Sandbox Reserved 712: Difference between revisions
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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 (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 (<scene name='Sandbox_Reserved_712/Activesiteasp25/1'>Asp25</scene>, <scene name='Sandbox_Reserved_712/Activesitethr26/1'>Thr26</scene> and | HIV proteases contain a highly conserved region Asp - Thr - Gly (<scene name='Sandbox_Reserved_712/Activesiteasp25/1'>Asp25</scene>, <scene name='Sandbox_Reserved_712/Activesitethr26/1'>Thr26</scene> and | ||
<scene name='Sandbox_Reserved_712/Activesitegly27/2'>Gly27</scene>), with the aspartic residue | <scene name='Sandbox_Reserved_712/Activesitegly27/2'>Gly27</scene>), with the aspartic residue being the <scene name='Sandbox_Reserved_712/Activesite/1'>active site</scene> | ||
in the aspartyl protease.<ref> PMID:3290901 </ref> | in the aspartyl protease.<ref> PMID:3290901 </ref> | ||
Because of its importance for the life-cycle of the retrovirus, HIV- | Because of its importance for the life-cycle of the retrovirus, HIV-PRs are the major target for anti-HIV treatment. | ||
HIV protease inhibitors are the most potent | HIV protease inhibitors are the most potent agents used in anti-HIV treatment. However it appears that HIV-PRs develop a resistance to the inhibitor. <ref> PMID:12543689 </ref> | ||
3ggu (also PR<sub>DRV5</sub>) 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> | 3ggu (also PR<sub>DRV5</sub>) 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> | ||
