Small-Molecule Inhibitors of the LEDGF/p75 Binding Site of Integrase Block HIV Replication and Modulate Integrase Multimerization
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Title
Small-Molecule Inhibitors of the LEDGF/p75 Binding Site of Integrase Block HIV Replication and Modulate Integrase Multimerization
Authors
Keywords
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Journal
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
Volume 56, Issue 8, Pages 4365-4374
Publisher
American Society for Microbiology
Online
2012-06-05
DOI
10.1128/aac.00717-12
References
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Related references
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- (2012) Cristina Tintori et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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- LEDGF/p75-Independent HIV-1 Replication Demonstrates a Role for HRP-2 and Remains Sensitive to Inhibition by LEDGINs
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- Resistance associated mutations to dolutegravir (S/GSK1349572) in HIV-infected patients – Impact of HIV subtypes and prior raltegravir experience
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- Efficacy and safety of once daily elvitegravir versus twice daily raltegravir in treatment-experienced patients with HIV-1 receiving a ritonavir-boosted protease inhibitor: randomised, double-blind, phase 3, non-inferiority study
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- Elvitegravir: a once daily alternative to raltegravir
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- FRET analysis reveals distinct conformations of IN tetramers in the presence of viral DNA or LEDGF/p75
- (2011) Jacques J. Kessl et al. NUCLEIC ACIDS RESEARCH
- Lersivirine, a Nonnucleoside Reverse Transcriptase Inhibitor with Activity against Drug-Resistant Human Immunodeficiency Virus Type 1
- (2010) R. Corbau et al. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
- Activity of Elvitegravir, a Once‐Daily Integrase Inhibitor, against Resistant HIV Type 1: Results of a Phase 2, Randomized, Controlled, Dose‐Ranging Clinical Trial
- (2010) Andrew R. Zolopa et al. JOURNAL OF INFECTIOUS DISEASES
- Retroviral intasome assembly and inhibition of DNA strand transfer
- (2010) Stephen Hare et al. NATURE
- Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication
- (2010) Frauke Christ et al. Nature Chemical Biology
- HIV Capsid is a Tractable Target for Small Molecule Therapeutic Intervention
- (2010) Wade S. Blair et al. PLoS Pathogens
- An Allosteric Mechanism for Inhibiting HIV-1 Integrase with a Small Molecule
- (2009) J. J. Kessl et al. MOLECULAR PHARMACOLOGY
- Mutations Associated with Failure of Raltegravir Treatment Affect Integrase Sensitivity to the Inhibitor In Vitro
- (2008) I. Malet et al. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
- A 1,536-Well [35S]GTPγS Scintillation Proximity Binding Assay for Ultra-High-Throughput Screening of an Orphan Gαi-Coupled GPCR
- (2008) Eric N. Johnson et al. ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES
- Comparison of Raltegravir and Elvitegravir on HIV-1 Integrase Catalytic Reactions and on a Series of Drug-Resistant Integrase Mutants†
- (2008) Jessica Marinello et al. BIOCHEMISTRY
- Discovery of Raltegravir, a Potent, Selective Orally Bioavailable HIV-Integrase Inhibitor for the Treatment of HIV-AIDS Infection
- (2008) Vincenzo Summa et al. JOURNAL OF MEDICINAL CHEMISTRY
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