Sona Krajcovicova

May 10, 2024 | onlinelibrary.wiley.com | Sona Krajcovicova

Introduction The advancements in peptide-based therapeutics, in order to improve the often-poor pharmacokinetic limitations of peptides, have seen a significant growth in the last decade. One of the driving forces for these advancements was peptide macrocyclisation, also known as a peptide stapling.

May 10, 2024 | chemistry-europe.onlinelibrary.wiley.com | Sona Krajcovicova

This Concept short review offers an insightful analysis of pivotal research papers and explores the key synthetic ideas behind the intersection of two realms in peptide chemistry: using tryptophan and Petasis multicomponent reactions for macrocyclisation and labelling of peptides.

Dec 6, 2023 | pubs.rsc.org | Jack Sydenham |Lensfield Road |Hikaru Seki |Sona Krajcovicova

Site-selective peptide functionalisation mediated via vinyl-triazine linchpins† Herein we introduce 3-vinyl-1,2,4-triazines derivatives as dual-reactive linkers that exhibit selectivity towards cysteine and specific strained alkynes, enabling conjugate addition and inverse electron-demand Diels–Alder (IEDDA) reactions.

Sep 20, 2023 | pubs.rsc.org | Jessica Iegre |Lensfield Road |Sona Krajcovicova |Anders Gunnarsson

A cell-active cyclic peptide targeting the Nrf2/Keap1 protein–protein interaction† The disruption of the protein–protein interaction (PPI) between Nrf2 and Keap1 is an attractive strategy to counteract the oxidative stress that characterises a variety of severe diseases. Peptides represent a complementary approach to small molecules for the inhibition of this therapeutically important PPI.

Jun 30, 2023 | onlinelibrary.wiley.com | Sona Krajcovicova |David R Spring

Graphical Abstract Two-component peptide stapling is an appealing method for preparing enzymatically stable peptides with incorporated biologically relevant tags. An unprecedented approach, utilising the tryptophan-mediated multicomponent Petasis reaction (TMPR), facilitates the generation of stapled peptides and enables their late-stage functionalisation. A variety of examples are presented to highlight the advantages of the method.