RNA display methods for the discovery of bioactive macrocycles

Y Huang, MM Wiedmann, H Suga - Chemical reviews, 2018 - ACS Publications
The past two decades have witnessed the emergence of macrocycles, including macrocyclic
peptides, as a promising yet underexploited class of de novo drug candidates. Both …

Directing evolution of novel ligands by mRNA display

G Kamalinia, BJ Grindel, TT Takahashi… - Chemical Society …, 2021 - pubs.rsc.org
mRNA display is a powerful biological display platform for the directed evolution of proteins
and peptides. mRNA display libraries covalently link the displayed peptide or protein …

Directing evolution: the next revolution in drug discovery?

AM Davis, AT Plowright, E Valeur - Nature Reviews Drug Discovery, 2017 - nature.com
The strong biological rationale to pursue challenging drug targets such as protein–protein
interactions has stimulated the development of novel screening strategies, such as DNA …

Directed evolution of cyclic peptides for inhibition of autophagy

JP Gray, MN Uddin, R Chaudhari, MN Sutton… - Chemical …, 2021 - pubs.rsc.org
In recent decades it has become increasingly clear that induction of autophagy plays an
important role in the development of treatment resistance and dormancy in many cancer …

Strategies for transitioning macrocyclic peptides to cell-permeable drug leads

LJ Walport, R Obexer, H Suga - Current opinion in biotechnology, 2017 - Elsevier
Highlights•Peptides are a highly versatile class of promising drug candidates.•Peptides can
be both passively and actively cell permeable.•It is now possible to develop cell permeable …

Macrocyclization of an all-d linear α-helical peptide imparts cellular permeability

S Kannan, PGA Aronica, S Ng, DTG Lian, Y Frosi… - Chemical …, 2020 - pubs.rsc.org
Peptide-based molecules hold great potential as targeted inhibitors of intracellular protein–
protein interactions (PPIs). Indeed, the vast diversity of chemical space conferred through …

Non-canonical amino acids in analyses of protease structure and function

P Goettig, NG Koch, N Budisa - International Journal of Molecular …, 2023 - mdpi.com
All known organisms encode 20 canonical amino acids by base triplets in the genetic code.
The cellular translational machinery produces proteins consisting mainly of these amino …

Directed evolution of PD-L1-targeted affibodies by mRNA display

BJ Grindel, BJ Engel, JN Ong… - ACS chemical …, 2022 - ACS Publications
Therapeutic monoclonal antibodies directed against PD-L1 (eg, atezolizumab) disrupt PD-
L1: PD-1 signaling and reactivate exhausted cytotoxic T-cells in the tumor compartment …

Bicyclic peptide library screening for the identification of Gαi protein modulators

A Pepanian, FA Binbay, S Roy… - Journal of Medicinal …, 2023 - ACS Publications
Noncanonical G protein activation and inactivation, particularly for the Gαi/s protein
subfamilies, have long been a focus of chemical research. Combinatorial libraries were …

Ultrahigh‐throughput screening system for directed polymer binding peptide evolution

L Apitius, K Rübsam, C Jakesch… - Biotechnology and …, 2019 - Wiley Online Library
Accumulation of plastics in the environment became a geological indicator of the
Anthropocene era. An effective reduction of long‐lasting plastics requires a treatment with …