ArticleAngewandte Chemie (International ed. in English)2017
Peptide-Directed Binding for the Discovery of Modulators of α-Helix-Mediated Protein-Protein Interactions: Proof-of-Concept Studies with the Apoptosis Regulator Mcl-1.
Article in Angewandte Chemie (International ed. in English), 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed.
- Discovery of SHANK1-PDZ Peptide-Fragment Inhibitors Using a Dynamic Ligation Screening Strategy.Biochemistry · 2026Article
- Synthesis and Biological Evaluation of 4‑(4-Nitrophenyl)‑1ACS omega · 2025Article
- Strategies for converting turn-motif and cyclic peptides to small molecules for targeting protein-protein interactions.RSC chemical biology · 2024Review
- 30th Annual GPPharmaceuticals (Basel, Switzerland) · 2023Article
- Computational approaches for the design of modulators targeting protein-protein interactions.Expert opinion on drug discovery · 2023Review
- 29th Annual GP2A Medicinal Chemistry Conference.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Article
- Identification of β-strand mediated protein-protein interaction inhibitors using ligand-directed fragment ligation.Chemical science · 2021Article
- Rational Design of Peptide-Based Inhibitors Disrupting Protein-Protein Interactions.Frontiers in chemistry · 2021Review
- Identification of selective protein-protein interaction inhibitors using efficientChemical science · 2019Article
- Peptide-Directed Binding for the Discovery of Modulators of α-Helix-Mediated Protein-Protein Interactions: Proof-of-Concept Studies with the Apoptosis Regulator Mcl-1.Angewandte Chemie (International ed. in English) · 2017Article
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Authors and funding
3 authors.
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Abstract
Targeting PPIs with small molecules can be challenging owing to large, hydrophobic binding surfaces. Herein, we describe a strategy that exploits selective α-helical PPIs, transferring these characteristics to small molecules. The proof of concept is demonstrated with the apoptosis regulator Mcl-1, commonly exploited by cancers to avoid cell death. Peptide-directed binding uses few synthetic transformations, requires the production of a small number of compounds, and generates a high percentage of hits. In this example, about 50 % of the small molecules prepared showed an IC
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