ArticleProceedings of the National Academy of Sciences of the United States of America2009
Catalytically-active complex of HIV-1 integrase with a viral DNA substrate binds anti-integrase drugs.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
What it found
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Who cites it
21 citing papers in PubMed, 36 citations in OpenAlex.
- Strain-specific effect on biphasic DNA binding by HIV-1 integrase.AIDS (London, England) · 2019Article
- Targeting Metalloenzymes for Therapeutic Intervention.Chemical reviews · 2019Review
- The conformational feasibility for the formation of reaching dimer in ASV and HIV integrase: a molecular dynamics study.Journal of biomolecular structure & dynamics · 2017Article
- Structural Basis for Inhibitor-Induced Aggregation of HIV Integrase.PLoS biology · 2016Article
- The Preserved HTH-Docking Cleft of HIV-1 Integrase Is Functionally Critical.Structure (London, England : 1993) · 2016Article
- Allosteric inhibition of human immunodeficiency virus integrase: late block during viral replication and abnormal multimerization involving specific protein domains.The Journal of biological chemistry · 2014Article
- A possible role for the asymmetric C-terminal domain dimer of Rous sarcoma virus integrase in viral DNA binding.PloS one · 2013Article
- Fabs enable single particle cryoEM studies of small proteins.Structure (London, England : 1993) · 2012Article
- HIV-1 integrase strand transfer inhibitors stabilize an integrase-single blunt-ended DNA complex.Journal of molecular biology · 2011Article
- HIV-1 integrase inhibitor resistance and its clinical implications.The Journal of infectious diseases · 2011Review
- 3-Hydroxypyrimidine-2,4-diones as an inhibitor scaffold of HIV integrase.Journal of medicinal chemistry · 2011Article
- Structural biology of retroviral DNA integration.Virology · 2011Review
- Localization of ASV integrase-DNA contacts by site-directed crosslinking and their structural analysis.PloS one · 2011Article
- HIV-1 integrase sequence variability in antiretroviral naïve patients and in triple-class experienced patients subsequently treated with raltegravir.AIDS research and human retroviruses · 2010Article
- Structure-based modeling of the functional HIV-1 intasome and its inhibition.Proceedings of the National Academy of Sciences of the United States of America · 2010Article
- Structural properties of HIV integrase. Lens epithelium-derived growth factor oligomers.The Journal of biological chemistry · 2010Article
- Scaffold rearrangement of dihydroxypyrimidine inhibitors of HIV integrase: Docking model revisited.Bioorganic & medicinal chemistry letters · 2010Article
- The HIV-1 integrase mutations Y143C/R are an alternative pathway for resistance to Raltegravir and impact the enzyme functions.PloS one · 2010Article
- Article
- HIV-1 Integrase-DNA Recognition Mechanisms.Viruses · 2009Article
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 2 countries.
Funding
Abstract
HIV-1 integration into the host cell genome is a multistep process catalyzed by the virally-encoded integrase (IN) protein. In view of the difficulty of obtaining a stable DNA-bound IN at high concentration as required for structure determination, we selected IN-DNA complexes that form disulfide linkages between 5'-thiolated DNA and several single mutations to cysteine around the catalytic site of IN. Mild reducing conditions allowed for selection of the most thermodynamically-stable disulfide-linked species. The most stable complexes induce tetramer formation of IN, as happens during the physiological integration reaction, and are able to catalyze the strand transfer step of retroviral integration. One of these complexes also binds strand-transfer inhibitors of HIV antiviral drugs, making it uniquely valuable among the mutants of this set for understanding portions of the integration reaction. This novel complex may help define substrate interactions and delineate the mechanism of action of known integration inhibitors.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.