Cationic Peptoids for Systemic In Vivo Cartilage-Targeting.

ABSTRACT: Although cartilage damage is key to the pathogenesis of many musculoskeletal diseases, including osteoarthritis and rheumatoid arthritis (RA), imaging and drug delivery to cartilage remain a demanding challenge. Cartilage is an avascular tissue with a dense matrix constraining the penetration of imaging and targeting agents. Here, a unique class of cationic peptidomimetics featuring peptoid residue Nlys (N-substituted butyl-amino glycine) is reported for cartilage targeting. Sulfo-Cyanine5 (Cy5) labeled Nlys-rich sequences are found to penetrate and be retained within millimeter-deep cartilage plugs in vitro by specific binding to the tissue's polyanionic glycosaminoglycan (GAG) chains. Owing to the unnatural sequences being undegradable by common proteases, these Nlys-peptidomimetics over

SUBMITTER: Zhang C 

PROVIDER: S-EPMC12631873 | biostudies-literature | 2025 Nov

REPOSITORIES: biostudies-literature