Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
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Retroviral intasome assembly and inhibition of DNA strand transferIntegrase Inhibitor Prodrugs: Approaches to Enhancing the Anti-HIV Activity of β-Diketo AcidsComputational methods in drug discoveryExploring the role of receptor flexibility in structure-based drug discoveryAllosteric Inhibition of Human Immunodeficiency Virus IntegraseFunctional and structural characterization of the integrase from the prototype foamy virusCrystal structure of the HIV-1 integrase core domain in complex with sucrose reveals details of an allosteric inhibitory binding siteStructure and inhibition of herpesvirus DNA packaging terminase nuclease domainMolecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance.Fragment-based design of ligands targeting a novel site on the integrase enzyme of human immunodeficiency virus 1Structural and Binding Analysis of Pyrimidinol Carboxylic Acid and N-Hydroxy Quinazolinedione HIV-1 RNase H InhibitorsStructural and Functional Analyses of the Second-Generation Integrase Strand Transfer Inhibitor Dolutegravir (S/GSK1349572)Small Molecule Inhibitors of the LEDGF Site of Human Immunodeficiency Virus Integrase Identified by Fragment Screening and Structure Based DesignStructural and Biochemical Basis for Development of Influenza Virus Inhibitors Targeting the PA EndonucleaseStructural Analysis of Specific Metal Chelating Inhibitor Binding to the Endonuclease Domain of Influenza pH1N1 (2009) PolymeraseAssembly of prototype foamy virus strand transfer complexes on product DNA bypassing catalysis of integrationActivities, Crystal Structures, and Molecular Dynamics of Dihydro-1 H -isoindole Derivatives, Inhibitors of HIV-1 IntegraseAllosteric integrase inhibitor potency is determined through the inhibition of HIV-1 particle maturation3′-Processing and strand transfer catalysed by retroviral integrasein crystalloParallel screening of low molecular weight fragment libraries: do differences in methodology affect hit identification?Long-term efficacy and safety of raltegravir in the management of HIV infection.A New Class of Allosteric HIV-1 Integrase Inhibitors Identified by Crystallographic Fragment Screening of the Catalytic Core DomainAn overview of the synthetic routes to the best selling drugs containing 6-membered heterocyclesSubstrate recognition and motion mode analyses of PFV integrase in complex with viral DNA via coarse-grained modelsResistance mutations outside the integrase coding region have an effect on human immunodeficiency virus replicative fitness but do not affect its susceptibility to integrase strand transfer inhibitorsMolecular features related to HIV integrase inhibition obtained from structure- and ligand-based approachesContribution of human immunodeficiency virus type 1 minority variants to reduced drug susceptibility in patients on an integrase strand transfer inhibitor-based therapyTherapy-Emergent Drug Resistance to Integrase Strand Transfer Inhibitors in HIV-1 Patients: A Subgroup Meta-Analysis of Clinical TrialsRetroviral DNA IntegrationMolecular dynamics simulations: from structure function relationships to drug discovery.Computational methods in drug discovery.Combinatorial approaches to the prevention and treatment of HIV-1 infectionA novel anti-HIV active integrase inhibitor with a favorable in vitro cytochrome P450 and uridine 5'-diphospho-glucuronosyltransferase metabolism profile.Identification of influenza endonuclease inhibitors using a novel fluorescence polarization assay.Molecular modeling study on the allosteric inhibition mechanism of HIV-1 integrase by LEDGF/p75 binding site inhibitors.An allosteric mechanism for inhibiting HIV-1 integrase with a small molecule.4-Substituted 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as a Novel Class of HIV-1 Integrase InhibitorsMicronucleated erythrocytes in newborn rats exposed to raltegravir placental transfer.A dynamic model of HIV integrase inhibition and drug resistance.Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
P2860
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P2860
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
description
2008 nî lūn-bûn
@nan
2008年の論文
@ja
2008年学术文章
@wuu
2008年学术文章
@zh
2008年学术文章
@zh-cn
2008年学术文章
@zh-hans
2008年学术文章
@zh-my
2008年学术文章
@zh-sg
2008年學術文章
@yue
2008年學術文章
@zh-hant
name
Discovery of raltegravir, a po ...... eatment of HIV-AIDS infection.
@en
Discovery of raltegravir, a po ...... eatment of HIV-AIDS infection.
@nl
type
label
Discovery of raltegravir, a po ...... eatment of HIV-AIDS infection.
@en
Discovery of raltegravir, a po ...... eatment of HIV-AIDS infection.
@nl
prefLabel
Discovery of raltegravir, a po ...... eatment of HIV-AIDS infection.
@en
Discovery of raltegravir, a po ...... eatment of HIV-AIDS infection.
@nl
P2093
P356
P1476
Discovery of raltegravir, a po ...... eatment of HIV-AIDS infection.
@en
P2093
Alessia Petrocchi
Benedetta Crescenzi
Cristina Gardelli
Daria J Hazuda
Edith Monteagudo
Emanuela Nizi
Ester Muraglia
Fabio Bonelli
Fabrizio Fiore
Federica Orvieto
P304
P356
10.1021/JM800245Z
P407
P577
2008-09-01T00:00:00Z