Marine Bromophenol Derivatives as a Novel Class of Potent Small-Molecule STING Agonists.

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Main Authors: Tang, Manqing, Guo, Qiuhui, Wang, Ping, Li, Yunfei, Jiang, Bo
Format: Artículo científico
Language:en
Published: Current issues in molecular biology 2026
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author Tang, Manqing
Guo, Qiuhui
Wang, Ping
Li, Yunfei
Jiang, Bo
author_facet Tang, Manqing
Guo, Qiuhui
Wang, Ping
Li, Yunfei
Jiang, Bo
Tang, Manqing
Guo, Qiuhui
Wang, Ping
Li, Yunfei
Jiang, Bo
collection PubMed - marine biology
contents Marine Bromophenol Derivatives as a Novel Class of Potent Small-Molecule STING Agonists. Tang, Manqing Guo, Qiuhui Wang, Ping Li, Yunfei Jiang, Bo Activation of the stimulator of interferon genes (STING) pathway has emerged as a promising strategy for cancer immunotherapy. However, the initial cyclic dinucleotide (CDN) analogs developed as STING agonists have shown limited efficacy in clinical trials, prompting interest in non-CDN small-molecule alternatives. In this study, we identified a novel series of bromophenol derivatives as effective STING agonists. Among these derivatives, OSBP63 robustly activated the STING signaling pathway, resulting in enhanced phosphorylation of interferon regulatory factor 3 (p-IRF3) and increased secretion of interferon-β (IFN-β). Co-administration of Marine Bromophenol Derivative (OSBP63) with paclitaxel (PTX), a conventional anticancer drug, significantly suppressed B-cell lymphoma-2 (BCL-2) expression and protein kinase B (AKT) phosphorylation, thereby demonstrating pronounced anti-tumor activity in a mouse model of breast cancer. These findings suggest that OSBP63 represents a promising non-CDN small-molecule STING agonist candidate, offering a valuable lead for future anticancer therapeutic development.
format Artículo científico
id pubmed_41614892
institution PubMed
language en
publishDate 2026
publisher Current issues in molecular biology
record_format pubmed
spellingShingle Marine Bromophenol Derivatives as a Novel Class of Potent Small-Molecule STING Agonists.
Tang, Manqing
Guo, Qiuhui
Wang, Ping
Li, Yunfei
Jiang, Bo
Marine Bromophenol Derivatives as a Novel Class of Potent Small-Molecule STING Agonists. Tang, Manqing Guo, Qiuhui Wang, Ping Li, Yunfei Jiang, Bo Activation of the stimulator of interferon genes (STING) pathway has emerged as a promising strategy for cancer immunotherapy. However, the initial cyclic dinucleotide (CDN) analogs developed as STING agonists have shown limited efficacy in clinical trials, prompting interest in non-CDN small-molecule alternatives. In this study, we identified a novel series of bromophenol derivatives as effective STING agonists. Among these derivatives, OSBP63 robustly activated the STING signaling pathway, resulting in enhanced phosphorylation of interferon regulatory factor 3 (p-IRF3) and increased secretion of interferon-β (IFN-β). Co-administration of Marine Bromophenol Derivative (OSBP63) with paclitaxel (PTX), a conventional anticancer drug, significantly suppressed B-cell lymphoma-2 (BCL-2) expression and protein kinase B (AKT) phosphorylation, thereby demonstrating pronounced anti-tumor activity in a mouse model of breast cancer. These findings suggest that OSBP63 represents a promising non-CDN small-molecule STING agonist candidate, offering a valuable lead for future anticancer therapeutic development.
title Marine Bromophenol Derivatives as a Novel Class of Potent Small-Molecule STING Agonists.
url https://pubmed.ncbi.nlm.nih.gov/41614892/