Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro.
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Spirodiketopiperazine-based CCR5 inhibitor which preserves CC-chemokine/CCR5 interactions and exerts potent activity against R5 human immunodeficiency virus type 1 in vitroEASY-HIT: HIV full-replication technology for broad discovery of multiple classes of HIV inhibitorsDarunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIVUnique Flap Conformation in an HIV-1 Protease with High-Level Darunavir Resistance.Design and Synthesis of HIV-1 Protease Inhibitors Incorporating Oxazolidinones as P2/P2‘ Ligands in Pseudosymmetric Dipeptide IsosteresEffect of Flap Mutations on Structure of HIV-1 Protease and Inhibition by Saquinavir and DarunavirFlexible Cyclic Ethers/Polyethers as Novel P2-Ligands for HIV-1 Protease Inhibitors: Design, Synthesis, Biological Evaluation, and Protein−Ligand X-ray Studies †Structural Evidence for Effectiveness of Darunavir and Two Related Antiviral Inhibitors against HIV-2 ProteasePotent HIV-1 protease inhibitors incorporating meso-bicyclic urethanes as P2-ligands: structure-based design, synthesis, biological evaluation and protein–ligand X-ray studiesDesign of HIV-1 Protease Inhibitors with Pyrrolidinones and Oxazolidinones as Novel P1′-Ligands To Enhance Backbone-Binding Interactions with Protease: Synthesis, Biological Evaluation, and Protein−Ligand X-ray Studies ∞Molecular Characterization of Clinical Isolates of Human Immunodeficiency Virus Resistant to the Protease Inhibitor DarunavirDesign, Synthesis, Protein−Ligand X-ray Structure, and Biological Evaluation of a Series of Novel Macrocyclic Human Immunodeficiency Virus-1 Protease Inhibitors to Combat Drug ResistanceHighly conserved glycine 86 and arginine 87 residues contribute differently to the structure and activity of the mature HIV-1 proteaseEvaluating the Substrate-Envelope Hypothesis: Structural Analysis of Novel HIV-1 Protease Inhibitors Designed To Be Robust against Drug ResistanceAmprenavir complexes with HIV-1 protease and its drug-resistant mutants altering hydrophobic clustersAutocatalytic maturation, physical/chemical properties, and crystal structure of group N HIV-1 protease: Relevance to drug resistanceProbing Multidrug-Resistance and Protein-Ligand Interactions with Oxatricyclic Designed Ligands in HIV-1 Protease InhibitorsStructure-Based Design, Synthesis, and Structure−Activity Relationship Studies of HIV-1 Protease Inhibitors Incorporating PhenyloxazolidinonesStructural basis for drug and substrate specificity exhibited by FIV encoding a chimeric FIV/HIV proteaseDesign of HIV-1 Protease Inhibitors with C3-Substituted Hexahydrocyclopentafuranyl Urethanes as P2-Ligands: Synthesis, Biological Evaluation, and Protein–Ligand X-ray Crystal StructureSubstituent effects on P2-cyclopentyltetrahydrofuranyl urethanes: Design, synthesis, and X-ray studies of potent HIV-1 protease inhibitorsPotent Antiviral HIV-1 Protease Inhibitor GRL-02031 Adapts to the Structures of Drug Resistant Mutants with Its P1′-Pyrrolidinone RingP2' Benzene Carboxylic Acid Moiety Is Associated with Decrease in Cellular Uptake: Evaluation of Novel Nonpeptidic HIV-1 Protease Inhibitors Containing P2 bis-Tetrahydrofuran MoietyHighly Potent HIV-1 Protease Inhibitors with Novel Tricyclic P2 Ligands: Design, Synthesis, and Protein–Ligand X-ray StudiesDesign, Synthesis, and Biological and Structural Evaluations of Novel HIV-1 Protease Inhibitors To Combat Drug ResistanceStructures of Darunavir-Resistant HIV-1 Protease Mutant Reveal Atypical Binding of Darunavir to Wide Open FlapsA Conserved Hydrogen-Bonding Network of P2 bis-Tetrahydrofuran-Containing HIV-1 Protease Inhibitors (PIs) with a Protease Active-Site Amino Acid Backbone Aids in Their Activity against PI-Resistant HIVStructural Basis of Why Nelfinavir-Resistant D30N Mutant of HIV-1 Protease Remains Susceptible to SaquinavirProbing Lipophilic Adamantyl Group as the P1-Ligand for HIV-1 Protease Inhibitors: Design, Synthesis, Protein X-ray Structural Studies, and Biological EvaluationA Modified P1 Moiety Enhances in vitro Antiviral Activity against Various Multi-Drug-Resistant HIV-1 Variants and in vitro CNS Penetration Properties of a Novel Nonpeptidic Protease Inhibitor, GRL-10413A Functional Interplay between Human Immunodeficiency Virus Type 1 Protease Residues 77 and 93 Involved in Differential Regulation of Precursor Autoprocessing and Mature Protease ActivityStructural Studies of a Rationally Selected Multi-Drug Resistant HIV-1 Protease Reveal Synergistic Effect of Distal Mutations on Flap DynamicsPotent anti-R5 human immunodeficiency virus type 1 effects of a CCR5 antagonist, AK602/ONO4128/GW873140, in a novel human peripheral blood mononuclear cell nonobese diabetic-SCID, interleukin-2 receptor gamma-chain-knocked-out AIDS mouse model.Prediction of potency of protease inhibitors using free energy simulations with polarizable quantum mechanics-based ligand charges and a hybrid water model.Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease.Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.Design and synthesis of potent macrocyclic HIV-1 protease inhibitors involving P1-P2 ligands.A multifaceted analysis of HIV-1 protease multidrug resistance phenotypesEfficacy and safety of darunavir (Prezista(®)) with low-dose ritonavir and other antiretroviral medications in subtype F HIV-1 infected, treatment-experienced subjects in Romania: a post-authorization, open-label, one-cohort, non-interventional, proIn vitro selection of highly darunavir-resistant and replication-competent HIV-1 variants by using a mixture of clinical HIV-1 isolates resistant to multiple conventional protease inhibitors.
P2860
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P2860
Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro.
description
2003 nî lūn-bûn
@nan
2003年の論文
@ja
2003年論文
@yue
2003年論文
@zh-hant
2003年論文
@zh-hk
2003年論文
@zh-mo
2003年論文
@zh-tw
2003年论文
@wuu
2003年论文
@zh
2003年论文
@zh-cn
name
Novel bis-tetrahydrofuranylure ...... munodeficiency virus in vitro.
@ast
Novel bis-tetrahydrofuranylure ...... munodeficiency virus in vitro.
@en
type
label
Novel bis-tetrahydrofuranylure ...... munodeficiency virus in vitro.
@ast
Novel bis-tetrahydrofuranylure ...... munodeficiency virus in vitro.
@en
prefLabel
Novel bis-tetrahydrofuranylure ...... munodeficiency virus in vitro.
@ast
Novel bis-tetrahydrofuranylure ...... munodeficiency virus in vitro.
@en
P2093
P2860
P1476
Novel bis-tetrahydrofuranylure ...... mmunodeficiency virus in vitro
@en
P2093
Arun K Ghosh
Geoffrey Bilcer
Hiroaki Mitsuya
Hiromi Ogata
Hirotomo Nakata
Irene T Weber
John F Kincaid
Laquasha Gaddis
Patra Volarath
Peter Boross
P2860
P304
P356
10.1128/AAC.47.10.3123-3129.2003
P407
P50
P577
2003-10-01T00:00:00Z