About: Structural basis for the interaction between carbonic anhydrase and 1,2,3,4-tetrahydroisoquinolin-2-ylsulfonamides     Goto   Sponge   NotDistinct   Permalink

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Description
  • lsoquinolinesulfonamides inhibit human carbonic anhydrases (hCAs) and display selectivity toward therapeutically relevant isozymes. The crystal structure of hCA 11 in complex with 6,7-dimethoxy-1-methyl-1,2,3,4-tetrahydroisoquinolin-2-ylsulfonamide revealed unusual inhibitor binding. Structural analyses allowed for discerning the fine details of the inhibitor binding mode to the active site, thus providing clues for the future design of even more selective inhibitors for druggable isoforms such as the cancer associated hCA IX and neuronal hCA VII.
  • lsoquinolinesulfonamides inhibit human carbonic anhydrases (hCAs) and display selectivity toward therapeutically relevant isozymes. The crystal structure of hCA 11 in complex with 6,7-dimethoxy-1-methyl-1,2,3,4-tetrahydroisoquinolin-2-ylsulfonamide revealed unusual inhibitor binding. Structural analyses allowed for discerning the fine details of the inhibitor binding mode to the active site, thus providing clues for the future design of even more selective inhibitors for druggable isoforms such as the cancer associated hCA IX and neuronal hCA VII. (en)
Title
  • Structural basis for the interaction between carbonic anhydrase and 1,2,3,4-tetrahydroisoquinolin-2-ylsulfonamides
  • Structural basis for the interaction between carbonic anhydrase and 1,2,3,4-tetrahydroisoquinolin-2-ylsulfonamides (en)
skos:prefLabel
  • Structural basis for the interaction between carbonic anhydrase and 1,2,3,4-tetrahydroisoquinolin-2-ylsulfonamides
  • Structural basis for the interaction between carbonic anhydrase and 1,2,3,4-tetrahydroisoquinolin-2-ylsulfonamides (en)
skos:notation
  • RIV/68378050:_____/11:00365071!RIV12-AV0-68378050
http://linked.open...avai/predkladatel
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • P(GA203/09/0820), Z(AV0Z40550506), Z(AV0Z50520514)
http://linked.open...iv/cisloPeriodika
  • 7
http://linked.open...vai/riv/dodaniDat
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  • 232731
http://linked.open...ai/riv/idVysledku
  • RIV/68378050:_____/11:00365071
http://linked.open...riv/jazykVysledku
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  • carbonic anhydrase; isoquinolinesulfonamides; selective inhibition; crystal structure (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • US - Spojené státy americké
http://linked.open...ontrolniKodProRIV
  • [6B1C07ECCC32]
http://linked.open...i/riv/nazevZdroje
  • Journal of Medicinal Chemistry
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
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http://linked.open...vavai/riv/projekt
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http://linked.open...v/svazekPeriodika
  • 54
http://linked.open...iv/tvurceVysledku
  • Brynda, Jiří
  • Pachl, Petr
  • Řezáčová, Pavlína
  • Agnello, S.
  • Chimirri, A.
  • Gitto, R.
  • Mader, Pavel
  • Supuran, C. T.
http://linked.open...ain/vavai/riv/wos
  • 000289215700048
http://linked.open...n/vavai/riv/zamer
issn
  • 0022-2623
number of pages
http://bibframe.org/vocab/doi
  • 10.1021/jm2000213
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