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@ARTICLE{Baranauskiene:140090,
author = {Baranauskiene, L. and Hilvo, M. and Matuliene, J. and
Golovenko, D. and Manakova, E. and Dudutiene, V. and
Michailoviene, V. and Torresan, J. and Jachno, J. and
Parkkila, S. and Maresca, A. and Supuran, C. and Grazulis,
S. and Matulis, D. and DESY},
title = {{I}nhibition and binding studies of carbonic anhydrase
isozymes {I}, {II} and {IX} with
benzimidazo[1,2-c][1,2,3]thiadiazole-7-sulphonamides},
journal = {Journal of enzyme inhibition and medicinal chemistry},
volume = {25},
issn = {1475-6374},
address = {London},
publisher = {Informa Healthcare},
reportid = {PHPPUBDB-24676},
pages = {863-870},
year = {2010},
abstract = {The 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.},
keywords = {Algorithms / Antigens, Neoplasm: genetics / Antigens,
Neoplasm: metabolism / Antineoplastic Agents: chemistry /
Antineoplastic Agents: metabolism / Antineoplastic Agents:
pharmacology / Benzimidazoles: chemistry / Benzimidazoles:
metabolism / Benzimidazoles: pharmacology / Calorimetry:
methods / Carbonic Anhydrase I: antagonists $\&$ inhibitors
/ Carbonic Anhydrase I: genetics / Carbonic Anhydrase I:
metabolism / Carbonic Anhydrase II: antagonists $\&$
inhibitors / Carbonic Anhydrase II: chemistry / Carbonic
Anhydrase II: genetics / Carbonic Anhydrase II: metabolism /
Carbonic Anhydrase Inhibitors: chemistry / Carbonic
Anhydrase Inhibitors: metabolism / Carbonic Anhydrase
Inhibitors: pharmacology / Carbonic Anhydrases: genetics /
Carbonic Anhydrases: metabolism / Catalytic Domain: drug
effects / Crystallography, X-Ray / Humans / Kinetics /
Ligands / Molecular Conformation / Recombinant Proteins:
antagonists $\&$ inhibitors / Recombinant Proteins:
chemistry / Recombinant Proteins: metabolism / Sulfonamides:
chemistry / Sulfonamides: metabolism / Sulfonamides:
pharmacology / Thiadiazoles: chemistry / Thiadiazoles:
metabolism / Thiadiazoles: pharmacology / Antigens, Neoplasm
(NLM Chemicals) / Antineoplastic Agents (NLM Chemicals) /
Benzimidazoles (NLM Chemicals) / Carbonic Anhydrase
Inhibitors (NLM Chemicals) / Ligands (NLM Chemicals) /
Recombinant Proteins (NLM Chemicals) / Sulfonamides (NLM
Chemicals) / Thiadiazoles (NLM Chemicals) / Carbonic
Anhydrase I (NLM Chemicals) / Carbonic Anhydrase II (NLM
Chemicals) / CA9 protein, human (NLM Chemicals) / Carbonic
Anhydrases (NLM Chemicals)},
cin = {HASYLAB / EMBL},
ddc = {570},
cid = {$I:(DE-H253)HASYLAB_-2012_-20130307$ /
$I:(DE-H253)EMBL_-2012_-20130307$},
pnm = {FS Beamline without reference (POF2-544)},
pid = {G:(DE-H253)POF2-No-Ref-20130405},
experiment = {EXP:(DE-H253)Unknown-BL-20150101},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:20166809},
UT = {WOS:000283939300016},
doi = {10.3109/14756360903571685},
url = {https://bib-pubdb1.desy.de/record/140090},
}