4m8y

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GS-8374, a Novel Phosphonate-Containing Inhibitor of HIV-1 Protease, Effectively Inhibits HIV PR Mutants with Amino Acid Insertions

Structural highlights

4m8y is a 2 chain structure with sequence from Human immunodeficiency virus 1. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 2.22Å
Ligands:KGQ
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

Q90JJ9_9HIV1

Publication Abstract from PubMed

Insertions in the protease (PR) region of human immunodeficiency virus (HIV) represent an interesting mechanism of antiviral resistance against HIV PR inhibitors (PIs). Here, we demonstrate the improved ability of a phosphonate-containing experimental HIV PI, GS-8374, relative to that of other PIs, to effectively inhibit patient-derived recombinant HIV strains bearing PR insertions and numerous other mutations. We correlate enzyme inhibition with the catalytic activities of corresponding recombinant PRs in vitro and provide a biochemical and structural analysis of the PR-inhibitor complex.

GS-8374, a prototype phosphonate-containing inhibitor of HIV-1 protease, effectively inhibits protease mutants with amino acid insertions.,Grantz Saskova K, Kozisek M, Stray K, de Jong D, Rezaova P, Brynda J, van Maarseveen NM, Nijhuis M, Cihlar T, Konvalinka J J Virol. 2014 Mar;88(6):3586-90. doi: 10.1128/JVI.02688-13. Epub 2013 Dec 26. PMID:24371077[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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See Also

References

  1. ↑ Grantz Saskova K, Kozisek M, Stray K, de Jong D, Rezaova P, Brynda J, van Maarseveen NM, Nijhuis M, Cihlar T, Konvalinka J. GS-8374, a prototype phosphonate-containing inhibitor of HIV-1 protease, effectively inhibits protease mutants with amino acid insertions. J Virol. 2014 Mar;88(6):3586-90. doi: 10.1128/JVI.02688-13. Epub 2013 Dec 26. PMID:24371077 doi:http://dx.doi.org/10.1128/JVI.02688-13

Contents


PDB ID 4m8y

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