Succinate drives macrophage inflammation by promoting GPR91 mitochondrial signaling in rheumatoid arthritis

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Authors: Wankang Zhang, Luping Wang, Yingjie Zhao, Yao Mu, Lei Qiu, Xinyu Feng, Yueye Wang, Jiemin Zhao, Yan Chang, Wei Wei, Xuezhi Yang
Cited by: 1
References: 36

Abstract

High succinate concentrations are implicated in rheumatoid arthritis (RA) and other inflammatory diseases through G protein–coupled receptor 91 (GPR91)–mediated signaling. Despite the therapeutic potential of targeting GPR91, conflicting reports on the receptor’s inflammatory roles have hindered treatment development. Here, we report that the effects of succinate on GPR91 signaling are biphasic and concentration dependent. At physiological succinate concentration, membrane-localized GPR91 promotes M2 polarization through G q -mediated activation of phospholipase C and intracellular calcium mobilization. In RA, elevated succinate induces GPR91 internalization and mitochondrial translocation, thereby disrupting G q signaling. Mechanistically, mitochondrial GPR91 recruits G s proteins and, together with intracellular succinate, activates the cyclic adenosine monophosphate (cAMP)–protein kinase A (PKA) pathway. PKA then phosphorylates cytidine/uridine monophosphate kinase 2 at serine-404, stabilizing it to enhance mitochondrial DNA (mtDNA) synthesis. Newly synthesized mtDNA is oxidized (forming ox-mtDNA) and released into the cytosol, activating the cyclic GMP-AMP synthase–stimulator of interferon genes pathway to drive macrophage inflammation. Myeloid-specific GPR91 deletion or inhibition of intracellular succinate accumulation alleviates arthritis in mice. This study reveals that GPR91 reprograms signaling by subcellular relocation, providing a promising therapeutic strategy for autoimmune diseases.

Fields of Study & Subjects

Immune cells in cancer Receptor Mechanisms and Signaling Protein Kinase Regulation and GTPase Signaling

Publication details

Journal / source
Science Translational Medicine
Publisher
American Association for the Advancement of Science (AAAS)
Volume
18
Issue
862
Pages
eaea8468–eaea8468
Publication date
12 August 2026
Language
EN