Selection of Nucleotide-Encoded Mass Libraries of Macrocyclic Peptides for Inaccessible Drug Targets

K Colas, D Bindl, H Suga - Chemical Reviews, 2024 - ACS Publications
Technological advances and breakthrough developments in the pharmaceutical field are
knocking at the door of the “undruggable” fortress with increasing insistence. Notably, the …

Systematic targeting of protein–protein interactions

AE Modell, SL Blosser, PS Arora - Trends in pharmacological sciences, 2016 - cell.com
Over the past decade, protein–protein interactions (PPIs) have gone from being neglected
as 'undruggable'to being considered attractive targets for the development of therapeutics …

Stapled peptide design: principles and roles of computation

YS Tan, DP Lane, CS Verma - Drug Discovery Today, 2016 - Elsevier
Highlights•One of the most widely adopted strategies for α-helix stabilisation is peptide
stapling.•Stapled peptides are highly promising therapeutic agents.•General design …

A protein tertiary structure mimetic modulator of the Hippo signalling pathway

H Adihou, R Gopalakrishnan, T Förster… - Nature …, 2020 - nature.com
Transcription factors are key protein effectors in the regulation of gene transcription, and in
many cases their activity is regulated via a complex network of protein–protein interactions …

DNA-Mediated Peptide Assembly into Protein Mimics

F Zhao, M Frandsen, S Capodaglio… - Journal of the American …, 2024 - ACS Publications
The design of new protein structures is challenging due to their vast sequence space and
the complexity of protein folding. Here, we report a new modular DNA-templated strategy to …

Protein domain mimics as modulators of protein–protein interactions

N Sawyer, AM Watkins, PS Arora - Accounts of chemical research, 2017 - ACS Publications
Conspectus Protein–protein interactions (PPIs) are ubiquitous in biological systems and
often misregulated in disease. As such, specific PPI modulators are desirable to unravel …

Bent into shape: Folded peptides to mimic protein structure and modulate protein function

HI Merritt, N Sawyer, PS Arora - Peptide Science, 2020 - Wiley Online Library
Protein secondary and tertiary structure mimics have served as model systems to probe
biophysical parameters that guide protein folding and as attractive reagents to modulate …

A dimeric proteomimetic prevents SARS-CoV-2 infection by dimerizing the spike protein

B Khatri, I Pramanick, SK Malladi, RS Rajmani… - Nature Chemical …, 2022 - nature.com
Protein tertiary structure mimetics are valuable tools to target large protein–protein
interaction interfaces. Here, we demonstrate a strategy for designing dimeric helix-hairpin …

A Sos proteomimetic as a pan-Ras inhibitor

SH Hong, DY Yoo, L Conway… - Proceedings of the …, 2021 - National Acad Sciences
Aberrant Ras signaling is linked to a wide spectrum of hyperproliferative diseases, and
components of the signaling pathway, including Ras, have been the subject of intense and …

De novo design of covalently constrained mesosize protein scaffolds with unique tertiary structures

B Dang, H Wu, VK Mulligan, M Mravic… - Proceedings of the …, 2017 - National Acad Sciences
The folding of natural proteins typically relies on hydrophobic packing, metal binding, or
disulfide bond formation in the protein core. Alternatively, a 3D structure can be defined by …