cGAS-STING Targeting Offers Novel Therapeutic Opportunities in Liver Diseases

  • Drug Des Devel Ther. 2025 Jul 9:19:5835-5853. doi: 10.2147/DDDT.S521397.
Yumin Wang  #  1 Rui Yang  #  1 Yuwei Cao  #  1 Yulin Li  1 Yonglin Zhu  1 Zhe Zhang  1 Joshua S Fleishman  2 Jichao Chen  1 Mingchao Ding  3
Affiliations
  • 1. Department of Respiratory and Critical Care Medicine, Aerospace Center Hospital, Peking University Aerospace School of Clinical Medicine, Beijing, 100049, People's Republic of China.
  • 2. Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, NY, 11439, USA.
  • 3. Department of Peripheral Vascular Intervention, Aerospace Center Hospital, Peking University Aerospace School of Clinical Medicine, Beijing, 100049, People's Republic of China.
  • # Contributed equally.
Abstract

Cyclic GMP/AMP (cGAMP) synthase (cGAS), coupled with the endoplasmic reticulum (ER)-anchored adaptor protein stimulator of interferon genes (STING), constitute key components of the type 1 interferon signaling network. cGAS detects both pathogen-derived DNA and aberrant cytosolic self-DNA, establishing the cGAS-STING pathway as a central player in autoimmune disorders, sterile inflammation, and senescence-related processes. However, sustained abnormal activation of this signaling axis is implicated in the pathogenesis of chronic inflammatory and autoimmune conditions. Recent studies have uncovered the pivotal role of cGAS-STING signaling in driving inflammation-associated pathologies, particularly hepatic disorders. Advances in understanding the molecular dynamics of this pathway have facilitated the development of targeted small-molecule inhibitors with therapeutic potential for cGAS-STING-driven liver diseases. In this review, we first delineate the core architecture of the cGAS-STING signaling cascade. Building on this framework, we analyze emerging evidence elucidating the mechanistic contributions of cGAS-STING activation to hepatic pathophysiology. Subsequently, we catalog pharmacologically active compounds capable of modulating this pathway in liver disease models. Finally, we critically evaluate current challenges in translating cGAS-STING-targeted therapies and propose strategic approaches to address these limitations. This synthesis underscores innovative therapeutic opportunities arising from precision modulation of the cGAS-STING axis in liver diseases.

Keywords
STING; antagonist; cGAS; liver diseases.
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