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| Description
| - The monoclonal antibodies 1696 and F11.2.32 strongly inhibit the activity of wild-type HIV-1 protease (PR) by binding to epitopes at the enzyme N-terminus (residues 1-6) and flap residues 36-46, respectively. Here we demonstrate that these antibodies are also potent inhibitors of PR variants resistant to active-site inhibitors used as anti-AIDS drugs. Our in vitro experiments revealed that the inhibitory potency of single-chain fragments (scFv) of these antibodies is not significantly affected by the presence of mutations in PR; inhibition constants for drug-resistant protease variants are 5-11 nM and 13-169 nM for scFv1696 and for scFvF11.2.32, respectively. Tethered dimer of HIV-1 PR variant proved to be a model protease variant resistant to dissociative inhibition by 1696, and, strikingly, it also displayed resistance to inhibition by F11.2.32, suggesting that dimer dissociation also plays a role in the inhibitory action of F11.2.32.
- The monoclonal antibodies 1696 and F11.2.32 strongly inhibit the activity of wild-type HIV-1 protease (PR) by binding to epitopes at the enzyme N-terminus (residues 1-6) and flap residues 36-46, respectively. Here we demonstrate that these antibodies are also potent inhibitors of PR variants resistant to active-site inhibitors used as anti-AIDS drugs. Our in vitro experiments revealed that the inhibitory potency of single-chain fragments (scFv) of these antibodies is not significantly affected by the presence of mutations in PR; inhibition constants for drug-resistant protease variants are 5-11 nM and 13-169 nM for scFv1696 and for scFvF11.2.32, respectively. Tethered dimer of HIV-1 PR variant proved to be a model protease variant resistant to dissociative inhibition by 1696, and, strikingly, it also displayed resistance to inhibition by F11.2.32, suggesting that dimer dissociation also plays a role in the inhibitory action of F11.2.32. (en)
- Monoklonální protilátky 1696 a F11.2.32 silně inhibují aktivitu přirozené HIV-1 proteasy (PR) vazbou na N-konec enzymu (aminokyseliny 1-6), resp. na oblast chlopní (aminokyseliny 36-46). Tyto protilátky jsou také dobrými inhibitory HIV-proteas rezistentních k inhibitorům aktivního místa, které se používají při léčbě AIDS. In vitro experimenty ukazují, že inhibiční potenciál rekombinantních single-chain fragmentů (scFv) odvozených od těchto protilátek není výrazně ovlivněn přítomností mutací v PR; inhibiční konstanty pro PR rezistentní k léčivům jsou 5-11 nM pro scFv1696 a 13-169 nM pro scFvF11.2.32. Kovalentně spojený dimer HIV-1 PR se ukázal jako vhodný model PR odolný k inhibici disociací nejen fragmentem 1696, ale překvapivě také F11.2.32. Tento fakt naznačuje, že disociace dimeru PR hraje roli i v inhibičním účinku F11.2.32. (cs)
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| Title
| - Potent inhibition of drug-resistant HIV protease variants by monoclonal antibodies
- Potent inhibition of drug-resistant HIV protease variants by monoclonal antibodies (en)
- Účinná inhibice k léčivům rezistentních mutantů HIV proteas (cs)
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| skos:prefLabel
| - Potent inhibition of drug-resistant HIV protease variants by monoclonal antibodies
- Potent inhibition of drug-resistant HIV protease variants by monoclonal antibodies (en)
- Účinná inhibice k léčivům rezistentních mutantů HIV proteas (cs)
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| skos:notation
| - RIV/61388963:_____/08:00306926!RIV09-MZ0-61388963
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| http://linked.open...avai/riv/aktivita
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| http://linked.open...avai/riv/aktivity
| - P(NR8571), R, Z(AV0Z40550506), Z(AV0Z50520514)
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| http://linked.open...iv/cisloPeriodika
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| http://linked.open...vai/riv/dodaniDat
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| http://linked.open...aciTvurceVysledku
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| http://linked.open.../riv/druhVysledku
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| http://linked.open...iv/duvernostUdaju
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| http://linked.open...titaPredkladatele
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| http://linked.open...dnocenehoVysledku
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| http://linked.open...ai/riv/idVysledku
| - RIV/61388963:_____/08:00306926
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| http://linked.open...riv/jazykVysledku
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| http://linked.open.../riv/klicovaSlova
| - HIV protease; drug resistance; Inhibiting antibody (en)
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| http://linked.open.../riv/klicoveSlovo
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| http://linked.open...odStatuVydavatele
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| http://linked.open...ontrolniKodProRIV
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| http://linked.open...i/riv/nazevZdroje
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| http://linked.open...in/vavai/riv/obor
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| http://linked.open...ichTvurcuVysledku
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| http://linked.open...cetTvurcuVysledku
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| http://linked.open...vavai/riv/projekt
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| http://linked.open...UplatneniVysledku
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| http://linked.open...v/svazekPeriodika
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| http://linked.open...iv/tvurceVysledku
| - Brynda, Jiří
- Fábry, Milan
- Král, Vlastimil
- Konvalinka, Jan
- Kožíšek, Milan
- Sieglová, Irena
- Řezáčová, Pavlína
- Grantz Šašková, Klára
- Sedláček, Juraj
- Hořejší, Magdalena
- Bartoňová, Vanda
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| http://linked.open...ain/vavai/riv/wos
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| http://linked.open...n/vavai/riv/zamer
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| issn
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| number of pages
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