Evolution of Potential Antimitotic Stapled Peptides from Multiple Helical Peptide Stretches of the Tubulin Heterodimer Interface: Helix-Mimicking Stapled Peptide Tubulin Inhibitors.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01116
Abstract: Protein-protein interactions play a crucial role in microtubule dynamics. Microtubules are considered as a key target for the design and development of anticancer therapeutics, where inhibition of tubulin-tubulin interactions plays a crucial role. Here, we… read more here.
Keywords: evolution potential; stapled peptide; potential antimitotic; tubulin ... See more keywords
Functionalized Double Strain-Promoted Stapled Peptides for Inhibiting the p53-MDM2 Interaction
Sign Up to like & getrecommendations! Published in 2020 at "ACS Omega"
DOI: 10.1021/acsomega.9b03459
Abstract: The Sondheimer dialkyne reagent has previously been employed in strain-promoted double-click cycloadditions with bis-azide peptides to generate stapled peptide inhibitors of protein-protein interactions. The substituted variants of the Sondheimer dialkyne can be used to generate… read more here.
Keywords: sondheimer dialkyne; strain promoted; stapled peptide; p53 mdm2 ... See more keywords
Structural Studies of a Stapled Peptide with Native Ion Mobility-Mass Spectrometry and Transition Metal Ion Förster Resonance Energy Transfer in the Gas Phase.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of the American Chemical Society"
DOI: 10.1021/jacs.2c02776
Abstract: Native mass spectrometry has emerged as an important tool for gas-phase structural biology. However, the conformations that a biomolecular ion adopts in the gas phase can differ from those found in solution. Herein, we report… read more here.
Keywords: mass spectrometry; gas phase; stapled peptide; ion ... See more keywords
A new strategy for the in vitro selection of stapled peptide inhibitors by mRNA display.
Sign Up to like & getrecommendations! Published in 2019 at "Chemical communications"
DOI: 10.1039/c8cc10192b
Abstract: Hydrocarbon stapled peptides are promising therapeutics for inhibition of intracellular protein-protein interactions. Here we develop a new high-throughput strategy for hydrocarbon stapled peptide discovery based on mRNA display of peptides containing α-methyl cysteine and cyclized… read more here.
Keywords: stapled peptide; vitro selection; mrna display; strategy vitro ... See more keywords
The Dual Interactions of p53 with MDM2 and p300: Implications for the Design of MDM2 Inhibitors
Sign Up to like & getrecommendations! Published in 2019 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms20235996
Abstract: Proteins that limit the activity of the tumour suppressor protein p53 are increasingly being targeted for inhibition in a variety of cancers. In addition to the development of small molecules, there has been interest in… read more here.
Keywords: mdm2 p300; mdm2; stapled peptide; p53 ... See more keywords
Design of stapled peptide-based PROTACs for MDM2/MDMX atypical degradation and tumor suppression
Sign Up to like & getrecommendations! Published in 2022 at "Theranostics"
DOI: 10.7150/thno.75444
Abstract: Rationale: Although stapled peptides offer a powerful solution to overcome the susceptibility of linear peptides to proteolytic degradation and improve their ability to cross membranes, an efficient and durable disease treatment strategy has not yet… read more here.
Keywords: peptide based; mdm2 mdmx; stapled peptide; atypical degradation ... See more keywords