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HIV Integrase (0):
Recent article
HIV Integrase
Abstract
We present a simple method, ARTSY, for extracting ¹J(NH) couplings and ¹H-¹⁵N RDCs from an interleaved set of two-dimensional ¹H-¹⁵N TROSY-HSQC spectra, based on the principle of quantitative J correlation. The primary advantage of the ARTSY method over other methods is the ability to measu...
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PMID: 20694505
PDF is available here.
PDF is available here.
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Abstract
Our best QSAR model reveals the polarizability, mass as the most influencing atomic properties in the structures of the carboxylic acid derivatives.
Crown Copyright 2010. Published by Elsevier Masson SAS. All rights reserved....
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PMID: 20561721
PDF is available here.
PDF is available here.
International Immunology (22)8 2010
Abstract
We present evidence showing that 22 of 24 (91.7%) IgMs purified from the sera of HIV-infected patients specifically hydrolyze only HIV IN but not many other tested proteins. Usually, proteolytic antibodies of AI patients are serine protease-like or metal dependent. Only 30% of IN-hydrolyzing IgMs we...
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PMID: 20507874
PDF is available here.
PDF is available here.
Chemmedchem (5)7 2010
Abstract
The tautomerism and corresponding transition states of four authentic HIV-1 integrase (IN) inhibitor prototype structures, alpha,gamma-diketo acid, alpha,gamma-diketotriazole, dihydroxypyrimidine carboxamide and 4-quinolone-3-carboxylic acid, were investigated at the B3LYP/6-311++G(d...
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PMID: 20533499
PDF is available here.
PDF is available here.
Neurochemical Research (35)6 2010
Abstract
We applied spectroscopy (circular dichroism, fluorescence) in a simplified model consisting in a peptide analogue (K156) of alpha4 helix involved in recognition of viral and cell DNA; an oligonucleotide corresponding to the U5' LTR DNA end; and an inhibitor (TB11) of the diketo acid (DKA) family. Re...
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PMID: 19937113
PDF is available here.
PDF is available here.
Nucleic Acids Research (38)11 2010
Abstract
We characterized the structural determinants of the 3'-processing reaction specificity--the first reaction of the integration process--at the DNA-binding level. We found that the integrase N-terminal domain, containing a pseudo zinc-finger motif, plays a key role, at least indirectly, in the formati...
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PMID: 20164093
PDF is available here.
PDF is available here.
Human Gene Therapy (21)5 2010
Abstract
We therefore developed a direct integrase fusion protein strategy as an alternative way to package heterologous proteins into vectors. The method was tested by creating two different integrase fusion proteins, IN-p53 and IN-mCherry, cloned into the 3' end of pol in the packaging plasmid. Lentiviral...
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PMID: 20039782
PDF is available here.
PDF is available here.
Abstract
An antiproliferative ribonuclease with a new N-terminal sequence was purified from fruiting bodies of the edible wild mushroom Russula delica in this study. This novel ribonuclease was unadsorbed on DEAE-cellulose, but absorbed on SP-Sepharose and Q-Sepharose. It had a molecular mass of 14 kDa as ju...
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PMID: 20467240
PDF is available here.
PDF is available here.
The Journal of Chemical Physics (132)13 2010
Abstract
We present a detailed dynamics study of the catalytic core domain (CCD) of HIV-1 integrase using both polarized and nonpolarized force fields. The numerical results reveal the critical role of protein polarization in stabilizing Mg(2+) coordination complex in CCD. Specifically, when nonpolarized for...
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PMID: 20387913
PDF is available here.
PDF is available here.
Abstract
We created an HIV-1 cloning vector, pNL4.3DeltaIN, to generate recombinant infectious molecular clones for analysis of patient-derived HIV-1 integrase coding regions. Using this vector, we constructed a panel of clinically derived viruses with the canonical patterns of raltegravir resistance mutatio...
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PMID: 19917747
PDF is available here.
PDF is available here.
Voprosy Virusologii (55)1 2010
Abstract
The paper presents the data of an investigation of the polymorphism of the pol gene encoding HIV-1 integrase in a HIV subtype G infected population formed during the 1989 HIV-infection outbreak. The investigators analyzed 41 samples of the viruses obtained in 2005-2007. Polymorphism at codons associ...
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PMID: 20364666
PDF is available here.
PDF is available here.
Molecular Medicine (16)1-2 2010
Abstract
We show, for the first time, that formation of an Rev-LEDGF/p75 complex is a crucial step in regulating viral cDNA integration. Coimmunoprecipitation experiments at various times after virus infection revealed that, first, an integrase enzyme (IN)-LEDGF/p75 complex is formed, which is then replaced...
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PMID: 19855849
PDF is available here.
PDF is available here.
Abstract
Our observations demonstrate that Y143R/C mutants are strongly impaired for both of these activities in vitro. However, Y143R/C activity can be kinetically restored, thereby reproducing the effect of the secondary G140S mutation that rescues the defect associated with the Q148R/H mutants. A molecula...
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PMID: 19901095
PDF is available here.
PDF is available here.
Current Medicinal Chemistry (17)29 2010
Abstract
In recent years, the number of useful chemical biology information of protein-protein interactions in the HIV life cycle and related inhibitors, is growing rapidly, which makes protein-protein interactions a new investigative area for antiviral drug intervention. This review will summarize recent wo...
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PMID: 20712566
PDF is available here.
PDF is available here.
Journal of Virology (84)2 2010
Abstract
Our hypothesis is that evolutionarily conserved regions in LEDGF/p75 exposed to solvent and harboring posttranslational modifications may be involved in its HIV-1 cofactor activity. Therefore, a panel of LEDGF/p75 deletion mutants targeting these protein regions were evaluated for their HIV-1 cofact...
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PMID: 19889764
PDF is available here.
PDF is available here.
Journal of Antibiotics (62)12 2009
Abstract
I and MK1688 were investigated in vitro against human immunodeficiency virus type-1 (HIV-1) integrase and Moloney murine leukemia virus reverse transcriptase. BEA, EN I and EN MK1688 exhibited strong inhibitory activities against HIV-1 integrase, whereas EN H showed relatively weak activity. None of...
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PMID: 19893585
PDF is available here.
PDF is available here.
Abstract
We show the synthesis and the detailed structure-activity relationship of the quinolone carboxylic acids as a novel monoketo acid class of integrase inhibitors. 6-(3-Chloro-2-fluorobenzyl)-1-((2S)-1-hydroxy-3,3-dimethylbutan-2-yl)-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 51, which show...
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PMID: 19719237
PDF is available here.
PDF is available here.
Abstract
These results therefore establish a system whereby biotinylated matrix protein in the context of replication-competent virus could be used to label and capture viral protein complexes in vivo....
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PMID: 19490971
PDF is available here.
PDF is available here.
Journal of Biological Chemistry (284)30 2009
Abstract
We purified and biochemically characterized INI1. We found that INI1 forms multimeric structures. Deletion analysis indicated that the Rpt1 and Rpt2 motifs form the minimal multimerization domain. We isolated mutants of INI1 that are defective for multimerization using a reverse yeast two-hybrid sys...
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PMID: 19398554
PDF is available here.
PDF is available here.
Abstract
A novel compound inhibiting HIV-1 integrase has been identified by means of virtual screening techniques. A small family of structurally related molecules has been synthesized and biologically evaluated with some of the compounds possessing micromolar activity both in enzymatic and c...
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PMID: 19447621
PDF is available here.
PDF is available here.
Abstract
This study undertook an exploratory data analysis of the binding parameters of HIV-1 integrase inhibitors. The study group involved inhibitors in preclinical development from the diketo acid, pyrroloquinoline and naphthyridine carboxamide families and the most advanced inhibitors Ral...
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PMID: 19450984
PDF is available here.
PDF is available here.
EMBO Journal (28)7 2009
Abstract
We produced a stable and functional complex between the wild-type full-length integrase (IN) and the cellular cofactor LEDGF/p75 that shows enhanced in vitro integration activity compared with the integrase alone. Mass spectrometry analysis and the fitting of known atomic structures in cryo negative...
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PMID: 19229293
PDF is available here.
PDF is available here.
Abstract
A prototype assay was used to genotype integrase (IN) from 120 HIV-1- infected IN inhibitor-naive adults from Argentina, Brazil, Cameroon, South Africa, Thailand, and Uganda. Subtype designations based on analysis of pol IN sequences were A (14), B (15), C (12), D (11), F (12), G (7), H (1), CRF01_A...
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PMID: 19327053
PDF is available here.
PDF is available here.
Acta Pharmaceutica (59)1 2009
Abstract
HIV integrase has emerged as a promising target for discovery of agents against the acquired immunodeficiency syndrome (AIDS) pandemic. With the purpose of designing new chemotypes with enhanced potencies against the HIV integrase enzyme, the QSAR study carried out on 37 novel phthalimide derivative...
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PMID: 19304556
PDF is available here.
PDF is available here.
Abstract
: Resistance to RAL appeared initially associated with selection of single variants (Y143R, Q148R N155H) in the majority of patients; however, in three patients, complex patterns of viral mutations were observed. The clonal analysis of viral quasispecies allowed to describe the evolution of each vira...
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PMID: 19165083
PDF is available here.
PDF is available here.
Abstract
Abstract
Integrase (IN) inhibitors have proven to be highly beneficial in the treatment of HIV infection. The recently approved inhibitor, raltegravir, the phase III clinical trials compound elvitegravir, and all other agents reported to be in clinical trials bind to the active site of IN and share the same...
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PMID: 19197790
PDF is available here.
PDF is available here.
Journal of Molecular Biology (385)2 2009
Abstract
A tetramer model for human immunodeficiency virus type 1 (HIV-1) integrase (IN) with DNA representing long terminal repeat (LTR) termini was previously assembled to predict the IN residues that interact with the LTR termini; these predictions were experimentally verified for nine amino acid residues...
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PMID: 19014951
PDF is available here.
PDF is available here.
Abstract
Neither ablation of CD9, CD63 and/or CD81, nor overexpression of these tetraspanins was found to affect the efficiency of virus release. However, confirming recently reported data, tetraspanin overexpression in virus-producing cells resulted in the release of virions with substantially reduced infec...
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PMID: 19602278
PDF is available here.
PDF is available here.
Abstract
We found by two hybrids that the karyophilic lentiviral-encoded integrase (IN) interacts with two yeast microtubule-associated proteins, Dyn2p (dynein light chain protein) and Stu2p, a centrosomal protein (de Soultrait et al., 2002). Thus, to investigate the hinge between cytoplasmic retrograde tran...
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PMID: 19180639
PDF is available here.
PDF is available here.
Abstract
We have obtained a L-CA binding mode that explains its observed potency and is consistent with available experimental data. Because of the alpha,beta-unsaturated ester functionality of the side arms of L-CA we first performed an extensive conformational analysis of L-CA using semiempirical and ab in...
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PMID: 19004651
PDF is available here.
PDF is available here.
Antiviral Therapy (14)1 2009
Abstract
The major IN mutations E92Q, Q148K/R/H, N155H and E157Q (implicated in the resistance of IN inhibitors RAL and EVG) are highly conserved between subtypes B and CRF02_AG and display a similar genetic barrier. However, subtype CRFO2_AG showed a higher genetic barrier to acquire mutations 6140S, 6140C...
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PMID: 19320246
PDF is available here.
PDF is available here.
Abstract
The collision-dissociation behavior of two novel dimeric G-quadruplexes of HIV-1 integrase inhibitors and their noncovalent complex ions with a perylene derivative (Tel03), polyamides (ImImImbetaDp and PyPyPybetaDp) was investigated by tandem-in-time electrospray ionization mass spectrometry (ESI-MS...
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PMID: 19940339
PDF is available here.
PDF is available here.
AIDS Reviews (11)1 2009
Abstract
The HIV-1 integrase, responsible for the chromosomal integration of the newly synthesized double-stranded viral DNA into the host genomic DNA, represents a new and important target of potential clinical relevance. For instance, two integrase inhibitors, raltegravir and elvitegravir, have been shown...
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PMID: 19290031
PDF is available here.
PDF is available here.
Abstract
4-Oxo-4H-quinolizine-3-carboxylic acid derivatives bearing sulfamido, carboxylamido, benzimidazole and benzothiazole substituents have been designed and synthesized. The structures of these new compounds were confirmed by (1)H-NMR, (13)C- NMR, IR and ESI (or HRMS) spectra. Compounds were screened fo...
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PMID: 19255545
PDF is available here.
PDF is available here.
Antiviral Therapy (14)7 2009
Abstract
Primary integrase inhibitor resistance mutations were not detected in the absence of drug exposure in keeping with sites of high constraint. Viral polymorphisms caused by immune selection and/or associated with non-subtype B might alter the genetic barrier to some non-primary resistance-associated m...
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PMID: 19918099
PDF is available here.
PDF is available here.
Biochemistry (Washington) (47)51 2008
Abstract
Specific HIV integrase strand transfer inhibitors are thought to bind to the integrase active site, positioned to coordinate with two catalytic magnesium atoms in a pocket flanked by the end of the viral LTR. A structural role for the 3' terminus of the viral LTR in the inhibitor-bound state has not...
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PMID: 18991395
PDF is available here.
PDF is available here.
Abstract
Virtual screening docking-based approach has been employed in order to select novel HIV-1 integrase (IN) potential inhibitors in large databases. Toxicity, metabolism and drug-like properties have been analyzed for the most promising compounds, using computational chemistry techniques. Results were...
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PMID: 19356102
PDF is available here.
PDF is available here.
Nucleic Acids Research (36)22 2008
Abstract
We performed in vitro functional analysis comparing IN preparations having different oligomerization properties. We demonstrate that in vitro IN concerted integration activity on a long DNA substrate containing both specific viral and nonspecific DNA sequences is highly dependent on binding of prefo...
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PMID: 18987001
PDF is available here.
PDF is available here.
Journal of Biological Chemistry (283)46 2008
Abstract
We have conducted detailed biochemical characterization of the interactions between full-length IN and LEDGF. Our results reveal a highly dynamic nature of IN subunit-subunit interactions. LEDGF strongly stabilized these interactions and promoted IN tetramerization. Mass spectrometric protein footpr...
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PMID: 18801737
PDF is available here.
PDF is available here.
Abstract
We used a novel resistance selection protocol to follow the emergence of resistant HIV in the presence of the integrase inhibitor elvitegravir (GS-9137). We find the primary resistance-conferring mutations to be Q148R, E92Q, and T66I and demonstrate that they confer a reduction in susceptibility not...
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PMID: 18715920
PDF is available here.
PDF is available here.
Abstract
Despite 40% heterogeneity between the HIV-1 and HIV-2 integrase genes, the phenotypic susceptibility of clinical HIV-2 isolates to INIs was similar to that of HIV-1. This new class of antiretroviral drugs thus represents a novel therapeutic possibility for HIV-2-infected patients who otherwise have...
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PMID: 18718922
PDF is available here.
PDF is available here.
Enfermedades Infecciosas y Microbiología Clínica (26 Suppl 12) 2008
Abstract
Integrase inhibitors are the most recently approved family of antiretroviral agents for the treatment of HIV infection. As with other antiretroviral agents, under pharmacological pressure, the virus selects resistance mutations if viral suppression is incomplete. Mutations are selected in the integr...
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PMID: 19572425
PDF is available here.
PDF is available here.
Enfermedades Infecciosas y Microbiología Clínica (26 Suppl 12) 2008
Abstract
Enfermedades Infecciosas y Microbiología Clínica (26 Suppl 12) 2008
Abstract
The HIV replication cycle passes through a stage of integrating proviral DNA into the cell's DNA. In this process, the viral enzyme, integrase, catalyses two reactions. The first reaction, which seems to occur in the cytoplasm, involves 3'-end processing, in which two nucleotides are removed from th...
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PMID: 19572420
PDF is available here.
PDF is available here.
Enfermedades Infecciosas y Microbiología Clínica (26 Suppl 12) 2008
Abstract
Raltegravir is the first in a new class of antiretroviral treatments called integrase inhibitors, which work by preventing HIV from inserting its genetic material into the DNA of the human chromosome. Phase I-III studies have shown this drug to have potent antiretroviral action, which is more rapid...
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PMID: 19572423
PDF is available here.
PDF is available here.
Enfermedades Infecciosas y Microbiología Clínica (26 Suppl 12) 2008
Abstract
Integrase inhibitors are a new therapeutic modality against HIV. Raltegravir is the first integrase inhibitor to have been approved by the health authorities for human use. This drug acts by inhibiting the HIV enzyme that catalyzes integration of the virus inside the genome of the host cell. In the...
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PMID: 19572424
PDF is available here.
PDF is available here.
Abstract
We reported that a benzoic acid derivative, 4-[(5-bromo-4-{[2,4-dioxo-3-(2-oxo-2-phenylethyl)-1,3-thiazolidin-5-ylidene]methyl}-2-ethoxyphenoxy)methyl]benzoic acid (D77) could potently inhibit the IN-LEDGF/p75 interaction and affect the HIV-1 IN nuclear distribution thus exhibiting antiretroviral ac...
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PMID: 18691555
PDF is available here.
PDF is available here.
Abstract
HIV-1 integrase catalyzes the insertion of viral DNA into the genome of the host cell. Integrase inhibitor N-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide selectively inhibits the strand transfer process of integration. 4-Substituted pyrrolidinones possessing various groups on the pyrro...
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PMID: 18774711
PDF is available here.
PDF is available here.
Abstract
We have now made several mutations designed to alter the length or flexibility of a mobile loop within this 35-amino-acid spacer region in full-length Rous sarcoma virus integrase. Surprisingly, most of the mutants had enzymatic activity, including ones that shortened or lengthened the loop by up to...
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PMID: 18687451
PDF is available here.
PDF is available here.
HIV Medicine (9)9 2008
Drug resistance profiles for the HIV integrase gene in patients failing raltegravir salvage therapy.
Abstract
Having rapidly established, resistance to RAL evolves and diversifies, and is likely to impact the efficacy of subsequently used second-generation integrase inhibitors. Moreover, RAL-resistance mutations can be archived early in PBMC....
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PMID: 18651855
PDF is available here.
PDF is available here.
Abstract
A successful synthesis of fukiic acid is described in 7% overall yield (6 steps from veratraldehyde). rac-Fukiic acid was found to be a potent inhibitor of HIV-1 integrase but did not reveal any antiviral activity in the MT-4 cells assay.
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PMID: 18243421
PDF is available here.
PDF is available here.
Abstract
The contribution of clade-specific polymorphisms in the HIV-1 integrase gene towards integrase inhibitor phenotypic susceptibility was tested on 137 clinical isolates, of which 60 were non-clade B strains. Control Q148R mutant virus showed fold change values of 17.85 +/- 2.77 and 88.94 +/- 9.02 for...
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PMID: 18753927
PDF is available here.
PDF is available here.
Biochemistry (Washington) (47)36 2008
Abstract
We found an inverse correlation between resistance and catalytic activity of the IN mutants....
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PMID: 18702518
PDF is available here.
PDF is available here.
Abstract
We explored the kinetics of product formation and strand transfer inhibition within reconstituted synaptic complexes capable of concerted integration. Synaptic complexes were formed with viral DNA donors containing either two blunt ends, two 3'-OH-processed ends, or one of each. We determined that o...
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PMID: 18591263
PDF is available here.
PDF is available here.
Journal of Virology (82)18 2008
Abstract
We have undertaken a study to fully characterize natural polymorphisms and amino acid covariation within an inhibitor-naïve sequence set spanning all defined HIV-1 subtypes. Inter- and intrasubtype variation was greatest in a 50-amino-acid segment of HIV-1 integrase incorporating the catalytic aspa...
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PMID: 18596095
PDF is available here.
PDF is available here.
Journal of Biological Chemistry (283)35 2008
Abstract
In this study, eight different HIV-1 integrase proteins containing mutations observed in strand transfer inhibitor-resistant viruses were expressed, purified, and used for detailed enzymatic analyses. All the variants examined were impaired for strand transfer activity compared with the wild type en...
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PMID: 18577511
PDF is available here.
PDF is available here.
Current Biology (18)16 2008
Abstract
Using yeast two-hybrid and pull-down, we identified and validated transportin-SR2 (TRN-SR2) as a bona fide binding partner of HIV-1 integrase. We confirmed the biological relevance of this interaction by RNAi. Depletion of TRN-SR2 interfered with the replication of HIV-1 and HIV-2 but not MoMLV in H...
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PMID: 18722123
PDF is available here.
PDF is available here.
Current Biology (18)16 2008
Abstract
Factors necessary for HIV-1 nuclear import have been sought for many years. Recent reports suggest that TNPO3/Transportin-SR2 binds to HIV-1 integrase and is required for HIV-1 infection of interphase cells.
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PMID: 18727908
PDF is available here.
PDF is available here.