Sandbox Reserved 712: Difference between revisions
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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. <ref> PMID:12543689 </ref> | 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. <ref> PMID:12543689 </ref> | ||
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> | 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 name="Molecular"> PMID:19535439 </ref> | ||
== '''Activity''' == | == '''Activity''' == | ||
=== Prevalence of daruanvir resistance mutations in a large clinical database === | === Prevalence of daruanvir resistance mutations in a large clinical database === | ||
=== Phenotypic susceptibiity to PIs === | === Phenotypic susceptibiity to PIs === | ||
=== Enzymatic analysis of recombinant PRs === | === Enzymatic analysis of recombinant PRs === | ||
Samples PRdrv1 to PRdrv6 have been cloned and expressed in ''E. coli''. Then they were purified anch characterized in vitro by monitoring cleavage of a chromogenic peptide substrate in the presence and absence of specific PIs. <ref | |||
Samples PRdrv1 to PRdrv6 have been cloned and expressed in ''E. coli''. Then they were purified anch characterized in vitro by monitoring cleavage of a chromogenic peptide substrate in the presence and absence of specific PIs. <ref name="Molecular" /> | |||
=== X-ray strucure analysis of PRdrv1 and PRdrv5 === | === X-ray strucure analysis of PRdrv1 and PRdrv5 === | ||
== '''Structure''' == | == '''Structure''' == | ||
