Ginsenoside Rh2- functionalized liposomes enhanced BRD4-PROTAC delivery and antitumor efficacy <i>via</i> improved tumor targeting and ECM remodeling.

ABSTRACT: PROTAC technology leverages the ubiquitin-proteasome system to selectively degrade target proteins, presenting a novel strategy for anticancer therapy. ARV825, a BRD4-targeting PROTAC, exerts potent antitumor effects by degrading BRD4, thereby suppressing Bcl-2 and PD-L1 expression, inducing apoptosis, and enhancing T cell-mediated immunity. However, its clinical translation is hindered by poor solubility, low membrane permeability, and off-target effects. While conventional liposomes (lip) improved ARV825 delivery, their efficacy remained limited by insufficient tumor targeting and collagen-rich extracellular matrix (ECM) barriers that restricted T cell infiltration. To address these challenges, ginsenoside Rh2 (GRh2)-functioned liposomes (Gip) were developed by replacing cholesterol with

SUBMITTER: Wen L 

PROVIDER: S-EPMC12818118 | biostudies-literature | 2026 Feb

REPOSITORIES: biostudies-literature