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 …

Overcoming endosomal entrapment in drug delivery

D Pei, M Buyanova - Bioconjugate chemistry, 2018 - ACS Publications
Intracellular delivery of biological agents such as peptides, proteins, and nucleic acids
generally rely on the endocytic pathway as the major uptake mechanism, resulting in their …

Discovery of Sulanemadlin (ALRN-6924), the first cell-permeating, stabilized α-helical peptide in clinical development

V Guerlavais, TK Sawyer, L Carvajal… - Journal of Medicinal …, 2023 - ACS Publications
We report the discovery of sulanemadlin (ALRN-6924), the first cell-permeating, stabilized α-
helical peptide to enter clinical trials. ALRN-6924 is a “stapled peptide” that mimics the N …

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 …

A gold mine for drug discovery: Strategies to develop cyclic peptides into therapies

X **g, K ** - Medicinal research reviews, 2020 - Wiley Online Library
As a versatile therapeutic modality, peptides attract much attention because of their great
binding affinity, low toxicity, and the capability of targeting traditionally “undruggable” protein …

Challenge to overcome current limitations of cell-penetrating peptides

GC Kim, DH Cheon, Y Lee - Biochimica et Biophysica Acta (BBA)-Proteins …, 2021 - Elsevier
The penetration of biological membranes is a prime obstacle for the delivery of
pharmaceutical drugs. Cell-penetrating peptide (CPP) is an efficient vehicle that can deliver …

Cyclic cell-penetrating peptides as efficient intracellular drug delivery tools

SE Park, MI Sajid, K Parang, RK Tiwari - Molecular pharmaceutics, 2019 - ACS Publications
Cyclic cell-penetrating peptides are relatively a newer class of peptides that have a huge
potential for the intracellular delivery of therapeutic agents aimed at treating challenging …

Macrocycles as protein–protein interaction inhibitors

PG Dougherty, Z Qian, D Pei - Biochemical Journal, 2017 - portlandpress.com
Macrocyclic compounds such as cyclic peptides have emerged as a new and exciting class
of drug candidates for inhibition of intracellular protein–protein interactions, which are …

Customized reversible stapling for selective delivery of bioactive peptides

Z Zeng, J Zhu, X Deng, H Chen, Y **… - Journal of the …, 2022 - ACS Publications
We have developed a new concept for reversible peptide stapling that involves
macrocyclization between two amino groups and decyclization promoted via dual 1, 4 …

Cell penetrating peptides in ocular drug delivery: State of the art

S Pescina, C Ostacolo, IM Gomez-Monterrey… - Journal of Controlled …, 2018 - Elsevier
Despite the increasing number of effective therapeutics for eye diseases, their treatment is
still challenging due to the presence of effective barriers protecting eye tissues. Cell …