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000140090 1001_ $$aBaranauskiene, L.
000140090 1101_ $$aDESY$$bExperiments with synchrotron radiation$$bEuropean Molecular Biology Laboratory
000140090 245__ $$aInhibition and binding studies of carbonic anhydrase isozymes I, II and IX with benzimidazo[1,2-c][1,2,3]thiadiazole-7-sulphonamides
000140090 260__ $$aLondon$$bInforma Healthcare$$c2010
000140090 300__ $$a863-870
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000140090 440_0 $$0PERI:(DE-600)2049579-1$$aJ Enzyme Inhib Med Chem$$v25$$x1475-6374
000140090 500__ $$3Converted on 2013-05-30 09:37
000140090 500__ $$3Converted on 2013-06-21 19:21
000140090 520__ $$aThe binding and inhibition strength of a series of benzimidazo[1,2-c][1,2,3]thiadiazole-7-sulphonamides were determined for recombinant human carbonic anhydrase isoforms I, II, and IX. The inhibition strength was determined by a stop-flow method to measure carbon dioxide hydration. Inhibitor-enzyme binding was determined by two biophysical techniques--isothermal titration calorimetry and thermal shift assay. The co-crystal structure was determined by X-ray crystallography. Comparing the results obtained using three different inhibition and binding methods increased the accuracy of compound affinity ranking and the ability to determine compound inhibitory specificity towards a particular carbonic anhydrase isoform. In most cases, all three methods yielded the same results despite using very different approaches to measure the binding and inhibition reactions. Some of the compounds studied are submicromolar inhibitors of the isoform IX, a prominent cancer target.
000140090 536__ $$0G:(DE-H253)POF2-No-Ref-20130405$$aFS Beamline without reference (POF2-544)$$cPOF2-544$$fPOF II$$x0
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000140090 650_2 $$2MeSH$$aAlgorithms
000140090 650_2 $$2MeSH$$aAntigens, Neoplasm: genetics
000140090 650_2 $$2MeSH$$aAntigens, Neoplasm: metabolism
000140090 650_2 $$2MeSH$$aAntineoplastic Agents: chemistry
000140090 650_2 $$2MeSH$$aAntineoplastic Agents: metabolism
000140090 650_2 $$2MeSH$$aAntineoplastic Agents: pharmacology
000140090 650_2 $$2MeSH$$aBenzimidazoles: chemistry
000140090 650_2 $$2MeSH$$aBenzimidazoles: metabolism
000140090 650_2 $$2MeSH$$aBenzimidazoles: pharmacology
000140090 650_2 $$2MeSH$$aCalorimetry: methods
000140090 650_2 $$2MeSH$$aCarbonic Anhydrase I: antagonists & inhibitors
000140090 650_2 $$2MeSH$$aCarbonic Anhydrase I: genetics
000140090 650_2 $$2MeSH$$aCarbonic Anhydrase I: metabolism
000140090 650_2 $$2MeSH$$aCarbonic Anhydrase II: antagonists & inhibitors
000140090 650_2 $$2MeSH$$aCarbonic Anhydrase II: chemistry
000140090 650_2 $$2MeSH$$aCarbonic Anhydrase II: genetics
000140090 650_2 $$2MeSH$$aCarbonic Anhydrase II: metabolism
000140090 650_2 $$2MeSH$$aCarbonic Anhydrase Inhibitors: chemistry
000140090 650_2 $$2MeSH$$aCarbonic Anhydrase Inhibitors: metabolism
000140090 650_2 $$2MeSH$$aCarbonic Anhydrase Inhibitors: pharmacology
000140090 650_2 $$2MeSH$$aCarbonic Anhydrases: genetics
000140090 650_2 $$2MeSH$$aCarbonic Anhydrases: metabolism
000140090 650_2 $$2MeSH$$aCatalytic Domain: drug effects
000140090 650_2 $$2MeSH$$aCrystallography, X-Ray
000140090 650_2 $$2MeSH$$aHumans
000140090 650_2 $$2MeSH$$aKinetics
000140090 650_2 $$2MeSH$$aLigands
000140090 650_2 $$2MeSH$$aMolecular Conformation
000140090 650_2 $$2MeSH$$aRecombinant Proteins: antagonists & inhibitors
000140090 650_2 $$2MeSH$$aRecombinant Proteins: chemistry
000140090 650_2 $$2MeSH$$aRecombinant Proteins: metabolism
000140090 650_2 $$2MeSH$$aSulfonamides: chemistry
000140090 650_2 $$2MeSH$$aSulfonamides: metabolism
000140090 650_2 $$2MeSH$$aSulfonamides: pharmacology
000140090 650_2 $$2MeSH$$aThiadiazoles: chemistry
000140090 650_2 $$2MeSH$$aThiadiazoles: metabolism
000140090 650_2 $$2MeSH$$aThiadiazoles: pharmacology
000140090 650_7 $$00$$2NLM Chemicals$$aAntigens, Neoplasm
000140090 650_7 $$00$$2NLM Chemicals$$aAntineoplastic Agents
000140090 650_7 $$00$$2NLM Chemicals$$aBenzimidazoles
000140090 650_7 $$00$$2NLM Chemicals$$aCarbonic Anhydrase Inhibitors
000140090 650_7 $$00$$2NLM Chemicals$$aLigands
000140090 650_7 $$00$$2NLM Chemicals$$aRecombinant Proteins
000140090 650_7 $$00$$2NLM Chemicals$$aSulfonamides
000140090 650_7 $$00$$2NLM Chemicals$$aThiadiazoles
000140090 650_7 $$0EC 4.2.1.-$$2NLM Chemicals$$aCarbonic Anhydrase I
000140090 650_7 $$0EC 4.2.1.-$$2NLM Chemicals$$aCarbonic Anhydrase II
000140090 650_7 $$0EC 4.2.1.1$$2NLM Chemicals$$aCA9 protein, human
000140090 650_7 $$0EC 4.2.1.1$$2NLM Chemicals$$aCarbonic Anhydrases
000140090 693__ $$0EXP:(DE-H253)Unknown-BL-20150101$$6EXP:(DE-H253)Unknown-BL-20150101$$fUnknown DESY Beamline$$x0
000140090 7001_ $$aHilvo, M.
000140090 7001_ $$aMatuliene, J.
000140090 7001_ $$aGolovenko, D.
000140090 7001_ $$aManakova, E.
000140090 7001_ $$aDudutiene, V.
000140090 7001_ $$aMichailoviene, V.
000140090 7001_ $$aTorresan, J.
000140090 7001_ $$aJachno, J.
000140090 7001_ $$aParkkila, S.
000140090 7001_ $$aMaresca, A.
000140090 7001_ $$aSupuran, C.
000140090 7001_ $$aGrazulis, S.
000140090 7001_ $$aMatulis, D.
000140090 773__ $$0PERI:(DE-600)2049579-1$$a10.3109/14756360903571685$$gVol. 25, p. 863-870$$p863-870$$q25<863-870$$tJournal of enzyme inhibition and medicinal chemistry$$v25$$x1475-6374$$y2010
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