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TitleGS-8374, a prototype phosphonate-containing inhibitor of HIV-1 protease, effectively inhibits protease mutants with amino acid insertions.
Journal, issue, pagesJ. Virol., Vol. 88, Page 3586-3590, Year 2014
Publish dateAug 14, 2013 (structure data deposition date)
AuthorsGrantz Saskova, K. / Kozisek, M. / Stray, K. / de Jong, D. / Rezaova, P. / Brynda, J. / van Maarseveen, N.M. / Nijhuis, M. / Cihlar, T. / Konvalinka, J.
External linksJ. Virol. / PubMed:24371077
MethodsX-ray diffraction
Resolution2.05 - 2.22 Å
Structure data

PDB-4m8x:
GS-8374, a Novel Phosphonate-Containing Inhibitor of HIV-1 Protease, Effectively Inhibits HIV PR Mutants with Amino Acid Insertions
Method: X-RAY DIFFRACTION / Resolution: 2.05 Å

PDB-4m8y:
GS-8374, a Novel Phosphonate-Containing Inhibitor of HIV-1 Protease, Effectively Inhibits HIV PR Mutants with Amino Acid Insertions
Method: X-RAY DIFFRACTION / Resolution: 2.22 Å

Chemicals

ChemComp-KGQ:
DIETHYL ({4-[(2S,3R)-2-({[(3R,3AS,6AR)-HEXAHYDROFURO[2,3-B]FURAN-3-YLOXY]CARBONYL}AMINO)-3-HYDROXY-4-{ISOBUTYL[(4-METHOXYPHENYL)SULFONYL]AMINO}BUTYL]PHENOXY}METHYL)PHOSPHONATE

ChemComp-HOH:
WATER

Source
  • human immunodeficiency virus 1
KeywordsHydrolase/Hydrolase Inhibitor / HIV protease / aspartic protease / GS8374 / Hydrolase-Hydrolase Inhibitor complex / HIV-1 protease / amino acid insertion

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