Loss of the protease dimerization inhibition activity of tipranavir (TPV) and its association with the acquisition of resistance to TPV by HIV-1.
about
Understanding HIV-1 protease autoprocessing for novel therapeutic development.Dimerization of HIV-1 protease occurs through two steps relating to the mechanism of protease dimerization inhibition by darunavir.HIV-1 Protease Dimerization Dynamics Reveals a Transient Druggable Binding Pocket at the Interface.C-5-Modified Tetrahydropyrano-Tetrahydofuran-Derived Protease Inhibitors (PIs) Exert Potent Inhibition of the Replication of HIV-1 Variants Highly Resistant to Various PIs, including DarunavirGRL-0519, a novel oxatricyclic ligand-containing nonpeptidic HIV-1 protease inhibitor (PI), potently suppresses replication of a wide spectrum of multi-PI-resistant HIV-1 variants in vitro.A novel central nervous system-penetrating protease inhibitor overcomes human immunodeficiency virus 1 resistance with unprecedented aM to pM potency.GRL-079, a novel P2-Tp-THF-C5-alkylamine- and P2' -Abt-containing HIV-1 protease inhibitor, is extremely potent against multi-drug-resistant HIV-1 variants including HIVDRVRp51 and has a high genetic barrier against the emergence of resistant varianDesign of Highly Potent, Dual Acting and Central Nervous System Penetrating HIV-1 Protease Inhibitors with Excellent Potency against Multidrug-Resistant HIV-1 Variants.Mechanism of Darunavir (DRV)'s High Genetic Barrier to HIV-1 Resistance: A Key V32I Substitution in Protease Rarely Occurs, but Once It Occurs, It Predisposes HIV-1 To Develop DRV Resistance.Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis.
P2860
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P2860
Loss of the protease dimerization inhibition activity of tipranavir (TPV) and its association with the acquisition of resistance to TPV by HIV-1.
description
2012 nî lūn-bûn
@nan
2012年の論文
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2012年学术文章
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2012年学术文章
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2012年学术文章
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2012年学术文章
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2012年学术文章
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2012年學術文章
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name
Loss of the protease dimerizat ...... of resistance to TPV by HIV-1.
@ast
Loss of the protease dimerizat ...... of resistance to TPV by HIV-1.
@en
type
label
Loss of the protease dimerizat ...... of resistance to TPV by HIV-1.
@ast
Loss of the protease dimerizat ...... of resistance to TPV by HIV-1.
@en
prefLabel
Loss of the protease dimerizat ...... of resistance to TPV by HIV-1.
@ast
Loss of the protease dimerizat ...... of resistance to TPV by HIV-1.
@en
P2093
P2860
P356
P1433
P1476
Loss of the protease dimerizat ...... of resistance to TPV by HIV-1
@en
P2093
Debananda Das
Hiroaki Mitsuya
Hiromi Aoki-Ogata
Kazuhiko Ide
Manabu Aoki
Matthew L Danish
Yasuhiro Koh
P2860
P304
13384-13396
P356
10.1128/JVI.07234-11
P407
P577
2012-09-26T00:00:00Z