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== '''Activity''' ==
== '''Activity''' ==
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=== Prevalence of daruanvir resistance mutations in a large clinical database ===
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=== Phenotypic susceptibiity to PIs ===
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=== Enzymatic analysis of recombinant PRs ===
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=== X-ray strucure analysis of PRdrv1 and PRdrv5 ===
== '''Structure''' ==
== '''Structure''' ==

Revision as of 14:35, 27 December 2012

Template:Sandbox ESBS 2012

3ggu

Drag the structure with the mouse to rotate

Contents

Description

3ggu is a drug resistant HIV protease. Shown is a patient's variant in complex with darunavir.

HIV proteases (PR) are essential for the functioning of the retrovirus that causes AIDS. HIV needs active proteases to process gag & gap - polymerase polyprotein precursors into mature structural proteins and replicative enzymes. HIV proteases contain a highly conserved region Asp - Thr - Gly (Asp25, Thr26 and Gly27), with the aspartic residue beeing the active site in the aspartyl protease.[1]

Because of its importance for the life-cycle of the retrovirus, HIV-PR are the major target for anti-HIV treatment. HIV protease inhibitors are the most potent agens used in anti-HIV treatment. However it occurs that HIV-PR develop a resistance to the inhibitor. [2]

3ggu (also PRdrv5) is a mutated clinically derived PR that shows phenotypical resistance to darunavir. Darunavir is a human immunodeficiency virus (HIV) protease (PR) inhibitor (PI) which has inhibiting effects on many HIV type 1 PR variants that show resistance to earlier-generation-PIs. [3]

Activity

Prevalence of daruanvir resistance mutations in a large clinical database

Phenotypic susceptibiity to PIs

Enzymatic analysis of recombinant PRs

X-ray strucure analysis of PRdrv1 and PRdrv5

Structure

Applications

External Resources

References

  1. ↑ Kohl NE, Emini EA, Schleif WA, Davis LJ, Heimbach JC, Dixon RA, Scolnick EM, Sigal IS. Active human immunodeficiency virus protease is required for viral infectivity. Proc Natl Acad Sci U S A. 1988 Jul;85(13):4686-90. PMID:3290901
  2. ↑ Watkins T, Resch W, Irlbeck D, Swanstrom R. Selection of high-level resistance to human immunodeficiency virus type 1 protease inhibitors. Antimicrob Agents Chemother. 2003 Feb;47(2):759-69. PMID:12543689
  3. ↑ Saskova KG, Kozisek M, Rezacova P, Brynda J, Yashina T, Kagan RM, Konvalinka J. Molecular characterization of clinical isolates of human immunodeficiency virus resistant to the protease inhibitor darunavir. J Virol. 2009 Sep;83(17):8810-8. Epub 2009 Jun 17. PMID:19535439 doi:10.1128/JVI.00451-09

Contributors

Julia Baaske, Angelika Wackerl

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