ArticleTetrahedron2014
Direct Ras Inhibitors Identified from a Structurally Rigidified Bicyclic Peptide Library.
Article in Tetrahedron, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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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
19 citing papers in PubMed, 39 citations in OpenAlex.
- Review
- Tackling Undruggable Targets with Designer Peptidomimetics and Synthetic Biologics.Chemical reviews · 2024Review
- Design, synthesis, and analysis of macrobicyclic peptides for targeting the Gαi protein.Journal of peptide science : an official publication of the European Peptide Society · 2024Article
- Bicyclic Peptide Library Screening for the Identification of Gαi Protein Modulators.Journal of medicinal chemistry · 2023Article
- Targeting the 'Undruggable' Driver Protein, KRAS, in Epithelial Cancers: Current Perspective.Cells · 2023Review
- Designing Cell-Permeable Peptide Therapeutics That Enter the Cell by Endocytosis.ACS symposium series. American Chemical Society · 2022Article
- Targeting the "undruggable" RAS with biologics.Advances in cancer research · 2022Review
- Discovery of a Bicyclic Peptidyl Pan-Ras Inhibitor.Journal of medicinal chemistry · 2021Article
- Approaches to inhibiting oncogenic K-Ras.Small GTPases · 2021Review
- Small and Simple, yet Sturdy: Conformationally Constrained Peptides with Remarkable Properties.International journal of molecular sciences · 2021Review
- Discovery of High-Affinity Noncovalent Allosteric KRAS Inhibitors That Disrupt Effector Binding.ACS omega · 2019Article
- The K-Ras, N-Ras, and H-Ras Isoforms: Unique Conformational Preferences and Implications for Targeting Oncogenic Mutants.Cold Spring Harbor perspectives in medicine · 2018Review
- Targeting Ras with Macromolecules.Cold Spring Harbor perspectives in medicine · 2018Review
- Bicyclic Peptides as Next-Generation Therapeutics.Chemistry (Weinheim an der Bergstrasse, Germany) · 2017Review
- Macrocycles as protein-protein interaction inhibitors.The Biochemical journal · 2017Review
- Drugging Ras GTPase: a comprehensive mechanistic and signaling structural view.Chemical Society reviews · 2016Review
- Discovery of a Direct Ras Inhibitor by Screening a Combinatorial Library of Cell-Permeable Bicyclic Peptides.ACS combinatorial science · 2016Article
- Inhibition of Ras signaling by blocking Ras-effector interactions with cyclic peptides.Angewandte Chemie (International ed. in English) · 2015Article
- Binding hotspots on K-ras: consensus ligand binding sites and other reactive regions from probe-based molecular dynamics analysis.Proteins · 2015Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
A one-bead-two-compound (OBTC) library of structurally rigidified bicyclic peptides was chemically synthesized on TentaGel microbeads (90 μm), with each bead displaying a unique bicyclic peptide on its surface and a linear encoding peptide of the same sequence in its interior. Screening of the library against oncogenic K-Ras G12V mutant identified two classes of Ras ligands. The class I ligands apparently bind to the effector-binding site and inhibit the Ras-Raf interaction, whereas the class II ligand appears to bind to a yet unidentified site different from the effector-binding site. These Ras ligands provide useful research tools and may be further developed into therapeutic agents.
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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.