Macrocyclic peptides as drug candidates: recent progress and remaining challenges

AA Vinogradov, Y Yin, H Suga - Journal of the American Chemical …, 2019 - ACS Publications
Peptides as a therapeutic modality attract much attention due to their synthetic accessibility,
high degree of specific binding, and the ability to target protein surfaces traditionally …

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 …

Orally absorbed cyclic peptides

DS Nielsen, NE Shepherd, W Xu, AJ Lucke… - Chemical …, 2017 - ACS Publications
Peptides and proteins are not orally bioavailable in mammals, although a few peptides are
intestinally absorbed in small amounts. Polypeptides are generally too large and polar to …

[HTML][HTML] From conception to development: investigating PROTACs features for improved cell permeability and successful protein degradation

C Cecchini, S Pannilunghi, S Tardy… - Frontiers in …, 2021 - frontiersin.org
Proteolysis Targeting Chimeras (PROTACs) are heterobifunctional degraders that
specifically eliminate targeted proteins by hijacking the ubiquitin-proteasome system (UPS) …

PROTAC degraders as chemical probes for studying target biology and target validation

V Němec, MP Schwalm, S Müller… - Chemical Society Reviews, 2022 - pubs.rsc.org
Small molecule degraders such as PROTACs (PROteolysis TArgeting Chimeras) have
emerged as new promising pharmacological modalities and the first PROTAC drug …

Beyond the rule of 5: lessons learned from AbbVie's drugs and compound collection: miniperspective

DA DeGoey, HJ Chen, PB Cox… - Journal of medicinal …, 2017 - ACS Publications
Recently, there has been an increasing focus on the pursuit of targets considered to be less
druggable that offer potential for development of promising new therapeutic agents for the …

[HTML][HTML] Systemic delivery of peptides by the oral route: Formulation and medicinal chemistry approaches

DJ Brayden, TA Hill, DP Fairlie, S Maher… - Advanced drug delivery …, 2020 - Elsevier
In its 33 years, ADDR has published regularly on the po5tential of oral delivery of biologics
especially peptides and proteins. In the intervening period, analysis of the preclinical and …

Cell-penetrating peptides: Design strategies beyond primary structure and amphipathicity

D Kalafatovic, E Giralt - molecules, 2017 - mdpi.com
Efficient intracellular drug delivery and target specificity are often hampered by the presence
of biological barriers. Thus, compounds that efficiently cross cell membranes are the key to …

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
Developing macrocyclic peptides that can reach intracellular targets is a significant
challenge. This review discusses the most recent strategies used to develop cell permeable …

The experimental power of FR900359 to study Gq-regulated biological processes

R Schrage, AL Schmitz, E Gaffal, S Annala… - Nature …, 2015 - nature.com
Despite the discovery of heterotrimeric αβγ G proteins∼ 25 years ago, their selective
perturbation by cell-permeable inhibitors remains a fundamental challenge. Here we report …