ReviewChemMedChem2011
Allosteric inhibitor development targeting HIV-1 integrase.
Review in ChemMedChem, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
18 citing papers in PubMed, 59 citations in OpenAlex.
- Targeting Human Immunodeficiency Virus Integrase Beyond the Active Site: The Discovery and Development of Allosteric Integrase Inhibitors.ChemMedChem · 2026Review
- Exploring Zinc C295 as a Dual HIV-1 Integrase Inhibitor: From Strand Transfer to 3'-Processing Suppression.Pharmaceuticals (Basel, Switzerland) · 2024Article
- The chromatin landscape at the HIV-1 provirus integration site determines viral expression.Nucleic acids research · 2020Article
- Block-And-Lock Strategies to Cure HIV Infection.Viruses · 2020Review
- Impact of LEDGIN treatment during virus production on residual HIV-1 transcription.Retrovirology · 2019Article
- Probing Resistance Mutations in Retroviral Integrases by Direct Measurement of Dolutegravir Fluorescence.Scientific reports · 2017Article
- Development and Identification of a Novel Anti-HIV-1 Peptide Derived by Modification of the N-Terminal Domain of HIV-1 Integrase.Frontiers in microbiology · 2016Article
- Cure for acquired immunodeficiency syndrome--a global battle.Chinese journal of integrative medicine · 2014Review
- Cofactor-independent phosphoglycerate mutase from nematodes has limited druggability, as revealed by two high-throughput screens.PLoS neglected tropical diseases · 2014Article
- Molecular modeling study on the allosteric inhibition mechanism of HIV-1 integrase by LEDGF/p75 binding site inhibitors.PloS one · 2014Article
- Allosteric inhibition of HIV-1 integrase activity.Current opinion in chemical biology · 2013Review
- LEDGINs inhibit late stage HIV-1 replication by modulating integrase multimerization in the virions.Retrovirology · 2013Article
- The activity of the integrase inhibitor dolutegravir against HIV-1 variants isolated from raltegravir-treated adults.Journal of acquired immune deficiency syndromes (1999) · 2012Article
- Phage display-directed discovery of LEDGF/p75 binding cyclic peptide inhibitors of HIV replication.Molecular therapy : the journal of the American Society of Gene Therapy · 2012Article
- In vitro evolution of an HIV integrase binding protein from a library of C-terminal domain γS-crystallin variants.Bioorganic & medicinal chemistry letters · 2012Article
- New class of HIV-1 integrase (IN) inhibitors with a dual mode of action.The Journal of biological chemistry · 2012Article
- Design of HIV-1 integrase inhibitors targeting the catalytic domain as well as its interaction with LEDGF/p75: a scaffold hopping approach using salicylate and catechol groups.Bioorganic & medicinal chemistry · 2011Article
- Localization of ASV integrase-DNA contacts by site-directed crosslinking and their structural analysis.PloS one · 2011Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
HIV-1 integrase (IN) is one of three essential enzymes for viral replication, and is a focus of ardent antiretroviral drug discovery and development efforts. Diligent research has led to the development of the strand-transfer-specific chemical class of IN inhibitors, with two compounds from this group, raltegravir and elvitegravir, advancing the farthest in the US Food and Drug Administration (FDA) approval process for any IN inhibitor discovered thus far. Raltegravir, developed by Merck & Co., has been approved by the FDA for HIV-1 therapy, whereas elvitegravir, developed by Gilead Sciences and Japan Tobacco, has reached phase III clinical trials. Although this is an undoubted success for the HIV-1 IN drug discovery field, the emergence of HIV-1 IN strand-transfer-specific drug-resistant viral strains upon clinical use of these compounds is expected. Furthermore, the problem of strand-transfer-specific IN drug resistance will be exacerbated by the development of cross-resistant viral strains due to an overlapping binding orientation at the IN active site and an equivalent inhibitory mechanism for the two compounds. This inevitability will result in no available IN-targeted therapeutic options for HIV-1 treatment-experienced patients. The development of allosterically targeted IN inhibitors presents an extremely advantageous approach for the discovery of compounds effective against IN strand-transfer drug-resistant viral strains, and would likely show synergy with all available FDA-approved antiretroviral HIV-1 therapeutics, including the IN strand-transfer-specific compounds. Herein we review the concept of allosteric IN inhibition, and the small molecules that have been investigated to bind non-active-site regions to inhibit IN function.
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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.