Understanding cell penetration of cyclic peptides

PG Dougherty, A Sahni, D Pei - Chemical Reviews, 2019 - ACS Publications
Approximately 75% of all disease-relevant human proteins, including those involved in
intracellular protein–protein interactions (PPIs), are undruggable with the current drug …

Multiscale simulations of biological membranes: the challenge to understand biological phenomena in a living substance

G Enkavi, M Javanainen, W Kulig, T Róg… - Chemical …, 2019 - ACS Publications
Biological membranes are tricky to investigate. They are complex in terms of molecular
composition and structure, functional over a wide range of time scales, and characterized by …

Development of orally bioavailable peptides targeting an intracellular protein: from a hit to a clinical KRAS inhibitor

M Tanada, M Tamiya, A Matsuo… - Journal of the …, 2023 - ACS Publications
Cyclic peptides as a therapeutic modality are attracting a lot of attention due to their potential
for oral absorption and accessibility to intracellular tough targets. Here, starting with a drug …

Accurate de novo design of membrane-traversing macrocycles

G Bhardwaj, J O'Connor, S Rettie, YH Huang… - Cell, 2022 - cell.com
We use computational design coupled with experimental characterization to systematically
investigate the design principles for macrocycle membrane permeability and oral …

An amide to thioamide substitution improves the permeability and bioavailability of macrocyclic peptides

P Ghosh, N Raj, H Verma, M Patel… - Nature …, 2023 - nature.com
Solvent shielding of the amide hydrogen bond donor (NH groups) through chemical
modification or conformational control has been successfully utilized to impart membrane …

Cyclic peptides as drugs for intracellular targets: the next frontier in peptide therapeutic development

LK Buckton, MN Rahimi… - Chemistry–A European …, 2021 - Wiley Online Library
Develo** macrocyclic peptides that can reach intracellular targets is a significant
challenge. This review discusses the most recent strategies used to develop cell permeable …

Strategies for fine-tuning the conformations of cyclic peptides

R Jwad, D Weissberger, L Hunter - Chemical Reviews, 2020 - ACS Publications
Cyclic peptides are promising scaffolds for drug development, attributable in part to their
increased conformational order compared to linear peptides. However, when optimizing the …

Cyclosporin structure and permeability: from A to Z and beyond

KM Corbett, L Ford, DB Warren… - Journal of Medicinal …, 2021 - ACS Publications
Cyclosporins are natural or synthetic undecapeptides with a wide range of actual and
potential pharmaceutical applications. Several members of the cyclosporin compound family …

Cyclic Peptide Screening Methods for Preclinical Drug Discovery: Miniperspective

X Li, TW Craven, PM Levine - Journal of Medicinal Chemistry, 2022 - ACS Publications
Cyclic peptides are among the most diverse architectures for current drug discovery efforts.
Their size, stability, and ease of synthesis provide attractive scaffolds to engage and …

Overcoming the shortcomings of peptide-based therapeutics

C Lamers - Future Drug Discovery, 2022 - Taylor & Francis
Peptides have traditionally been perceived as poor drug candidates due to unfavorable
characteristics mainly regarding their pharmacokinetic behavior, including plasma stability …