AI Article Synopsis
- The development of bifunctional molecules for targeted RNA or protein manipulation is complex and time-consuming, requiring extensive optimization.
- A novel split-and-mix nanoplatform is introduced, which allows for easier screening and optimization of ligand ratios for various applications in biomolecule targeting.
- The potential of this platform is showcased through the successful use of SM-PROTACs to disrupt key intracellular targets, indicating its effectiveness and versatility in biomolecule regulation across multiple fields like epigenetics and gene editing.
Article Abstract
The development of bifunction al molecules, which can enable targeted RNA degradation, targeted protein acetylation, or targeted protein degradation, remains a time-consuming process that requires tedious optimization. We propose a split-and-mix nanoplatform that serves as a self-adjustable platform capable of facile screening, programmable ligand ratios, self-optimized biomolecule spatial recognition, and multifunctional applications. Herein, we demonstrate the potential of our proposed nanoplatform by showcasing proteolysis-targeting chimeras (PROTACs), namely, split-and-mix PROTAC (SM-PROTAC). We highlight the scope of our platform through the targeted disruption of intracellular therapeutic targets involving ERα, CDK4/6, AR, MEK1/2, BRD2/4, BCR-ABL, etc. These studies confirm the effectiveness and universality of the SM-PROTAC platform for proximity-induced applications. This platform is programmable, with significant potential applications to biomolecule regulation, including the fields of epigenetics, gene editing, and biomolecule modification regulation.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/jacs.2c12824 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!