2. Academic Validation
  3. Theranostic Rhenium(I)-Based ER-Phagy Retardant Promotes Immunogenic Cell Death

Theranostic Rhenium(I)-Based ER-Phagy Retardant Promotes Immunogenic Cell Death

  • J Med Chem. 2025 Jan 9;68(1):338-347. doi: 10.1021/acs.jmedchem.4c01948.
Liang Hao 1 2,  Yu-Yi Ling 1,  Jie Wang 1,  Qing-Hua Shen 1,  Zhi-Yuan Li 1,  Cai-Ping Tan 1 3
Affiliations

Affiliations

  • 1 MOE Key Laboratory of Bioinorganic and Synthetic Chemistry, School of Chemistry, Sun Yat-Sen University, Guangzhou 510006, P. R. China.
  • 2 The Marine Biomedical Research Institute of Guangdong Zhanjiang, School of Ocean and Tropical Medicine, Guangdong Medical University, Zhanjiang, Guangdong 524023, P. R. China.
  • 3 Guangdong Basic Research Center of Excellence for Functional Molecular Engineering, Guangzhou 510006, P. R. China.
PMID: 39720929 DOI: 10.1021/acs.jmedchem.4c01948
Abstract

ER-phagy is a double-edged sword in the occurrence, development, and treatment of cancer; especially, its functions in immunotherapy are still unknown. In this work, we designed a theranostic Re complex (Re1) containing a BODIPY-derived ligand and a β-carboline ligand to target the endoplasmic reticulum (ER) and block ER-phagy at the late stages. Interestingly, as validated both in vitro and in vivo, ER-phagy blockage greatly enhances the capability of Re1 to induce immunogenic cell death (ICD). In summary, we dexterously fused two molecular modules for ER targeting and ER-phagy blockage into a coordination complex to afford a highly effective ICD inducer, which provides clues for designing new Cancer immunotherapeutics.

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