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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)]]
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)]]
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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)
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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. <ref> PMID:19535439 </ref>
== '''Activity''' ==
== '''Activity''' ==

Revision as of 12:50, 27 December 2012

Template:Sandbox ESBS 2012

3ggu

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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. [1]

Activity

Structure

Applications

External Resources

References

  1. ↑ 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

(1) Kohl, N. E., E. A. Emini, W. A. Schleif, L. J. Davis, J. C. Heimbach, R. A. F. Dixon, E. M. Scolnick, and I. S. Sigal. 1988. Active human immunodeficiency virus protease is required for viral infectivity. Proc. Natl. Acad. Sci. USA 85:4686-4690.

(2) Watkins T, Resch W, Irlbeck D, Swanstrom R (February 2003). "Selection of high-level resistance to human immunodeficiency virus type 1 protease inhibitors". Antimicrob. Agents Chemother. 47 (2): 759–69. doi:10.1128/AAC.47.2.759-769.2003. PMC 151730. PMID 12543689.

Contributors

Julia Baaske, Angelika Wackerl

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