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Understanding cell penetration of cyclic peptides
Approximately 75% of all disease-relevant human proteins, including those involved in
intracellular protein–protein interactions (PPIs), are undruggable with the current drug …
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
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 …
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 …
for oral absorption and accessibility to intracellular tough targets. Here, starting with a drug …
Accurate de novo design of membrane-traversing macrocycles
We use computational design coupled with experimental characterization to systematically
investigate the design principles for macrocycle membrane permeability and oral …
investigate the design principles for macrocycle membrane permeability and oral …
An amide to thioamide substitution improves the permeability and bioavailability of macrocyclic peptides
Solvent shielding of the amide hydrogen bond donor (NH groups) through chemical
modification or conformational control has been successfully utilized to impart membrane …
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 …
challenge. This review discusses the most recent strategies used to develop cell permeable …
Strategies for fine-tuning the conformations of cyclic peptides
Cyclic peptides are promising scaffolds for drug development, attributable in part to their
increased conformational order compared to linear peptides. However, when optimizing the …
increased conformational order compared to linear peptides. However, when optimizing the …
Cyclosporin structure and permeability: from A to Z and beyond
Cyclosporins are natural or synthetic undecapeptides with a wide range of actual and
potential pharmaceutical applications. Several members of the cyclosporin compound family …
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 …
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 …
characteristics mainly regarding their pharmacokinetic behavior, including plasma stability …