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 …
Overcoming endosomal entrapment in drug delivery
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 …
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 …
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
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 …
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 …
binding affinity, low toxicity, and the capability of targeting traditionally “undruggable” protein …
Challenge to overcome current limitations of cell-penetrating peptides
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 …
pharmaceutical drugs. Cell-penetrating peptide (CPP) is an efficient vehicle that can deliver …
Cyclic cell-penetrating peptides as efficient intracellular drug delivery tools
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 …
potential for the intracellular delivery of therapeutic agents aimed at treating challenging …
Macrocycles as protein–protein interaction inhibitors
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 …
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 …
macrocyclization between two amino groups and decyclization promoted via dual 1, 4 …
Cell penetrating peptides in ocular drug delivery: State of the art
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 …
still challenging due to the presence of effective barriers protecting eye tissues. Cell …