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https://www.readbyqxmd.com/read/28087816/acetazolamide-potentiates-the-afferent-drive-to-prefrontal-cortex-in%C3%A2-vivo
#1
Lezio S Bueno-Junior, Rafael N Ruggiero, Matheus T Rossignoli, Elaine A Del Bel, Joao P Leite, Osvaldo D Uchitel
The knowledge on real-time neurophysiological effects of acetazolamide is still far behind the wide clinical use of this drug. Acetazolamide - a carbonic anhydrase inhibitor - has been shown to affect the neuromuscular transmission, implying a pH-mediated influence on the central synaptic transmission. To start filling such a gap, we chose a central substrate: hippocampal-prefrontal cortical projections; and a synaptic phenomenon: paired-pulse facilitation (a form of synaptic plasticity) to probe this drug's effects on interareal brain communication in chronically implanted rats...
January 2017: Physiological Reports
https://www.readbyqxmd.com/read/28079504/anti-carbonic-anhydrase-autoantibodies-and-serum-beta-2-microglobulin-correlate-with-the-clinessdai-score-in-patients-with-sj%C3%A3-gren-s-syndrome
#2
Marja Pertovaara, Seppo Parkkila, Markku Korpela
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January 5, 2017: Clinical and Experimental Rheumatology
https://www.readbyqxmd.com/read/28076854/open-angle-glaucoma-drug-development-pipeline-during-the-last-20-years-1995-2015
#3
André Vicente, Sylvie Prud'homme, Joana Ferreira, Luís Abegão Pinto, Ingeborg Stalmans
OBJECTIVES: To analyse drug development for open-angle glaucoma during the last 20 years. METHODS: Research was performed by referring to clinical trials registered at the International Clinical Trials Registry Platform (ICTRP). A search for the condition "open-angle glaucoma" with the intervention "drug" was performed. We included trials registered from 01/01/1995 to 01/01/2015, only involving studies in phases 1, 2, and 3. Only studies resorting to novel treatment strategies (either novel drugs or yet-untested fixed associations of approved medication) were considered...
January 12, 2017: Ophthalmic Research
https://www.readbyqxmd.com/read/28075587/design-and-synthesis-of-novel-non-steroidal-anti-inflammatory-drugs-and-carbonic-anhydrase-inhibitors-hybrids-nsaids-cais-for-the-treatment-of-rheumatoid-arthritis
#4
Silvia Bua, Lorenzo Di Cesare Mannelli, Daniela Vullo, Carla Ghelardini, Gian Luca Bartolucci, Andrea Scozzafava, Claudiu T Supuran, Fabrizio Carta
We report the synthesis of a series of 6- and 7-substituted coumarins with commercially available NSAIDs (13a-h and 14a-h) as potential tools for the treatment of RA and related diseases. All compounds resulted effective in inhibiting the RA over-expressed hCA IV with KIs comprised between 0.44-9.8 nM. Among the other RA relevant hCA isoforms (i.e. IX and XII), compounds 13f and 14a,b resulted commonly effective in inhibiting their activity. The antihyperalgesic activity of such compounds was assessed by means of the Paw-pressure and Incapacitance tests using an in vivo RA model induced by CFA...
January 11, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28075522/crucial-role-of-carbonic-anhydrase-ix-in-tumorigenicity-of-xenotransplanted-adult-t-cell-leukemia-derived-cells
#5
Kentaro Nasu, Kazunori Yamaguchi, Tomoka Takanashi, Keiichi Tamai, Ikuro Sato, Shoji Ine, Osamu Sasaki, Kennichi Satoh, Nobuyuki Tanaka, Yuetsu Tanaka, Takuya Fukushima, Hideo Harigae, Kazuo Sugamura
Carbonic anhydrase IX (CA9) is a membrane-associated carbonic anhydrase that regulates cellular pH, is upregulated in various solid tumors, and is considered to be a therapeutic target. Here, we describe the essential role of CA9 in the tumorigenicity of cells derived from human adult T-cell leukemia/lymphoma (ATL). We previously established the highly tumorigenic ST1-N6 subline from the ATL-derived ST1 cell line by serial xenotransplantation in NOG mice. In the present study, we first show that CA9 expression is strongly enhanced in ST1-N6 cells...
January 11, 2017: Cancer Science
https://www.readbyqxmd.com/read/28074971/bio-orthogonal-click-and-release-donation-of-caged-carbonyl-sulfide-cos-and-hydrogen-sulfide-h2s
#6
Andrea K Steiger, Yang Yang, Maksim Royzen, Michael D Pluth
Hydrogen sulfide (H2S) is an important biomolecule with high therapeutic potential. Here we leverage the inverse-electron demand Diels-Alder (IEDDA) click reaction between a thiocarbamate-functionalized trans-cyclooctene and a tetrazine to deliver carbonyl sulfide (COS), which is quickly converted to H2S by the uniquitous enzyme carbonic anhydrase (CA), thus providing a new strategy for bio-orthogonal COS/H2S donation.
January 11, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28074546/-hypoxia-and-cellular-metabolism-in-tumour-pathophysiology
#7
Scott K Parks, Yann Cormerais, Jacques Pouysségur
Cancer cells are optimized for growth and survival via an ability to outcompete normal cells in their microenvironment. Many of these advantageous cellular adaptations are promoted by the pathophysiological hypoxia that arises in solid tumours due to incomplete vascularisation. Tumour cells are thus faced with the challenge of an increased need for nutrients to support the drive for proliferation in the face of a diminished extracellular supply. Among the many modifications occurring in tumour cells, Hypoxia Inducible Factors (HIFs) act as essential drivers of key pro-survival pathways via the promotion of numerous membrane and cytosolic proteins...
January 10, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28067526/extraction-of-thermodynamic-parameters-of-protein-unfolding-using-parallelized-differential-scanning-fluorimetry
#8
Thaiesha A Wright, Jamie M Stewart, Richard Christopher Page, Dominik Konkolewicz
Thermodynamic properties of protein unfolding have been extensively studied; however, the methods used have typically required significant preparation time and high protein concentrations. Here, we present a facile, simple, and parallelized differential scanning fluorimetry (DSF) method that enables thermodynamic parameters of protein unfolding to be extracted. This method assumes a two-state, reversible protein unfolding mechanism and provides the capacity to quickly analyze the biophysical mechanisms of changes in protein stability and to more thoroughly characterize the effect of mutations, additives, inhibitors, or pH...
January 9, 2017: Journal of Physical Chemistry Letters
https://www.readbyqxmd.com/read/28067010/hit-validation-methodologies-for-ligands-isolated-from-dna-encoded-chemical-libraries
#9
Gunther Zimmermann, Yizhou Li, Ulrike Rieder, Martin Mattarella, Dario Neri, Jörg Scheuermann
DNA-encoded chemical libraries (DECLs) are large collections of compounds linked to DNA fragments, serving as amplifiable barcodes, which can be screened on target proteins of interest. In typical DECL selections, preferential binders are identified by high-throughput DNA sequencing, comparing their frequency before and after the affinity capture step. Hits identified in this procedure need to be confirmed, by resynthesis and by performing affinity measurements. In this article, we present novel methods, based on the hybridization of oligonucleotide conjugates with fluorescently-labeled complementary oligonucleotides, which facilitate the determination of affinity constants and kinetic dissociation constants...
January 9, 2017: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/28065864/value-of-ph-regulators-in-the-diagnosis-prognosis-and-treatment-of-cancer
#10
REVIEW
Sara Granja, Diana Tavares-Valente, Odília Queirós, Fátima Baltazar
Altered metabolism, associated with acidification of the extracellular milieu, is one of the major features of cancer. As pH regulation is crucial for the maintenance of all biological functions, cancer cells rely on the activity of lactate exporters and proton transporters to regulate their intracellular pH. The major players in cancer pH regulation are proton pump ATPases, sodium-proton exchangers (NHEs), monocarboxylate transporters (MCTs), carbonic anhydrases (CAs) and anion exchangers (AEs), which have been shown to be upregulated in several human malignancies...
January 5, 2017: Seminars in Cancer Biology
https://www.readbyqxmd.com/read/28065499/benzenesulfonamide-bearing-imidazothiadiazole-and-thiazolotriazole-scaffolds-as-potent-tumor-associated-human-carbonic-anhydrase-ix-and-xii-inhibitors
#11
Rajiv Kumar, Silvia Bua, Sita Ram, Sonia Del Prete, Clemente Capasso, Claudiu T Supuran, Pawan K Sharma
Two series of 20 novel heterocyclic compounds, imidazothiadiazoles (3a-3j) and thiazolotriazoles (4a-4j) bearing benzenesulfonamide moiety were synthesized in order to investigate the inhibition potential of both scaffolds against four selected human carbonic anhydrase isoforms (hCA I, II, IX & XII). Against human isoform hCA I, compounds 3j, 4a-4c, and 4j showed better inhibition potential (Ki<100nM) than the standard drug acetazolamide (AZA). Against hCA II, all the compounds showed moderate inhibition with the exception of 3a which showed nearly two fold better profile compared to AZA...
December 29, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28062849/interplay-between-a-cytosolic-and-a-cell-surface-carbonic-anhydrase-in-ph-homeostasis-and-acid-tolerance-of-leishmania
#12
Dhiman Sankar Pal, Mazharul Abbasi, Dipon Kumar Mondal, Binitha Anu Varghese, Ritama Paul, Shalini Singh, Rupak Datta
Leishmania parasites have evolved to endure the acidic phagolysosomal environment within host macrophages. How Leishmania cells maintain near-neutral intracellular pH and proliferate in such proton-rich milieu remains poorly understood. We report here that for thriving in acidic condition Leishmania major relies on a cytosolic and a cell surface carbonic anhydrase viz. LmCA1 and LmCA2. Upon exposure to acidic medium, intracellular pH of the LmCA1(+/-), LmCA2(+/-) and LmCA1(+/-): LmCA2(+/-) mutant strains dropped by varying extents that led to cell cycle delay, growth retardation and morphological abnormalities...
January 6, 2017: Journal of Cell Science
https://www.readbyqxmd.com/read/28058154/intravitreal-dexamethasone-implant-ozurdex-for-refractory-macular-edema-secondary-to-retinitis-pigmentosa
#13
Nurgül Örnek, Kemal Örnek, İnci Elif Erbahçeci
Macular edema (ME) in retinitis pigmentosa (RP) often impairs central vision dramatically. A 41-year-old woman diagnosed with RP was referred to our outpatient clinic due to severe visual deterioration in both eyes. The patient was treated with topical carbonic anhydrase inhibitors, topical corticosteroids and intravitreal triamcinolone acetonide injections, but her ME recurred. Intravitreal 0.7 mg dexamethasone implant (Ozurdex, Allergan) was administered into both eyes without complications. On the fourth day after both injections, visual acuity improved and ME almost totally resolved...
August 2016: Turkish Journal of Ophthalmology
https://www.readbyqxmd.com/read/28057408/dithiocarbamates-effectively-inhibit-the-%C3%AE-carbonic-anhydrase-from-the-dandruff-producing-fungus-malassezia-globosa
#14
Daniela Vullo, Sonia Del Prete, Alessio Nocentini, Sameh M Osman, Zeid AlOthman, Clemente Capasso, Murat Bozdag, Fabrizio Carta, Paola Gratteri, Claudiu T Supuran
A series of dithiocarbamates (DTCs) was investigated for the inhibition of the β-class carbonic anhydrase (CAs, EC 4.2.1.1) from the fungal parasite Malassezia globosa, MgCA, a validated anti-dandruff drug target. These DTCs incorporate various scaffold, among which those of N,N-dimethylaminoethylenediamine, the aminoalcohols with 3-5 carbon atoms in their molecule, 3-amino-quinuclidine, piperidine, morpholine and piperazine derivatives, as well as phenethylamine and its 4-sulfamoylated derivative. Several DTCs resulted more effective in inhibiting MgCA compared to the standard sulfonamide drug acetazolamide (KI of 74μM), with KIs ranging between 383 and 6235nM...
December 27, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28055960/-genetic-disruption-of-the-phi-regulating-proteins-na-h-exchanger-1-slc9a1-and-carbonic-anhydrase-9-severely-reduces-growth-of-colon-cancer-cells
#15
Scott K Parks, Yann Cormerais, Jerome Durivault, Jacques Pouyssegur
Hypoxia and extracellular acidosis are pathophysiological hallmarks of aggressive solid tumors. Regulation of intracellular pH (pHi) is essential for the maintenance of tumor cell metabolism and proliferation in this microenvironment and key proteins involved in pHi regulation are of interest for therapeutic development. Carbonic anhydrase 9 (CA9) is one of the most robustly regulated proteins by the hypoxia inducible factor (HIF) and contributes to pHi regulation. Here, we have investigated for the first time, the role of CA9 via complete genomic knockout (ko) and compared its impact on tumor cell physiology with the essential pHi regulator Na+/H+ exchanger 1 (NHE1)...
December 30, 2016: Oncotarget
https://www.readbyqxmd.com/read/28051026/blood-oxygenation-level-dependent-magnetic-resonance-imaging-of-breast-cancer-correlation-with-carbonic-anhydrase-ix-and-vascular-endothelial-growth-factor
#16
Ying Wang, Min Liu, Mu-Lan Jin
BACKGROUND: Blood oxygenation level-dependent magnetic resonance imaging (BOLD-MRI) is a functional MRI technique which involves using the paramagnetic properties of deoxyhemoglobin to image the local tissue oxygen concentration. The purpose of this study was to investigate whether BOLD-MRI could evaluate hypoxia and angiogenesis of breast invasive ductal carcinoma (IDC). METHODS: Ninety-eight female patients with IDC were retrospectively included in this research...
2017: Chinese Medical Journal
https://www.readbyqxmd.com/read/28049405/inhibition-of-bacterial-carbonic-anhydrases-as-a-novel-approach-to-escape-drug-resistance
#17
Clemente Capasso, Claudiu Supuran
BACKGROUND: Clinically used antibiotics act through one of these four mechanisms: cell wall biosynthesis inhibition, inhibition of protein biosynthesis, interference with DNA and RNA synthesis and the folate pathway. OBJECTIVE: The metalloenzymes carbonic anhydrases (CAs, EC 4.2.1.1) widespread in microorganisms and present as three genetically distinct families may be considered for the design of antiinfective agents with a different mechanism of action compared to the clinically used antibiotics...
January 3, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28048959/expression-and-localization-of-carbonic-anhydrase-genes-in-the-serpulid-polychaete-hydroides-elegans
#18
Grant Batzel, Brian T Nedved, Michael G Hadfield
The metalloenzyme, carbonic anhydrase (CA), catalyzes the reversible hydration of carbon dioxide into bicarbonate, and is responsible for biomineralization processes in animals. In the Annelida, the marine worms in the family Serpulidae are typified by the construction of calcium carbonate tubes. Hydroides elegans, a common member of warmwater biofouling communities around the world, provides an outstanding model for studies of calcification. To better understand the molecular process of biomineralization in H...
December 2016: Biological Bulletin
https://www.readbyqxmd.com/read/28043719/synthesis-characterization-anticancer-antimicrobial-and-carbonic-anhydrase-inhibition-profiles-of-novel-3ar-4s-7r-7as-2-4-e-3-3-aryl-acryloyl-phenyl-3a-4-7-7a-tetrahydro-1h-4-7-methanoisoindole-1-3-2h-dione-derivatives
#19
Umit M Kocyigit, Yakup Budak, Meliha Burcu Gürdere, Şaban Tekin, Tuğba Kul Köprülü, Fatih Ertürk, Kezban Özcan, İlhami Gülçin, Mustafa Ceylan
In the present study, a series of new hybrid compounds containing chalcone and methanoisoindole units 7a-n ((3aR,4S,7R,7aS)-2-(4-((E)-3-(3-aryl)acryloyl) phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione) were synthesized, characterized and investigated for their anticancer activity against C6 gliocarcinoma cell in rats, and antimicrobial activity against some human pathogen microorganisms. The compounds 7e, 7h, 7j, 7k, 7L and 7n showed very high anticancer activity with the inhibition range of 80...
December 23, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28040798/a-mem1-like-motif-directs-mesophyll-cell-specific-expression-of-the-gene-encoding-the-c4-carbonic-anhydrase-in-flaveria
#20
Udo Gowik, Stefanie Schulze, Montserrat Saladié, Vivien Rolland, Sandra K Tanz, Peter Westhoff, Martha Ludwig
The first two reactions of C4 photosynthesis are catalysed by carbonic anhydrase (CA) and phosphoenolpyruvate carboxylase (PEPC) in the leaf mesophyll (M) cell cytosol. Translatome experiments using a tagged ribosomal protein expressed under the control of M and bundle-sheath (BS) cell-specific promoters showed transcripts encoding CA3 from the C4 species Flaveria bidentis were highly enriched in polysomes from M cells relative to those of the BS. Localisation experiments employing a CA3-green fluorescent protein fusion protein showed F...
December 30, 2016: Journal of Experimental Botany
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