ArticleACS chemical biology2016
N-Methylation as a Strategy for Enhancing the Affinity and Selectivity of RNA-binding Peptides: Application to the HIV-1 Frameshift-Stimulating RNA.
Article in ACS chemical biology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 39 citations in OpenAlex.
- Small Molecules Targeting Viral RNA.International journal of molecular sciences · 2023Review
- Modelling the structures of frameshift-stimulatory pseudoknots from representative bat coronaviruses.PLoS computational biology · 2023Article
- Perturbing HIV-1 Ribosomal Frameshifting Frequency Reveals aJournal of virology · 2022Article
- The Deuterated "Magic Methyl" Group: A Guide to Site-Selective Trideuteromethyl Incorporation and Labeling by Using CDChemistry (Weinheim an der Bergstrasse, Germany) · 2021Review
- Anti-Frameshifting Ligand Active against SARS Coronavirus-2 Is Resistant to Natural Mutations of the Frameshift-Stimulatory Pseudoknot.Journal of molecular biology · 2020Article
- Targeting mRNA processing as an anticancer strategy.Nature reviews. Drug discovery · 2020Review
- Enhancing the ligand efficiency of anti-HIV compounds targeting frameshift-stimulating RNA.Bioorganic & medicinal chemistry · 2019Article
- Understanding the Contributions of Conformational Changes, Thermodynamics, and Kinetics of RNA-Small Molecule Interactions.ACS chemical biology · 2019Review
- RNA Structural Differentiation: Opportunities with Pattern Recognition.Biochemistry · 2019Review
- Insights into the development of chemical probes for RNA.Nucleic acids research · 2018Article
- Incorporating uracil and 5-halouracils into short peptide nucleic acids for enhanced recognition of A-U pairs in dsRNAs.Nucleic acids research · 2018Article
- Translation Elongation and Recoding in Eukaryotes.Cold Spring Harbor perspectives in biology · 2018Review
- Specific reverse transcriptase slippage at the HIV ribosomal frameshift sequence: potential implications for modulation of GagPol synthesis.Nucleic acids research · 2017Article
- HIV-1 Frameshift RNA-Targeted Triazoles Inhibit Propagation of Replication-Competent and Multi-Drug-Resistant HIV in Human Cells.ACS chemical biology · 2017Article
- DMAP-assisted sulfonylation as an efficient step for the methylation of primary amine motifs on solid support.Beilstein journal of organic chemistry · 2017Article
- Engineering an Affinity-Enhanced Peptide through Optimization of Cyclization Chemistry.Bioconjugate chemistry · 2016Article
- Development of peptide inhibitors of HIV transmission.Bioactive materials · 2016Review
- The Emerging Role of RNA as a Therapeutic Target for Small Molecules.Cell chemical biology · 2016Review
- Ribosomal frameshifting and transcriptional slippage: From genetic steganography and cryptography to adventitious use.Nucleic acids research · 2016Review
- Probing the geometric constraints of RNA binding via dynamic covalent chemistry.Bioorganic & medicinal chemistry · 2016Article
Corrections and comments
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Authors and funding
11 authors at 4 institutions in 1 country.
Funding
Abstract
Human Immunodeficiency Virus (HIV) type 1 uses a -1 programmed ribosomal frameshift (-1 PRF) event to translate its enzymes from the same transcript used to encode the virus' structural proteins. The frequency of this event is highly regulated, and significant deviation from the normal 5-10% frequency has been demonstrated to decrease viral infectivity. Frameshifting is primarily regulated by the Frameshift Stimulatory Signal RNA (FSS-RNA), a thermodynamically stable, highly conserved stem loop that has been proposed as a therapeutic target. We describe the design, synthesis, and testing of a series of N-methyl peptides able to bind the HIV-1 FSS RNA stem loop with low nanomolar affinity and high selectivity. Surface plasmon resonance (SPR) data indicates increased affinity is a reflection of a substantially enhanced on rate. Compounds readily penetrate cell membranes and inhibit HIV infectivity in a pseudotyped virus assay. Viral infectivity inhibition correlates with compound-dependent changes in the ratios of Gag and Gag-Pol in virus particles. As the first compounds with both single digit nanomolar affinities for the FSS RNA and an ability to inhibit HIV in cells, these studies support the use of N-methylation for enhancing the affinity, selectivity, and bioactivity of RNA-binding peptides.
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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.