Highly efficient and long-acting split-and-mix proteolysis targeting chimera based on self-assembled polylactic acid.

ABSTRACT: Proteolysis targeting chimera (PROTAC) technology has received extensive attention due to its "event-driven" mechanism of action. However, existing chimera molecules tend to have higher molecular weight and higher polar surface area and exhibit lower druggable properties. In order to effectively improve the bioavailability, circulation time and other proprietary drug parameters of "chimera molecules", we combine the characteristics of nanotechnology and chimera technology, and propose the strategy of "Split-and-Mix" proteolysis degradation (SM-PROTAC) technology. However, both peptide- and liposome-based SM-PROTAC showed suboptimal in vivo efficiency. Hence, in this study, we incorporated Polylactic acid (PLA), an FDA-approved biomedical material, as the self-assembled matrix for SM-PROTAC

SUBMITTER: Zhan MM 

PROVIDER: S-EPMC12658001 | biostudies-literature | 2025 Nov

REPOSITORIES: biostudies-literature