2. Academic Validation
  3. Marine Bromophenol Derivatives as a Novel Class of Potent Small-Molecule STING Agonists

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

  • Curr Issues Mol Biol. 2026 Jan 5;48(1):61. doi: 10.3390/cimb48010061.
Manqing Tang 1,  Qiuhui Guo 1,  Ping Wang 1,  Yunfei Li 1,  Bo Jiang 2 3
Affiliations

Affiliations

  • 1 College of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China.
  • 2 Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences, Qingdao 266000, China.
  • 3 Nantong Zhong Ke Marine Science and Technology R&D Center, Nantong 226000, China.
PMID: 41614892 DOI: 10.3390/cimb48010061
Abstract

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.

Keywords

STING agonists; bromophenol derivatives; cancer immunotherapy.

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