Sandbox Reserved 712: Difference between revisions
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== '''Darunavir: HIV-Protease Inhibitor''' == | == '''Darunavir: HIV-Protease Inhibitor''' == | ||
Darunavir (also known as TMC114) is a HIV-PR Inhibitor. The wild-type HIV as well as a large penal of PI-resistant recombinant viruses derived from clinical samples show high susceptibility to darunavir. <ref> PMID:15917527 </ref> | [[Darunavir]] (also known as TMC114) is a HIV-PR Inhibitor. The wild-type HIV as well as a large penal of PI-resistant recombinant viruses derived from clinical samples show high susceptibility to [[darunavir]]. <ref> PMID:15917527 </ref> | ||
One reason for the high potency of darunavir is the strong binding of the PI to the main-chains of the protease active-site amino acids. <ref> PMID:14506019 </ref> A second reason might be the ability of the PI to fit closely into the substrate envelope. <ref>PMID:15479840</ref> | One reason for the high potency of darunavir is the strong binding of the PI to the main-chains of the protease active-site amino acids. <ref> PMID:14506019 </ref> A second reason might be the ability of the PI to fit closely into the substrate envelope. <ref>PMID:15479840</ref> | ||
Darunavir shows a high genetical barrier to resistance development. In fact studies indicate that the development of resistance needs more specific mutations and develops more slowly. <ref> PMID:15917527 </ref> | [[Darunavir]] shows a high genetical barrier to resistance development. In fact studies indicate that the development of resistance needs more specific mutations and develops more slowly. <ref> PMID:15917527 </ref> | ||
Darunavir resistance-associated mutations are V11I, V32I, <scene name='Sandbox_Reserved_712/L33f/1'>L33F</scene>, I47V, I50V, I54L, I54M, G73S, L76V, <scene name='Sandbox_Reserved_712/I84v/2'>I84V</scene> and | [[Darunavir]] resistance-associated mutations are V11I, V32I, <scene name='Sandbox_Reserved_712/L33f/1'>L33F</scene>, I47V, I50V, I54L, I54M, G73S, L76V, <scene name='Sandbox_Reserved_712/I84v/2'>I84V</scene> and | ||
<scene name='Sandbox_Reserved_712/L89v/1'>L89V</scene> ([[HIV Protease Resistance]]). Those mutations occurred in patients who have a high number of PI resistance-associated mutations. <ref> PMID:17416261 </ref> | <scene name='Sandbox_Reserved_712/L89v/1'>L89V</scene> ([[HIV Protease Resistance]]). Those mutations occurred in patients who have a high number of PI resistance-associated mutations. <ref> PMID:17416261 </ref> | ||
