ArticleAngewandte Chemie (International ed. in English)2017
Development of Cell-Permeable, Non-Helical Constrained Peptides to Target a Key Protein-Protein Interaction in Ovarian Cancer.
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 15 papers.
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Who cites it
15 citing papers in PubMed, 46 citations in OpenAlex.
- A Sydnonimine-based Click-and-Release Approach to Cyclic Products.Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
- Transanal total mesorectal excision and transabdominal robotic surgery for rectal cancer: A retrospective study.Annals of medicine and surgery (2012) · 2021Article
- Macrocyclization strategies for cyclic peptides and peptidomimetics.RSC medicinal chemistry · 2021Review
- Cyclisation strategies for stabilising peptides with irregular conformations.RSC medicinal chemistry · 2021Review
- Peptide-based inhibitors of protein-protein interactions: biophysical, structural and cellular consequences of introducing a constraint.Chemical science · 2021Review
- Computational Design of Macrocyclic Binders of S100B(ββ): Novel Peptide Theranostics.Molecules (Basel, Switzerland) · 2021Article
- Macrocyclization of an all-d linear α-helical peptide imparts cellular permeability.Chemical science · 2020Article
- Regulator of G-protein signaling (RGS) proteins as drug targets: Progress and future potentials.The Journal of biological chemistry · 2019Review
- Efficient development of stable and highly functionalised peptides targeting the CK2α/CK2β protein-protein interaction.Chemical science · 2019Article
- Dithiocarbamate-inspired side chain stapling chemistry for peptide drug design.Chemical science · 2019Article
- Emerging Methods and Design Principles for Cell-Penetrant Peptides.Angewandte Chemie (International ed. in English) · 2018Review
- Using Peptidomimetics and Constrained Peptides as Valuable Tools for Inhibiting Protein⁻Protein Interactions.Molecules (Basel, Switzerland) · 2018Review
- Reversible stapling of unprotected peptidesChemical science · 2018Article
- Macrocyclized Extended Peptides: Inhibiting the Substrate-Recognition Domain of Tankyrase.Journal of the American Chemical Society · 2017Article
- Development of Cell-Permeable, Non-Helical Constrained Peptides to Target a Key Protein-Protein Interaction in Ovarian Cancer.Angewandte Chemie (International ed. in English) · 2017Article
Corrections and comments
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Authors and funding
11 authors at 4 institutions in 4 countries.
Funding
Abstract
There is a lack of current treatment options for ovarian clear cell carcinoma (CCC) and the cancer is often resistant to platinum-based chemotherapy. Hence there is an urgent need for novel therapeutics. The transcription factor hepatocyte nuclear factor 1β (HNF1β) is ubiquitously overexpressed in CCC and is seen as an attractive therapeutic target. This was validated through shRNA-mediated knockdown of the target protein, HNF1β, in five high- and low-HNF1β-expressing CCC lines. To inhibit the protein function, cell-permeable, non-helical constrained proteomimetics to target the HNF1β-importin α protein-protein interaction were designed, guided by X-ray crystallographic data and molecular dynamics simulations. In this way, we developed the first reported series of constrained peptide nuclear import inhibitors. Importantly, this general approach may be extended to other transcription factors.
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Registered trials
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