Recent Advances in Late‐Stage Construction of Stapled Peptides via C−H Activation
Sign Up to like & getrecommendations! Published in 2021 at "ChemBioChem"
DOI: 10.1002/cbic.202100044
Abstract: Stapled peptides have been widely applied in many fields, including pharmaceutical chemistry, diagnostic reagents, and materials science. However, most traditional stapled peptide preparation methods rely on prefunctionalizations, which limit the diversity of stapled peptides. Recently,… read more here.
Keywords: late stage; stage construction; stapled peptides; activation ... See more keywords
Bicyclic stapled peptides based on p53 as dual inhibitors for the interactions of p53 with MDM2 and MDMX
Sign Up to like & getrecommendations! Published in 2021 at "Chinese Chemical Letters"
DOI: 10.1016/j.cclet.2021.08.130
Abstract: ABSTRACT In recent years, the strategy of inhibiting the interactions of p53 with murine double minute 2 (MDM2) and murine double minute X (MDMX) has been proved to be a promising approach for tumor therapy.… read more here.
Keywords: mdm2 mdmx; stapled peptides; p53; bicyclic stapled ... See more keywords
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
Stapled Peptides as Direct Inhibitors of Nrf2-sMAF Transcription Factors.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c02037
Abstract: Nuclear factor erythroid-related 2-factor 2 (Nrf2) is a transcription factor traditionally thought of as a cellular protector. However, in many cancers, Nrf2 is constitutively activated and correlated with therapeutic resistance. Nrf2 heterodimerizes with small musculoaponeurotic… read more here.
Keywords: transcription; smaf transcription; peptides direct; transcription factors ... See more keywords
Importance of Net Hydrophobicity in the Cellular Uptake of All-Hydrocarbon Stapled Peptides.
Sign Up to like & getrecommendations! Published in 2018 at "Molecular pharmaceutics"
DOI: 10.1021/acs.molpharmaceut.7b01130
Abstract: All-hydrocarbon stapled peptides make up a promising class of protein-protein interaction regulators; their potential therapeutic benefit arises because they have a high binding affinity and specificity for intracellular molecules. The cell permeation efficacy of these… read more here.
Keywords: cellular uptake; hydrocarbon stapled; stapled peptides; hydrophobicity ... See more keywords
Conjugates of Aminoglycosides with Stapled Peptides as a Way to Target Antibiotic-Resistant Bacteria
Sign Up to like & getrecommendations! Published in 2023 at "ACS Omega"
DOI: 10.1021/acsomega.3c02071
Abstract: The misuse and overuse of antibiotics led to the development of bacterial resistance to existing aminoglycoside (AMG) antibiotics and limited their use. Consequently, there is a growing need to develop effective antimicrobials against multidrug-resistant bacteria.… read more here.
Keywords: peptides way; aminoglycosides stapled; conjugates aminoglycosides; resistant bacteria ... See more keywords
Design and synthesis of Nrf2-derived hydrocarbon stapled peptides for the disruption of protein-DNA-interactions
Sign Up to like & getrecommendations! Published in 2022 at "PLoS ONE"
DOI: 10.1371/journal.pone.0267651
Abstract: Misregulation and mutations of the transcription factor Nrf2 are involved in the development of a variety of human diseases. In this study, we employed the technology of stapled peptides to address a protein-DNA-complex and designed… read more here.
Keywords: design synthesis; dna; synthesis nrf2; protein dna ... See more keywords
Screening of Hydrocarbon-Stapled Peptides for Inhibition of Calcium-Triggered Exocytosis
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2022.891041
Abstract: The so-called primary interface between the SNARE complex and synaptotagmin-1 (Syt1) is essential for Ca2+-triggered neurotransmitter release in neuronal synapses. The interacting residues of the primary interface are conserved across different species for synaptotagmins (Syt1,… read more here.
Keywords: stapled peptides; primary interface; ca2; hydrocarbon stapled ... See more keywords