derived-from-%C3%AE-benzylphenethylamines-as-acetylcholinesterase-butyrylcholinesterase-and-carbonic-anhydrase-enzymes-inhibitors
#12
Akın Akıncıoğlu, Ebutalib Kocaman, Hülya Akıncıoğlu, Ramin Ekhteiari Salmas, Serdar Durdagi, İlhami Gülçin, Claudiu T Supuran, Süleyman Göksu
In this study, a series of novel β-benzylphenethylamines and their sulfamide derivatives were synthesized starting from (Z)-2,3-diphenylacrylonitriles. Pd-C catalysed hydrogenation of diphenylacrylonitriles, reduction of propanenitriles with LiAlH4 in the presence of AlCl3 followed by addition of conc. HCl afforded β-benzylphenethylamine hydrochloride salts. The reactions of these amine hydrochloride salts with chlorosulfonyl isocyanate (CSI) in the presence of tert-BuOH and excess Et3N gave sulfamoylcarbamates...
August 23, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28858156/comparison-of-efficacy-and-complications-of-cyclophotocoagulation-and-second-glaucoma-drainage-device-after-initial-glaucoma-drainage-device-failure
#13
Margaret Y Wang, Kishan Patel, Lauren S Blieden, Alice Z Chuang, Laura A Baker, Nicholas P Bell, Robert M Feldman
PURPOSE: Compare intraocular pressure (IOP) control and complication rates of a second glaucoma drainage device (GDD) to diode transscleral cyclophotocoagulation (TSCPC) following failure of an initial GDD. PATIENTS AND METHODS: Eyes with one GDD that required a second GDD or TSCPC for glaucoma control were included. Exclusion criteria were a cyclodestructive procedure prior to initial GDD, no light perception vision, or follow-up less than one year. Failure was defined as one or more of (1) reoperation for lowering IOP; (2) explantation of second GDD; (3) persistent hypotony; (4) use of oral carbonic anhydrase inhibitor for lowering IOP in the study eye; or (5) loss of light perception...
August 28, 2017: Journal of Glaucoma
https://www.readbyqxmd.com/read/28835790/n-acylbenzenesulfonamide-dihydro-1-3-4-oxadiazole-hybrids-seeking-selectivity-toward-carbonic-anhydrase-isoforms
#14
Giulia Bianco, Rita Meleddu, Simona Distinto, Filippo Cottiglia, Marco Gaspari, Claudia Melis, Angela Corona, Rossella Angius, Andrea Angeli, Domenico Taverna, Stefano Alcaro, Janis Leitans, Andris Kazaks, Kaspars Tars, Claudiu T Supuran, Elias Maccioni
A series of N-acylbenzenesulfonamide dihydro-1,3,4-oxadiazole hybrids (EMAC8000a-m) was designed and synthesized with the aim to target tumor associated carbonic anhydrase (hCA) isoforms IX and XII. Most of the compounds were selective inhibitors of the tumor associated hCA XII. Moreover, resolution of EMAC8000d racemic mixture led to the isolation of the levorotatory eutomer exhibiting an increase of hCA XII inhibition potency and selectivity with respect to hCA II. Computational studies corroborated these data...
August 10, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28830777/biological-evaluation-of-p-toluene-sulphonylhydrazone-as-carbonic-anhydrase-ix-inhibitors-an-approach-to-fight-hypoxia-induced-tumors
#15
Aarfa Queen, Parvez Khan, Danish Idrees, Amir Azam, Md Imtaiyaz Hassan
To find potential inhibitors of human carbonic anhydrase IX (CAIX), we have successfully deigned, synthesized and characterized three p-Toluene sulphonylhydrazone derivatives (1-3). Molecular docking studies provided the structural basis of CAIX inhibition and a deeper insight into the protein-ligand interactions. p-Toluene sulphonylhydrazone derivatives show a well organized conformational compatibility with the active site of CAIX. This protein-ligand complex was stabilized by several non-covalent interactions offered by residues present in the active site cavity...
August 19, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28817930/identification-of-a-new-zinc-binding-chemotype-by-fragment-screening
#16
Panagiotis K Chrysanthopoulos, Prashant Mujumdar, Lucy A Woods, Olan Dolezal, Bin Ren, Thomas S Peat, Sally-Ann Poulsen
The discovery of a new zinc binding chemotype from screening a nonbiased fragment library is reported. Using the orthogonal fragment screening methods of native state mass spectrometry and surface plasmon resonance a 3-unsubstituted 2,4-oxazolidinedione fragment was found to have low micromolar binding affinity to the zinc metalloenzyme carbonic anhydrase II (CA II). This affinity approached that of fragment sized primary benzenesulfonamides, the classical zinc binding group found in most CA II inhibitors. Protein X-ray crystallography established that 3-unsubstituted 2,4-oxazolidinediones bound to CA II via an interaction of the acidic ring nitrogen with the CA II active site zinc, as well as two hydrogen bonds between the oxazolidinedione ring oxygen and the CA II protein backbone...
September 1, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28803235/18f-fdg-uptake-in-well-differentiated-neuroendocrine-tumors-correlates-with-both-ki-67-and-vhl-pathway-inactivation
#17
Margot Bucau, Astrid Laurent-Bellue, Nicolas Poté, Olivia Hentic, Jérôme Cros, Nidaa Mikail, Vinciane Rebours, Philippe Ruszniewski, Rachida Lebtahi, Anne Couvelard
<br>Introduction: 18FDG PET-scanner positivity correlates with poor prognosis in neuroendocrine neoplasms (NEN). Glucose transporter 1 (GLUT1) and carbonic anhydrase 9 (CA9) are markers of agressivity in tumors. Together with pVHL, they are involved in tumor cell metabolism via the hypoxia-inducible factor (HIF) signaling pathway. The aim of this study was to compare, in a series of well-differentiated neuroendocrine tumors (NET), the 18-FDG uptake and expression of proliferation marker Ki-67, GLUT-1, CA9 and pVHL...
August 11, 2017: Neuroendocrinology
https://www.readbyqxmd.com/read/28802125/novel-4-3-4-oxo-5-2-oxoindolin-3-ylidene-thiazolidin-2-ylidene-amino-benzenesulfonamides-synthesis-carbonic-anhydrase-inhibitory-activity-anticancer-activity-and-molecular-modelling-studies
#18
Wagdy M Eldehna, Mahmoud F Abo-Ashour, Alessio Nocentini, Paola Gratteri, Ibrahim H Eissa, Mohamed Fares, Omnia E Ismael, Hazem A Ghabbour, Mahmoud M Elaasser, Hatem A Abdel-Aziz, Claudiu T Supuran
Herein we report the synthesis of two series of novel 4/3-((4-oxo-5-(2-oxoindolin-3-ylidene)thiazolidin-2-ylidene)amino)benzenesulfonamides (4a-m and 7a-g). All the newly prepared sulfonamides were in vitro investigated as inhibitors of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1) isoforms hCA I, II, IV and IX, using a stopped-flow CO2 hydrase assay. In particular, hCA isoforms II and IX (tumor-associated) were more susceptible to inhibition by the synthesized derivatives, with KIs in the range of 2...
August 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28800181/synephrine-and-phenylephrine-act-as-%C3%AE-amylase-%C3%AE-glycosidase-acetylcholinesterase-butyrylcholinesterase-and-carbonic-anhydrase-enzymes-inhibitors
#19
Parham Taslimi, Hülya Akıncıoglu, İlhami Gülçin
In this paper, synephrine and phenylephrine compounds showed excellent inhibitory effects against human carbonic anhydrase (hCA) isoforms I and II, α-amylase, α-glycosidase, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE). Synephrine and phenylephrine had Ki values of 199.02 ± 16.01 and 65.01 ± 5.00 μM against hCA I and 336.02 ± 74.01 and 92.04  ±  18.03 μM against hCA II, respectively. On the other hand, their Ki values were found to be 169.10  ±  80.03 and 88.03  ±  5...
August 11, 2017: Journal of Biochemical and Molecular Toxicology
https://www.readbyqxmd.com/read/28797449/nomogram-for-risk-prediction-of-malignant-transformation-in-oral-leukoplakia-patients-using-combined-biomarkers
#20
Xianglan Zhang, Ki-Yeol Kim, Zhenlong Zheng, Shadavlonjid Bazarsad, Jin Kim
OBJECTIVE: Squamous cell carcinomas (SCC) are the most common malignancies in the oral mucosa; these carcinomas have been preceded by potentially malignant oral disorders (PMODs), mostly oral leukoplakia (OL). No specific biomarker has been widely accepted for predicting the risk of malignant transformation of PMODs. The aim of this study was to develop an accurate prediction model for the malignant transformation of OL using clinical variables and candidate biomarkers. MATERIALS AND METHODS: To achieve this goal, 10 candidate biomarkers that had previously been reported as useful molecules were investigated: P53, Ki-67, P16, β-catenin, c-jun, c-met, insulin like growth factor II mRNA-binding protein (IMP-3), cyclooxygenase (COX-2), podoplanin (PDPN) and carbonic anhydrase 9 (CA9)...
September 2017: Oral Oncology
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