Stapled helical peptides bearing different anchoring residues

X Li, S Chen, WD Zhang, HG Hu - Chemical Reviews, 2020 - ACS Publications
A large proportion of protein–protein interactions (PPIs) occur between a short peptide and a
globular protein domain; the peptides involved in surface interactions play important roles …

Macrocyclization strategies for cyclic peptides and peptidomimetics

C Bechtler, C Lamers - RSC Medicinal Chemistry, 2021 - pubs.rsc.org
Peptides are a growing therapeutic class due to their unique spatial characteristics that can
target traditionally “undruggable” protein–protein interactions and surfaces. Despite their …

Multicomponent reaction toolbox for peptide macrocyclization and stapling

L Reguera, DG Rivera - Chemical reviews, 2019 - ACS Publications
In the past decade, multicomponent reactions have experienced a renaissance as powerful
peptide macrocyclization tools enabling the rapid creation of skeletal complexity and …

A gold mine for drug discovery: Strategies to develop cyclic peptides into therapies

X Jing, K Jin - Medicinal research reviews, 2020 - Wiley Online Library
As a versatile therapeutic modality, peptides attract much attention because of their great
binding affinity, low toxicity, and the capability of targeting traditionally “undruggable” protein …

Multicomponent reactions in ligation and bioconjugation chemistry

L Reguera, Y Méndez, AR Humpierre… - Accounts of Chemical …, 2018 - ACS Publications
Conspectus Multicomponent reactions (MCRs) encompass an exciting class of chemical
transformations that have proven success in almost all fields of synthetic organic chemistry …

Construction of complex macromulticyclic peptides via stitching with formaldehyde and guanidine

B Li, Z Wan, H Zheng, S Cai, HW Tian… - Journal of the …, 2022 - ACS Publications
There is a growing interest in constructing multicyclic peptide structures to expand the
chemical space of peptides. Conventional strategies for constructing large peptide structures …

Chemical conjugation in drug delivery systems

A Eras, D Castillo, M Suárez, NS Vispo… - Frontiers in …, 2022 - frontiersin.org
Cancer is one of the diseases with the highest mortality rate. Treatments to mitigate cancer
are usually so intense and invasive that they weaken the patient to cure as dangerous as the …

Introducing the petasis reaction for late‐stage multicomponent diversification, labeling, and stapling of peptides

MG Ricardo, D Llanes, LA Wessjohann… - Angewandte Chemie …, 2019 - Wiley Online Library
For the first time, the Petasis (borono‐Mannich) reaction is employed for the multicomponent
labeling and stapling of peptides. The report includes the solid‐phase derivatization of …

A multicomponent stapling approach to exocyclic functionalized helical peptides: adding lipids, sugars, PEGs, labels, and handles to the lactam bridge

AV Vasco, Y Méndez, A Porzel, J Balbach… - Bioconjugate …, 2018 - ACS Publications
Peptide stapling is traditionally used to lock peptide conformations into α-helical structures
using a variety of macrocyclization chemistries. In an endeavor to add a diversity-generating …

Multicomponent polysaccharide–protein bioconjugation in the development of antibacterial glycoconjugate vaccine candidates

Y Méndez, J Chang, AR Humpierre, A Zanuy… - Chemical …, 2018 - pubs.rsc.org
A new synthetic strategy for the development of multivalent antibacterial glycoconjugate
vaccines is described. The approach comprises the utilization of an isocyanide-based …