ArticleProceedings of the National Academy of Sciences of the United States of America2004
Guanidine alkaloid analogs as inhibitors of HIV-1 Nef interactions with p53, actin, and p56lck.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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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.
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Who cites it
27 citing papers in PubMed, 64 citations in OpenAlex.
- DRAM triggers lysosomal membrane permeabilization and cell death in CD4(+) T cells infected with HIV.PLoS pathogens · 2013Trial
- Manipulation of the cell cycle by HIV-1.Biochemical Society transactions · 2026Review
- Hypervalent Iodine-Mediated Synthesis of Steroidal 5/5-Spiroiminals.Molecules (Basel, Switzerland) · 2024Article
- Marine-Derived Anticancer Agents Targeting Apoptotic Pathways: Exploring the Depths for Novel Cancer Therapies.Marine drugs · 2024Review
- Investigating the structure-activity relationship of marine polycyclic batzelladine alkaloids as promising inhibitors for SARS-CoV-2 main protease (MComputers in biology and medicine · 2022Article
- Comprehensive Virtual Screening of the Antiviral Potentialities of Marine Polycyclic Guanidine Alkaloids against SARS-CoV-2 (COVID-19).Biomolecules · 2021Article
- Crambescin C1 Acts as A Possible Substrate of iNOS and eNOS Increasing Nitric Oxide Production and InducingFrontiers in pharmacology · 2021Article
- Concise Synthesis and Antimicrobial Evaluation of the Guanidinium Alkaloid Batzelladine D: Development of a Stereodivergent Strategy.Journal of the American Chemical Society · 2020Article
- HIV-1 Impairment via UBE3A and HIV-1 Nef Interactions Utilizing the Ubiquitin Proteasome System.Viruses · 2019Article
- Kinase-Based Screening of Marine Natural Extracts Leads to the Identification of a Cytotoxic High Molecular Weight Metabolite from the Mediterranean SpongeMarine drugs · 2019Article
- Review of Current Cell-Penetrating Antibody Developments for HIV-1 Therapy.Molecules (Basel, Switzerland) · 2018Review
- Review
- Structure, synthesis and biological properties of the pentacyclic guanidinium alkaloids.Bioorganic & medicinal chemistry · 2017Review
- Crambescin C1 Exerts a Cytoprotective Effect on HepG2 Cells through Metallothionein Induction.Marine drugs · 2015Article
- Syntheses of Cyclic Guanidine-Containing Natural Products.Tetrahedron · 2015Article
- Identification of a novel binding site between HIV type 1 Nef C-terminal flexible loop and AP2 required for Nef-mediated CD4 downregulation.AIDS research and human retroviruses · 2013Article
- The scope of phage display for membrane proteins.Journal of molecular biology · 2011Article
- Computational design and selections for an engineered, thermostable terpene synthase.Protein science : a publication of the Protein Society · 2011Article
- Discovery of new antimalarial chemotypes through chemical methodology and library development.Proceedings of the National Academy of Sciences of the United States of America · 2011Article
- The identification of a small molecule compound that reduces HIV-1 Nef-mediated viral infectivity enhancement.PloS one · 2011Article
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
Abstract
With current anti-HIV treatments targeting only 4 of the 15 HIV proteins, many potential viral vulnerabilities remain unexploited. We report small-molecule inhibitors of the HIV-1 protein Nef. In addition to expanding the anti-HIV arsenal, small-molecule inhibitors against untargeted HIV proteins could be used to dissect key events in the HIV lifecycle. Numerous incompletely characterized interactions between Nef and cellular ligands, for example, present a challenge to understanding molecular events during HIV progression to AIDS. Assays with phage-displayed Nef from HIV(NL4-3) were used to identify a series of guanidine alkaloid-based inhibitors of Nef interactions with p53, actin, and p56(lck). The guanidines, synthetic analogs of batzellidine and crambescidin natural products, inhibit the Nef-ligand interactions with IC(50) values in the low micromolar range. In addition, sensitive in vivo assays for Nef inhibition are reported. Although compounds that are effective in vitro proved to be too cytotoxic for cellular assays, the reported Nef inhibitors provide proof-of-concept for disrupting a new HIV target and offer useful leads for drug development.
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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.