Published in J Virol on September 05, 2007
Dose-response curve slope sets class-specific limits on inhibitory potential of anti-HIV drugs. Nat Med (2008) 3.28
Structure-based modeling of the functional HIV-1 intasome and its inhibition. Proc Natl Acad Sci U S A (2010) 2.16
Functional and structural characterization of the integrase from the prototype foamy virus. Nucleic Acids Res (2008) 2.07
Identification of nevirapine-resistant HIV-1 in the latent reservoir after single-dose nevirapine to prevent mother-to-child transmission of HIV-1. J Infect Dis (2009) 1.93
Structural biology of retroviral DNA integration. Virology (2011) 1.37
Molecular Interactions between HIV-1 integrase and the two viral DNA ends within the synaptic complex that mediates concerted integration. J Mol Biol (2009) 1.19
Nucleoprotein intermediates in HIV-1 DNA integration visualized by atomic force microscopy. J Mol Biol (2010) 1.14
A critical subset model provides a conceptual basis for the high antiviral activity of major HIV drugs. Sci Transl Med (2011) 1.11
Nucleoprotein complex intermediates in HIV-1 integration. Methods (2009) 1.03
Physical trapping of HIV-1 synaptic complex by different structural classes of integrase strand transfer inhibitors. Biochemistry (2010) 0.96
The HIV-1 integrase monomer induces a specific interaction with LTR DNA for concerted integration. Biochemistry (2011) 0.95
Mechanisms of human immunodeficiency virus type 1 concerted integration related to strand transfer inhibition and drug resistance. Antimicrob Agents Chemother (2008) 0.94
Inhibiting the HIV integration process: past, present, and the future. J Med Chem (2013) 0.93
HIV-1 Integrase Strand Transfer Inhibitors: Novel Insights into their Mechanism of Action. Retrovirology (Auckl) (2008) 0.86
Biochemical and biophysical analyses of concerted (U5/U3) integration. Methods (2008) 0.83
A protein ballet around the viral genome orchestrated by HIV-1 reverse transcriptase leads to an architectural switch: from nucleocapsid-condensed RNA to Vpr-bridged DNA. Virus Res (2012) 0.83
HIV-1 integrase strand transfer inhibitors stabilize an integrase-single blunt-ended DNA complex. J Mol Biol (2011) 0.80
Raltegravir in HIV-1 infection: Safety and Efficacy in Treatment-naïve Patients. Clin Med Rev Ther (2011) 0.80
Rous sarcoma virus synaptic complex capable of concerted integration is kinetically trapped by human immunodeficiency virus integrase strand transfer inhibitors. J Biol Chem (2014) 0.78
Prospective strategies for targeting HIV-1 integrase function. Future Med Chem (2010) 0.78
Critical appraisal of elvitegravir in the treatment of HIV-1/AIDS. HIV AIDS (Auckl) (2014) 0.77
Retroviral integrase protein and intasome nucleoprotein complex structures. World J Biol Chem (2017) 0.75
Mechanistic and pharmacological analyses of HIV-1 integration. Methods (2009) 0.75
Decline in the AIDS and death rates in the EuroSIDA study: an observational study. Lancet (2003) 7.94
Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells. Science (2000) 7.01
Residues critical for retroviral integrative recombination in a region that is highly conserved among retroviral/retrotransposon integrases and bacterial insertion sequence transposases. Mol Cell Biol (1992) 6.77
Human immunodeficiency virus type 1 preintegration complexes: studies of organization and composition. J Virol (1997) 5.73
Antiretroviral activity, pharmacokinetics, and tolerability of MK-0518, a novel inhibitor of HIV-1 integrase, dosed as monotherapy for 10 days in treatment-naive HIV-1-infected individuals. J Acquir Immune Defic Syndr (2006) 4.71
Integrase inhibitors to treat HIV/AIDS. Nat Rev Drug Discov (2005) 4.46
Domains of the integrase protein of human immunodeficiency virus type 1 responsible for polynucleotidyl transfer and zinc binding. Proc Natl Acad Sci U S A (1993) 3.99
Retroviral DNA integration: reaction pathway and critical intermediates. EMBO J (2006) 3.68
Diketo acid inhibitor mechanism and HIV-1 integrase: implications for metal binding in the active site of phosphotransferase enzymes. Proc Natl Acad Sci U S A (2002) 3.40
HIV-1 integrase inhibitors that compete with the target DNA substrate define a unique strand transfer conformation for integrase. Proc Natl Acad Sci U S A (2000) 3.00
Sequence specificity of viral end DNA binding by HIV-1 integrase reveals critical regions for protein-DNA interaction. EMBO J (1998) 2.84
Structure of the HIV-1 integrase catalytic domain complexed with an inhibitor: a platform for antiviral drug design. Proc Natl Acad Sci U S A (1999) 2.69
A soluble active mutant of HIV-1 integrase: involvement of both the core and carboxyl-terminal domains in multimerization. J Biol Chem (1996) 2.58
A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase. Proc Natl Acad Sci U S A (2004) 2.55
Zinc folds the N-terminal domain of HIV-1 integrase, promotes multimerization, and enhances catalytic activity. Proc Natl Acad Sci U S A (1996) 2.46
Integrase inhibitors and cellular immunity suppress retroviral replication in rhesus macaques. Science (2004) 2.12
Processing of viral DNA ends channels the HIV-1 integration reaction to concerted integration. J Biol Chem (2005) 1.84
Multiple integrase functions are required to form the native structure of the human immunodeficiency virus type I intasome. J Biol Chem (1999) 1.77
Structure-based mutagenesis of the human immunodeficiency virus type 1 DNA attachment site: effects on integration and cDNA synthesis. J Virol (1999) 1.64
Efficient concerted integration by recombinant human immunodeficiency virus type 1 integrase without cellular or viral cofactors. J Virol (2002) 1.56
Asymmetric processing of human immunodeficiency virus type 1 cDNA in vivo: implications for functional end coupling during the chemical steps of DNA transposition. Mol Cell Biol (2001) 1.49
Central core domain of retroviral integrase is responsible for target site selection. J Biol Chem (1997) 1.48
Multimerization determinants reside in both the catalytic core and C terminus of avian sarcoma virus integrase. J Biol Chem (1995) 1.35
Structural determinants for HIV-1 integrase inhibition by beta-diketo acids. J Biol Chem (2002) 1.26
Comparison of DNA binding and integration half-site selection by avian myeloblastosis virus integrase. J Virol (1993) 1.26
Metal-dependent inhibition of HIV-1 integrase by beta-diketo acids and resistance of the soluble double-mutant (F185K/C280S). Mol Pharmacol (2003) 1.22
Activity of recombinant HIV-1 integrase on mini-HIV DNA. Nucleic Acids Res (1999) 1.22
Transcriptional coactivator LEDGF/p75 modulates human immunodeficiency virus type 1 integrase-mediated concerted integration. J Virol (2007) 1.21
An amino acid in the central catalytic domain of three retroviral integrases that affects target site selection in nonviral DNA. J Virol (2003) 1.16
In vitro human immunodeficiency virus type 1 integrase assays. Methods Enzymol (2001) 1.15
DNase protection analysis of retrovirus integrase at the viral DNA ends for full-site integration in vitro. J Virol (2001) 1.13
Role of the nonspecific DNA-binding region and alpha helices within the core domain of retroviral integrase in selecting target DNA sites for integration. J Biol Chem (2001) 1.12
HIV-1 integrase inhibitors: a decade of research and two drugs in clinical trial. Curr Top Med Chem (2004) 1.10
Structural determinants of metal-induced conformational changes in HIV-1 integrase. J Biol Chem (1998) 1.08
Molecular and genetic determinants of rous sarcoma virus integrase for concerted DNA integration. J Virol (2003) 0.96
Structural organization of avian retrovirus integrase in assembled intasomes mediating full-site integration. J Biol Chem (2004) 0.93
Synaptic complex formation of two retrovirus DNA attachment sites by integrase: a fluorescence energy transfer study. Biochemistry (2005) 0.93
Analysis of conserved and non-conserved amino acids critical for ALSV (Avian leukemia and sarcoma viruses) integrase functions in vitro. Arch Virol (2002) 0.91
HIV-1 integrase: a target for new AIDS chemotherapeutics. Curr Top Med Chem (2004) 0.91
Characterization of a replication-defective human immunodeficiency virus type 1 att site mutant that is blocked after the 3' processing step of retroviral integration. J Virol (2000) 0.90
The challenge of finding a cure for HIV infection. Science (2009) 8.41
Expression of latent HIV induced by the potent HDAC inhibitor suberoylanilide hydroxamic acid. AIDS Res Hum Retroviruses (2009) 4.32
Diketo acid inhibitor mechanism and HIV-1 integrase: implications for metal binding in the active site of phosphotransferase enzymes. Proc Natl Acad Sci U S A (2002) 3.40
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection. J Med Chem (2008) 3.09
Raltegravir once daily or twice daily in previously untreated patients with HIV-1: a randomised, active-controlled, phase 3 non-inferiority trial. Lancet Infect Dis (2011) 2.66
Loss of raltegravir susceptibility by human immunodeficiency virus type 1 is conferred via multiple nonoverlapping genetic pathways. J Virol (2009) 2.19
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. Antimicrob Agents Chemother (2009) 1.80
Efficient concerted integration by recombinant human immunodeficiency virus type 1 integrase without cellular or viral cofactors. J Virol (2002) 1.56
Presenilin-1 and presenilin-2 exhibit distinct yet overlapping gamma-secretase activities. J Biol Chem (2003) 1.54
LRRTM3 promotes processing of amyloid-precursor protein by BACE1 and is a positional candidate gene for late-onset Alzheimer's disease. Proc Natl Acad Sci U S A (2006) 1.50
Natural polymorphisms of human immunodeficiency virus type 1 integrase and inherent susceptibilities to a panel of integrase inhibitors. Antimicrob Agents Chemother (2009) 1.27
Robust antiviral efficacy upon administration of a nucleoside analog to hepatitis C virus-infected chimpanzees. Antimicrob Agents Chemother (2008) 1.26
Transcriptional coactivator LEDGF/p75 modulates human immunodeficiency virus type 1 integrase-mediated concerted integration. J Virol (2007) 1.21
Molecular Interactions between HIV-1 integrase and the two viral DNA ends within the synaptic complex that mediates concerted integration. J Mol Biol (2009) 1.19
First demonstration of cerebrospinal fluid and plasma A beta lowering with oral administration of a beta-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates. J Pharmacol Exp Ther (2008) 1.16
A novel structure of DNA repair protein RecO from Deinococcus radiodurans. Structure (2004) 1.10
Postexposure protection of macaques from vaginal SHIV infection by topical integrase inhibitors. Sci Transl Med (2014) 1.03
Sustained viral response in a hepatitis C virus-infected chimpanzee via a combination of direct-acting antiviral agents. Antimicrob Agents Chemother (2010) 0.98
Molecular and genetic determinants of rous sarcoma virus integrase for concerted DNA integration. J Virol (2003) 0.96
Physical trapping of HIV-1 synaptic complex by different structural classes of integrase strand transfer inhibitors. Biochemistry (2010) 0.96
Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: effects of fused heterocycles on antiviral activity and pharmacokinetic properties. Bioorg Med Chem Lett (2005) 0.95
The HIV-1 integrase monomer induces a specific interaction with LTR DNA for concerted integration. Biochemistry (2011) 0.95
Mechanisms of human immunodeficiency virus type 1 concerted integration related to strand transfer inhibition and drug resistance. Antimicrob Agents Chemother (2008) 0.94
Structural organization of avian retrovirus integrase in assembled intasomes mediating full-site integration. J Biol Chem (2004) 0.93
Synaptic complex formation of two retrovirus DNA attachment sites by integrase: a fluorescence energy transfer study. Biochemistry (2005) 0.93
Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors. J Med Chem (2007) 0.91
Macrocyclic inhibitors of beta-secretase: functional activity in an animal model. J Med Chem (2006) 0.90
siRNA screening of a targeted library of DNA repair factors in HIV infection reveals a role for base excision repair in HIV integration. PLoS One (2011) 0.90
Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones. J Med Chem (2007) 0.88
A genome wide analysis of ubiquitin ligases in APP processing identifies a novel regulator of BACE1 mRNA levels. Mol Cell Neurosci (2006) 0.88
The base excision repair pathway is required for efficient lentivirus integration. PLoS One (2011) 0.86
BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres. Bioorg Med Chem Lett (2006) 0.86
Synthesis and evaluation of CCR5 antagonists containing modified 4-piperidinyl-2-phenyl-1-(phenylsulfonylamino)-butane. Bioorg Med Chem Lett (2005) 0.86
HIV-1 Integrase Strand Transfer Inhibitors: Novel Insights into their Mechanism of Action. Retrovirology (Auckl) (2008) 0.86
Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase. J Med Chem (2008) 0.85
Human immunodeficiency virus type 1 (HIV-1) integration: a potential target for microbicides to prevent cell-free or cell-associated HIV-1 infection. Antimicrob Agents Chemother (2008) 0.85
Rational design and synthesis of selective BACE-1 inhibitors. Bioorg Med Chem Lett (2004) 0.85
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 1: Discovery and SAR study of 4-pyrazolylpiperidine side chains. Bioorg Med Chem Lett (2004) 0.84
Biochemical and biophysical analyses of concerted (U5/U3) integration. Methods (2008) 0.83
A possible role for the asymmetric C-terminal domain dimer of Rous sarcoma virus integrase in viral DNA binding. PLoS One (2013) 0.82
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 2: Discovery of potent, selective, and orally bioavailable compounds. Bioorg Med Chem Lett (2004) 0.81
1,3,4 Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains. Bioorg Med Chem Lett (2003) 0.81
HIV-1 integrase strand transfer inhibitors stabilize an integrase-single blunt-ended DNA complex. J Mol Biol (2011) 0.80
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment. Bioorg Med Chem Lett (2004) 0.78
A presenilin-independent aspartyl protease prefers the gamma-42 site cleavage. J Neurochem (2005) 0.77
Avian retrovirus integrase-enhanced transgene integration into mammalian cell DNA in vivo. Biotechniques (2003) 0.77
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains. Bioorg Med Chem Lett (2003) 0.77
Innovation and greater probability of success in drug discovery and development -- from target to biomarkers. Curr Opin Biotechnol (2005) 0.75
Exploring possibilities. Posit Aware (2014) 0.75
Syntheses and biological evaluation of 5-(piperidin-1-yl)-3-phenyl-pentylsulfones as CCR5 antagonists. Bioorg Med Chem Lett (2004) 0.75
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV. Bioorg Med Chem Lett (2002) 0.75
CCR5 antagonists: 3-(pyrrolidin-1-yl)propionic acid analogues with potent anti-HIV activity. Org Lett (2003) 0.75
Next generation therapeutics. Curr Opin Chem Biol (2013) 0.75
Syntheses and SAR studies of 4-(heteroarylpiperdin-1-yl-methyl)-pyrrolidin-1-yl-acetic acid antagonists of the human CCR5 chemokine receptor. Bioorg Med Chem Lett (2004) 0.75
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: polar functionality and its effect on anti-HIV-1 activity. Bioorg Med Chem Lett (2002) 0.75
CCR5 antagonists: bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines. Bioorg Med Chem Lett (2002) 0.75