Small Activating RNA Modulation of the G Protein‐Coupled Receptor for Cancer Treatment (Adv. Sci. 26/2022)

Abstract

Small Activating RNA Modulation In article number 2200562, Ling Peng, Leo Tsz On Lee, and co‐workers, report for the first time that small activating RNA (saRNA) delivered by amphiphilic dendrimer can effectively modulate a G protein‐coupled receptors (GPCR), Mas receptor, for cancer treatment. This project provides not only a new strategy for cancer therapy, but also a new avenue to address undruggable GPCRs.

A PD‐L1 Antibody‐Conjugated PAMAM Dendrimer Nanosystem for Simultaneously Inhibiting Glycolysis and Promoting Immune Response in Fighting Breast Cancer

“…effective vector for siRNA delivery and gene knockdown in various cells, including cancer cells, stems cells, and primary immune cells, as well as in animal models of different diseases. [25][26][27][28] AD can complex siRNA molecules into small and uniform nanoparticles that protect them from degradation and promote cell uptake. In the present work, we employed AD for siPDK1 delivery.…”

“…Recently, we developed amphiphilic dendrimers as precision vectors for siRNA delivery by virtue of their well-defined dendritic structure and cooperative multivalence. [23][24][25][26][27][28] These amphiphilic dendrimers also boast combined delivery advantages of both lipid and polymer vectors, the two most advanced vectors for siRNA delivery. Notably, cationic amphiphilic dendrimers strongly bind to negatively charged siRNAs, forming stable nanoparticles that protect the RNA molecules from degradation and prolong its half-life, leading to enhanced siRNA accumulation in tumor lesions via the enhanced permeation and retention (EPR) effect, also known as passive tumor targeting.…”