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== '''Darunavir: HIV-Protease Inhibitor''' == | == '''Darunavir: HIV-Protease Inhibitor''' == | ||
Darunavir (also known as TMC114) is a HIV-PR 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> | ||
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> | ||