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| rdf:type
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| Description
| - The X-ray structure of a complex of HIV-1 protease (PR) with a phenylnorstatine inhibitor Z-Pns-Phe-Glu-Glu-NH(2) has been determined at 1.03 A, the highest resolution so far reported for any HIV PR complex. The inhibitor shows subnanomolar K(i) values for both the wild-type PR and the variant representing one of the most common mutations linked to resistance development. The structure comprising the phenylnorstatine moiety of (2R,3S)-chirality displays a unique pattern of hydrogen bonding to the two catalytic aspartate residues. This high resolution makes it possible to assess the donor and acceptor relations of this hydrogen bonding and to indicate a proton shared by the two catalytic residues. A structural mechanism for the unimpaired inhibition of the protease Val82Ala mutant is also suggested, based on energy calculations and analyses
- The X-ray structure of a complex of HIV-1 protease (PR) with a phenylnorstatine inhibitor Z-Pns-Phe-Glu-Glu-NH(2) has been determined at 1.03 A, the highest resolution so far reported for any HIV PR complex. The inhibitor shows subnanomolar K(i) values for both the wild-type PR and the variant representing one of the most common mutations linked to resistance development. The structure comprising the phenylnorstatine moiety of (2R,3S)-chirality displays a unique pattern of hydrogen bonding to the two catalytic aspartate residues. This high resolution makes it possible to assess the donor and acceptor relations of this hydrogen bonding and to indicate a proton shared by the two catalytic residues. A structural mechanism for the unimpaired inhibition of the protease Val82Ala mutant is also suggested, based on energy calculations and analyses (en)
- Byla určena rentgenová struktura komplexu proteázy HIV-1 (PR) s fenylnorstatinovým inhibitorem Z-Pns-Phe-Glu-Glu-NH(2) při rozlišení 1,03 A, nejvyšším rozlišení, které bylo doposud uvedeno pro kterýkoli komplex HIV PR. Tento inhibitor vykazuje subnanomolární hodnoty K(i) jak pro PR divokého typu, tak pro variantu představující jednu z nejběžnějších mutací spojenou s vývojem rezistence. Struktura obsahující fenylnorstatinovou část chirality (2R,3S) vykazuje jedinečný obraz vazby vodíkových můstků na dva katalytické aspartátové zbytky. Toto vysoké rozlišení umožňuje zjistit donorové a akceptorové vztahy těchto vodíkových můstků a určit proton sdílený oběma katalytickými zbytky. Je také navržen strukturální mechanismus nenarušené inhibice mutanty proteázy Val82Ala založený na energetických výpočtech a analýzách (cs)
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| Title
| - A Phenylnorstatine Inhibitor Binding to HIV-1 Protease: Geometry, Protonation, and Subsite-Pocket Interactions Analyzed at Atomic Resolution
- A Phenylnorstatine Inhibitor Binding to HIV-1 Protease: Geometry, Protonation, and Subsite-Pocket Interactions Analyzed at Atomic Resolution (en)
- Vazba fenylnorstatinového inhibitoru na proteázu HIV-1: geometrie, protonace a interakce kapes podřadných míst analyzované při atomovém rozlišení (cs)
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| skos:prefLabel
| - A Phenylnorstatine Inhibitor Binding to HIV-1 Protease: Geometry, Protonation, and Subsite-Pocket Interactions Analyzed at Atomic Resolution
- A Phenylnorstatine Inhibitor Binding to HIV-1 Protease: Geometry, Protonation, and Subsite-Pocket Interactions Analyzed at Atomic Resolution (en)
- Vazba fenylnorstatinového inhibitoru na proteázu HIV-1: geometrie, protonace a interakce kapes podřadných míst analyzované při atomovém rozlišení (cs)
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| skos:notation
| - RIV/68378050:_____/04:00105275!RIV/2005/AV0/A23005/N
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| http://linked.open.../vavai/riv/strany
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| http://linked.open...avai/riv/aktivita
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| http://linked.open...avai/riv/aktivity
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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/68378050:_____/04:00105275
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| http://linked.open...riv/jazykVysledku
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| http://linked.open.../riv/klicovaSlova
| - inhibitor; HIV protease; atomic resolution (en)
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| http://linked.open.../riv/klicoveSlovo
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| http://linked.open...odStatuVydavatele
| - US - Spojené státy americké
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| http://linked.open...ontrolniKodProRIV
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| http://linked.open...i/riv/nazevZdroje
| - Journal of Medicinal Chemistry
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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...UplatneniVysledku
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| http://linked.open...v/svazekPeriodika
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| http://linked.open...iv/tvurceVysledku
| - Brynda, Jiří
- Fábry, Milan
- Konvalinka, Jan
- Lepšík, Martin
- Řezáčová, Pavlína
- Souček, Milan
- Sedláček, Juraj
- Hořejší, Magdalena
- Hradílek, Martin
- Štouračová, Renata
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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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