ArticleThe Biochemical journal2010
Identification of broad-based HIV-1 protease inhibitors from combinatorial libraries.
Article in The Biochemical journal, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 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
14 citing papers in PubMed, 19 citations in OpenAlex.
- High-throughput screening for the identification of small-molecule inhibitors of the flaviviral protease.Antiviral research · 2016Article
- Review
- Discovery libraries targeting the major enzyme classes: the serine hydrolases.Bioorganic & medicinal chemistry letters · 2014Article
- An allosteric modulator of HIV-1 protease shows equipotent inhibition of wild-type and drug-resistant proteases.Journal of medicinal chemistry · 2014Article
- Understanding HIV-1 protease autoprocessing for novel therapeutic development.Future medicinal chemistry · 2013Article
- Effects of HIV-1 protease on cellular functions and their potential applications in antiretroviral therapy.Cell & bioscience · 2012Article
- Review
- Discovery of HIV fusion inhibitors targeting gp41 using a comprehensive α-helix mimetic library.Bioorganic & medicinal chemistry letters · 2012Article
- Protease-Mediated Maturation of HIV: Inhibitors of Protease and the Maturation Process.Molecular biology international · 2012Article
- Flexible catalytic site conformations implicated in modulation of HIV-1 protease autoprocessing reactions.Retrovirology · 2011Article
- Design, synthesis, and validation of a β-turn mimetic library targeting protein-protein and peptide-receptor interactions.Journal of the American Chemical Society · 2011Article
- Tetrahydrofuran, tetrahydropyran, triazoles and related heterocyclic derivatives as HIV protease inhibitors.Future medicinal chemistry · 2011Review
- Novel approaches in anti-arenaviral drug development.Virology · 2011Review
- Emerging principles in protease-based drug discovery.Nature reviews. Drug discovery · 2010Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
11 authors at 1 institution in 1 country.
Funding
Abstract
Clinically approved inhibitors of the HIV-1 protease function via a competitive mechanism. A particular vulnerability of competitive inhibitors is their sensitivity to increases in substrate concentration, as may occur during virion assembly, budding and processing into a mature infectious viral particle. Advances in chemical synthesis have led to the development of new high-diversity chemical libraries using rapid in-solution syntheses. These libraries have been shown previously to be effective at disrupting protein-protein and protein-nucleic acid interfaces. We have screened 44000 compounds from such a library to identify inhibitors of the HIV-1 protease. One compound was identified that inhibits wild-type protease, as well as a drug-resistant protease with six mutations. Moreover, analysis of this compound suggests an allosteric non-competitive mechanism of inhibition and may represent a starting point for an additional strategy for anti-retroviral therapy.
Indexed as
Identifiers
What OpenQuestion holds
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.