ArticleChembiochem : a European journal of chemical biology2011
Peptide structure stabilization by membrane anchoring and its general applicability to the development of potent cell-permeable inhibitors.
Article in Chembiochem : a European journal of chemical biology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- Article
- Application ofMolecules (Basel, Switzerland) · 2019Article
- Position of lipidation influences anticancer activity of Smac analogs.Bioorganic & medicinal chemistry letters · 2019Article
- Computational and experimental analysis of bioactive peptide linear motifs in the integrin adhesome.PloS one · 2019Article
- Cholesterol-modified Hydroxychloroquine-loaded Nanocarriers in Bleomycin-induced Pulmonary Fibrosis.Scientific reports · 2017Article
- Peptide Lipidation - A Synthetic Strategy to Afford Peptide Based Therapeutics.Advances in experimental medicine and biology · 2017Review
- High-Affinity Interaction of the K-Ras4B Hypervariable Region with the Ras Active Site.Biophysical journal · 2015Article
- Small cyclic agonists of iron regulatory hormone hepcidin.Bioorganic & medicinal chemistry letters · 2015Article
- Lipid-conjugated Smac analogues.Bioorganic & medicinal chemistry letters · 2015Article
- Article
- Review
- Turning receptors on and off with intracellular pepducins: new insights into G-protein-coupled receptor drug development.The Journal of biological chemistry · 2012Review
- A lipid-anchored neurokinin 1 receptor antagonist prolongs pain relief by a three-pronged mechanism of action targeting the receptor at the plasma membrane and in endosomes.The Journal of biological chemistryArticle
Corrections and comments
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Authors and funding
8 authors.
Funding
Abstract
Isolated protein motifs that are involved in interactions with their binding partners can be used to inhibit these interactions. However, peptides corresponding to protein fragments tend to have no defined secondary or tertiary structure in the absence of scaffolding by the rest of protein molecule. This results in low inhibitor potency. NMR and CD spectroscopy studies of lipopeptide inhibitors of the Hedgehog pathway revealed that membrane anchoring allows the cell membrane to function as a scaffold and facilitate the folding of short peptides. In addition, lipidation enhances cell permeability and increases the concentration of the compounds near the membrane, thus facilitating potent inhibition. The general applicability of this rational approach was further confirmed by the generation of selective antagonists of the insulin-like growth factor 1 receptor with GI(50) values in the nanomolar range. Lipopeptides corresponding to protein fragments were found to serve as potent and selective inhibitors of a number of nondruggable molecular targets.
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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.