An orally available non-nucleotide STING agonist with antitumor activity

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1. Additional file 12 of Combination of oral STING agonist MSA-2 and anti-TGF-β/PD-L1 bispecific antibody YM101: a novel immune cocktail therapy for non-inflamed tumors
   Yi, Ming, Mengke Niu, Yuze Wu, Ge, Hong, Jiao, Dechao, Zhu, Shuangli, Jing Zhang, Yongxiang Yan, Zhou, Pengfei, Chu, Qian et al. · 2022 · Figshare
2. Additional file 8 of Combination of oral STING agonist MSA-2 and anti-TGF-β/PD-L1 bispecific antibody YM101: a novel immune cocktail therapy for non-inflamed tumors
   Yi, Ming, Mengke Niu, Yuze Wu, Ge, Hong, Jiao, Dechao, Zhu, Shuangli, Jing Zhang, Yongxiang Yan, Pengfei Zhou, Chu, Qian et al. · 2022 · Figshare
3. Additional file 7 of Combination of oral STING agonist MSA-2 and anti-TGF-β/PD-L1 bispecific antibody YM101: a novel immune cocktail therapy for non-inflamed tumors
   Yi, Ming, Mengke Niu, Yuze Wu, Ge, Hong, Jiao, Dechao, Zhu, Shuangli, Jing Zhang, Yongxiang Yan, Pengfei Zhou, Qian Chu et al. · 2022 · Figshare
4. Additional file 11 of Combination of oral STING agonist MSA-2 and anti-TGF-β/PD-L1 bispecific antibody YM101: a novel immune cocktail therapy for non-inflamed tumors
   Ming Yi, Mengke Niu, Yuze Wu, Ge, Hong, Jiao, Dechao, Zhu, Shuangli, Jing Zhang, Yongxiang Yan, Pengfei Zhou, Chu, Qian et al. · 2022 · Figshare
5. Pirenzepine exhibits anti-prostate cancer activity and enhances checkpoint inhibitor-based immunotherapy by targeting STING
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6. Simple Hydrophobic Modification of bPEI Confers Potent, STING-Dependent Innate Immunostimulatory Activity
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7. Marine Bromophenol Derivatives as a Novel Class of Potent Small-Molecule STING Agonists
   Manqing Tang, Qiuhui Guo, Ping Wang, Yunfei Li, Bo Jiang · 2026 · Current Issues in Molecular Biology
8. Halogen-methyl hybridization unlocks orally bioavailable STING agonist for tumor immunotherapy
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9. Simultaneous activation of apoptosis and cGAS-STING pathway with a mitochondria-targeted dehydrocholic acid compound for enhanced hepatocellular carcinoma chemoimmunotherapy
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10. A Chemoenzymatic Synthesis of STING Agonist MK-2118
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11. Development of 68Ga-labeled macrocyclic peptide for targeting stimulator of interferon genes
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12. Mechanisms of topical Mahoniae Caulis against acute mastitis: Integrating SMR, network pharmacology, molecular docking, and experimental validation
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13. A NIR-Ⅱ-Immunostimulatory nanoplatform rewires immunometabolism to unleash STING-driven antitumor immunity
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14. Albumin‐Bound STING Agonist Reprograms HSPCs to Antitumor Neutrophils Enhancing CD8 + T Cell Immunity
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15. An exosome-inspired docetaxel prodrug nanoplatform for potent STING activation and synergistic chemoimmunotherapy
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16. Preclinical efficacy of a systemically-administered, second-generation STING agonist that promotes antitumour immunity in combination with radiotherapy
    Malin Pedersen, Lisa C. Hubbard, Shane Foo, Anton Patrikeev, Antonio Rullan, Holly Baldock, Christian Mandl, Paolo Chetta, Jehanne Hassan, Isaac Dean et al. · 2026 · bioRxiv (Cold Spring Harbor Laboratory)
17. Assembled DNA Nanostructure to Precisely Induced cGAS‐STING Activation for Cancer Immunotherapy
    Li He, Yu Zhang, Shujuan Cao, Shixu Kou, Sen Li, Jian Jin, Zhaoqi Yang, Teng Wang · 2026 · Advanced Healthcare Materials
18. Ultrasound-activated in situ nano-vaccines (SATNAV) for precise CRPC sono-immunotherapy via multi-reprograming the immunosuppressive microenvironment
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19. DNA Damage Response and Immune Checkpoint: Recent Advances in Basic Science
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20. Peptide Coacervates Promote Cytosolic Delivery of STING Agonists for Cancer Immunotherapy
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21. Identification of cGAS-like receptors and characterization of STING mediated NF-κB activation in Drosophila melanogaster
    Kasper Grønbjerg Winther · 2024 · theses.fr (ABES)
22. Contribution of the DNA sensing pathway STING in neutrophilic allergic asthma exacerbation
    Yasmine Messaoud-Nacer · 2023
23. Photoactivatable Cascade DNAzyme Nanomachines for Amplified Imaging of Tumor Response to STING-Activated Immunotherapy
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25. BBB-penetrating biomimetic nanoparticles orchestrate STING activation and metabolic immunomodulation for potent glioma immunotherapy
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26. MoB MBene Based Nanoplatform for Enhanced Cancer Immunotherapy via cGAS Demethylation and Hypoxia Reversion
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27. Betrixaban activates cGAS-STING to promote antitumor immunity without pathological inflammation
    Y Q Zhao, Xingyu Chen, LiRui Tang, Hanjie Liu, Boming Kang, Shuailong Zheng, Songying Ouyang, Y D Xie, Fuping You · 2026 · EMBO Molecular Medicine
28. Costimulatory biomarker-specific CD28 PET for early prediction of the response to PD-1 blockade in lung cancer
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29. The Emerging Role of Nanocarrier-Based Delivery Systems for cGAS-STING Activation in Cancer Immunotherapy
    Guanxiong Zhu, D Li, Hongru Zhang, Jingyuan Wang, Xinyi Li, Liting Zeng, L Zhang, Lina Yu · 2026 · International Journal of Nanomedicine
30. Control of poorly immunogenic tumors with systemic STING agonist‐loaded liposomes targeting cross‐presenting dendritic cells
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31. Construction of Coumarin‐Conjugated Macromolecular Probe for Photoactivatable Bioimaging
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32. A neutrophil-tumor cascade-targeting Trojan horse for heterobifunctional prodrug delivery to enhance cGAS-STING cancer immunotherapy
    Huamiao Zhang, Yang Li, Qiuchen Bi, Heping Zhu, H Wang, Zhangyi Wang, Zhangqiang Ma, Huiping Liu, Xiaoling Zhu, Jiaqi Cao et al. · 2026 · Journal of Nanobiotechnology
33. Biomimetic self-assembled copper nanoadjuvant potentiates hepatocellular carcinoma immunotherapy via cuproptosis-driven cGAS-STING activation
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34. Discovery of MK-2118, a Small-Molecule Agonist of STING
    Timothy Henderson, Michael D. Altman, Alexei V. Buevich, Brandon Cash, Sašo Čemerski, Wonsuk Chang, Yiping Chen, Matthew Childers, Jared N. Cumming, Peter J. Dandliker et al. · 2026 · ACS Medicinal Chemistry Letters
35. Discovery of FAP-Targeted Platinum(IV)-Esterified STING Agonist as Small-Molecule Dual Prodrug Conjugates for Tumor-Specific Metalloimmunotherapy
    Ende He, J Sun, Zhengyuan Wang, Yiming Fan, Zilan Song, Ao Zhang, Chunyong Ding · 2026 · JACS Au
36. Activation-induced SLC7A1 expression enhances T cell sensitivity to cGAMP-mediated STING signaling
    Valentino Sudaryo, Dayanne R. Carvalho, Jacqueline A. Carozza, Xujun Cao, Courtney Kernick, Anthony F. Cordova, J. Michelle Lee, Theodore L. Roth, Lingyin Li · 2026 · Cell Reports
37. Tumor-responsive nanoparticles precisely overcome hypoxia-mediated STING dysfunction to unleash potent antitumor immunity
    Linna Hai, Junfeng Wang, Liu D, Kaiqing Yun, Kongshuo Ma, Yuxuan Peng, Mengdi Xu, Xinbo Ma, Shan Gao, Qin Wang et al. · 2026 · Acta Pharmaceutica Sinica B
38. Self-assembled supramolecular nanoparticles of α-mangostin for targeted STING activation and enhanced tumor immunotherapy
    Jiaqian Miao, Yanjie Liu, Sisi Chen, Yi Zhou, Jun Liu, Danni Xu, Xuan Mo, Junjie Wang, Qianli Zhu, Chunyang Yu et al. · 2026 · Acta Pharmaceutica Sinica B
39. Comparative characteristics of pharmaceutical substances activators of the STING signaling pathway
    S. D. Shceglov, M. Dmitrieva, A. P. Kolpaksidi, Ya. Sadovskaya, A. Karimova, O. Solopova, D. Gusev, Zh. M. Kozlova · 2026 · Farmaciya (Pharmacy)
40. Engineered Lipid Nanoparticles with Promoted Endosomal Escape and R283S-Mediated Stimulator of Interferon Genes (STING) Activation for Pancreatic Cancer Immunotherapy
    Sizhen Wang, Qiwei Tai, Kehui Wang, Jianyu Zheng, Beibei Guo, Feng Hua Yang, C Wang · 2026 · Pharmaceutics
41. Platinum‐Based Strategies for cGAS‐STING Activation: From Molecular Design to Nanomedicine
    Yang Sun, Shuo Shi · 2026 · Advanced Functional Materials
42. Targeting innate immunity to overcome immune evasion in HPV-associated cancers
    Xianguang Bai, Hongmei Dai, Zebao Lu, S J Yu · 2026 · Frontiers in Cellular and Infection Microbiology
43. STING agonists in tumor therapy: structural pharmacology, determinants of productive activation, and barrier-matched therapeutic strategies
    Can Li, Lanxiang Wu · 2026 · Biochemical Pharmacology
44. Discovery of a novel STING-binding peptide associated with reduced cGAMP-induced inflammatory gene expression
    Junling Lu, Rui Dong, Shudan Yang, Xinyu Yuan, Gang Wang, Jun Wang · 2026 · Journal of Enzyme Inhibition and Medicinal Chemistry
45. Leveraging Mitochondria‐Endoplasmic Reticulum Functional Interplay With an On‐Demand Nanoparticle to Boost mtDNA‐Based STING Immunotherapy
    Han Chen, Haijing Qu, Yuqing Pan, Wei Cheng, Jianmin Wu, Ning Wang, Jiaqi Shen, Meng W, Zejian Wang, Xiangdong Xue · 2026 · Advanced Materials
46. Delivery systems of STING agonists for the immunotherapy of malignant neoplasms
    S. D. Shceglov, Yana O. Sadovskaya, Anastasia O. Karimova, О. Н. Солопова, Zh. M. Kozlova · 2026 · Russian Journal of Biotherapy
47. An Insight into the cGAS–STING Pathway Modulation by Metal Complexes to Initiate Immunogenic Cell Death in Cancer
    Shilpendu Ghosh, Sujato Mukherjee, Arindam Mukherjee · 2026 · Journal of Medicinal Chemistry
48. STING agonist profiling by nucleotide library defines structural determinants of cyclic dinucleotide recognition
    Indra Bekere, Yuliia Hubarzhevska, Sabrina V. Egender, Patrick K. Quoika, Rupert Öllinger, Marie Rose Schrimpf, Roland Rad, Martin Zacharias, Carina C. de Oliveira Mann · 2026 · iScience
49. Current Perspectives on STING Agonists for Anticancer Drug Development
    Dilay Kahvecioglu · 2026 · Chemical Biology & Drug Design
50. Biomimetic PD-1-Functionalized Immunostimulatory Nanomedicine Enables STING Activation and Durable Antitumor Immunity in Hepatocellular Carcinoma
    Yanbing Cao, Xinyi Lin, Bingchen Wu, Yang Li, Wenrui Zhu, Binxin Liu, Aixian Zheng, Lingjie Wu, Yanyang Wang, Xiaolong Liu et al. · 2026 · Nano-Micro Letters
51. Mn(III)‐Derived MnO 2‐x Passivated Graphene Quantum Dots for Tumor‐Specific Chemo‐Immunotherapy Through Triggering Ferroptosis and Activating cGAS‐STING Pathway
    Jinyan Hu, Xinyan Liu, Yuqi Xiang, Zhenlin Zhang, Lang Yan, Bijiang Geng, Yiliang Su, Yun Wu · 2026 · Small
52. Benzothiazole derivatives target oligoadenylate synthetase and enhance RSV vaccine efficacy as adjuvants
    Xuanli Jin, Zhihui Zhang, Hong Liu, Yunzhi Tan, Peiying Luo, Zhenfu Wen, Haolin Chen, Lixin Liu, Yongming Chen · 2026 · Bioactive Materials
53. In situ macrophage reprogramming via micropatch engineering for safe and effective antitumor adoptive cell therapy
    Yongkang Xu, Lei Cao, Yuyan Zhou, Wenhao Li, Han Lin, Yuan Yong, Jianlin Shi, Wencheng Wu · 2026 · 中国科学通报：英文版
54. Electroporation-primed cascade nanocatalysis boosts STING-driven chemoimmunotherapy in hepatocellular carcinoma
    Jiaxin Zhao, Zheyu Fang, Ziang Luo, Jingye Yang, Sakarie Mustafe Hidig, Jie Zhou, Fangshen Xu, Huilin Zheng, Lei Zhang, Shengyong Yin et al. · 2026 · Materials Today Bio
55. A ROS-responsive injectable hydrogel orchestrating photothermal–immune synergy for osteosarcoma therapy through spatiotemporal immuno-microenvironment remodeling
    Zhaolong Yu, Qiuqun Xiao, Zhongyi Sun, Xiaojiang Sun, Ding Baozhi, Xiaofei Cheng, Jiefeng Zhang, Minzhao Lin, Jiwei Tian · 2026 · Photodiagnosis and Photodynamic Therapy
56. An intelligent gatekeeping nanoplatform evades cytokine storms and cascade-amplifies STING activation for safe sonocatalytic immunotherapy
    Yan Zhao, Lijun Ren, Jinyan Hu, Lang Yan, Yingtang Zhou, Bijiang Geng, Xing Zhang · 2026 · Chemical Engineering Journal
57. Cathepsin L potentiates autoimmunity by inhibiting lysosome-mediated STING degradation
    Jia‐Qing Xing, Zhi-Hao Zhang, Zeng-Lin Guo, Hong Cai, Qiuying Han, Jie Pan, Min-Yi Feng, Wen Xue, Ming Zhao, Kai Wang et al. · 2026 · Frontiers in Immunology
58. CXCR2-engineered biomimetic prodrug nanoplatform restores STING signaling and enhances anti-glioma immunity
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59. A GSH-responsive stapled oncolytic peptide-STING agonist conjugate for tumor-selective immunotherapy
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60. Manganese-doped zinc oxide Nano-agonists activating the cGAS-STING pathway to potentiate anti-tumor immunotherapy and reprogram the immunosuppressive tumor microenvironment
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61. Context-Dependent cGAS-STING Activation Shapes Metastatic Progression and Dormancy
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62. A metal-phenolic nanoregulator for intrinsic PI3K/AKT brake-releasing and STING-activating to unleash antitumor immunity in TNBC
    Ziying Chen, 冯海明, Yanzhao Diao, Wansheng Geng, Lifeng Hang, Jin Fang, Yuan Xu, Wenjin Li, Benhao Feng, Hua Wen et al. · 2026 · Chemical Engineering Journal
63. A Defect‐Engineered Sono‐Piezocatalytic In Situ Hydrogel for Preventing Hepatocellular Carcinoma Recurrence After Incomplete Radiofrequency Ablation
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64. Beyond Agonist Delivery: Metallic Nanomaterials as Active Regulators of cGAS-STING Signaling in Cancer Immunotherapy
    Yunqi Guo, Zhihao Zhao, Liangcan He, Wei Tang · 2026 · ACS Nano Medicine
65. Thymine-functionalized bPEI nanocomplexes for synergistic STING activation and PD-L1 silencing to potentiate cancer immunotherapy
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66. Targeting innate immunity in cancer: mechanistic foundations, therapeutic vaccination, and clinical translation
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67. CD200–CD200R as a myeloid immune checkpoint in solid tumors: mechanisms, context-dependent functions, and therapeutic opportunities
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68. Toll-like Receptor 2 Recognition of Microbiota Lipoproteins and Lipids in Immunity and Therapy
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69. The cGAS-STING pathway: mechanistic basis, dual biological functions and translational therapeutic advances
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70. Intranasal ginseng-derived nanovesicles integrate mitochondrial-targeted sonodynamic therapy with STING-driven immune reprogramming for glioblastoma treatment
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71. D-π-A configured carbon dot-driven morphology and vacancy dual-engineering of hollow Mn3O4 sonozymes for cGAS-STING activation enhanced sonodynamic immunotherapy
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72. Hybridization‐Mediated Reversible sgRNA Caging Enables Tumor‐Selective Gene Editing for Potentiating Antitumor Immunity via cGAS Demethylation
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73. Hybridization‐Mediated Reversible sgRNA Caging Enables Tumor‐Selective Gene Editing for Potentiating Antitumor Immunity via cGAS Demethylation
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74. Preclinical efficacy of a systemically-administered, second-generation STING agonist that promotes anti-tumour immunity in combination with radiotherapy
    Malin Pedersen, Lisa C. Hubbard, Shane Foo, Anton Patrikeev, Antonio Rullan, Holly Baldock, Christian Mandl, Paolo Chetta, Jehanne Hassan, Isaac Dean et al. · 2026 · British Journal of Cancer
75. Same organ, divergent immunity: T-cell exhaustion versus stromal exclusion in hepatocellular carcinoma and intrahepatic cholangiocarcinoma
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76. Nanoengineered STING agonists for cancer therapy: toward immunodynamic control
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77. A dynamic molecular glue targets a plastic MDA5 filament interface to stimulate innate immunity
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78. Discovery of Novel Orally Bioavailable STING Inhibitors with 4,5,6,7-Tetrahydropyrazolo[1,5- a ]pyrazine Moiety for STING-Mediated Inflammatory Disorders
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79. Chemical Modulation of the cGAS‐STING‐ENPP1 Axis: Medicinal Chemistry and Clinical Perspective
    Akash U. Shinde, Sandip Bibishan Bharate · 2026 · Medicinal Research Reviews
80. BindingDB Entry 50023807: Synthesis and structure-activity evaluation of a series of novel tricyclic STING activators.
    BindingDB · 2026 · UC San Diego
81. BindingDB Entry 50015584: STING, a promising target for small molecular immune modulator: A review.
    BindingDB · 2023 · UC San Diego
82. BindingDB Entry 50023426: Discovery of an Orally Bioavailable STING Inhibitor with In Vivo Anti-Inflammatory Activity in Mice with STING-Mediated Inflammation.
    BindingDB · 2026 · UC San Diego
83. BindingDB Entry 50015625: Small molecule approaches to treat autoimmune and inflammatory diseases (Part II): Nucleic acid sensing antagonists and inhibitors.
    BindingDB · 2023 · UC San Diego
84. BindingDB Entry 50020231: Structure-Activity Relationship Study of 1
    BindingDB · 2024 · UC San Diego
85. BindingDB Entry 50022447: Discovery of novel amidobenzimidazole derivatives as orally available small molecule modulators of stimulator of interferon genes for cancer immunotherapy.
    BindingDB · 2025 · UC San Diego
86. BindingDB Entry 50018006: Discovery of Selenium-Containing STING Agonists as Orally Available Antitumor Agents.
    BindingDB · 2023 · UC San Diego
87. BindingDB Entry 50023761: Discovery of 3-(Fluoro-imidazolyl)pyridazine Derivatives as Potent STING Agonists with Antitumor Activity.
    BindingDB · 2026 · UC San Diego
88. BindingDB Entry 50021273: Discovery of Pyrido[2,3-d]pyrimidin-7-one Derivatives as Highly Potent and Efficacious Ectonucleotide Pyrophosphatase/Phosphodiesterase 1 (ENPP1) Inhibitors for Cancer Treatment.
    BindingDB · 2025 · UC San Diego
89. BindingDB Entry 50015272: Discovery of Non-Nucleotide Small-Molecule STING Agonists
    BindingDB · 2023 · UC San Diego
90. BindingDB Entry 50019243: Design, Synthesis, and Biological Evaluation of Bipyridazine Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists.
    BindingDB · 2024 · UC San Diego
91. BindingDB Entry 50023467: Discovery of orally bioavailable phosphonate prodrugs of potent ENPP1 inhibitors for cancer treatment.
    BindingDB · 2026 · UC San Diego
92. BindingDB Entry 50021865: [1,2,4]Triazolo[1,5-a]pyrimidine derivatives: Structure-activity relationship study leading to highly selective ENPP1 inhibitors.
    BindingDB · 2025 · UC San Diego
93. BindingDB Entry 50018630: If small molecules immunotherapy comes, can the prime be far behind?
    BindingDB · 2024 · UC San Diego
94. BindingDB Entry 50015845: Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
    BindingDB · 2023 · UC San Diego
95. BindingDB Entry 50016102: Discovery of novel Thieno[2,3-d]imidazole derivatives as agonists of human STING for antitumor immunotherapy using systemic administration.
    BindingDB · 2023 · UC San Diego
96. BindingDB Entry 50015070: Identification of Novel Carbocyclic Pyrimidine Cyclic Dinucleotide STING Agonists for Antitumor Immunotherapy Using Systemic Intravenous Route.
    BindingDB · 2023 · UC San Diego
97. BindingDB Entry 50020700: Development of Orally Bioavailable Amidobenzimidazole Analogues Targeting Stimulator of Interferon Gene (STING) Receptor.
    BindingDB · 2024 · UC San Diego
98. BindingDB Entry 50019508: Structure-activity relationship study of amidobenzimidazole derivatives as stimulator of interferon genes (STING) agonists.
    BindingDB · 2024 · UC San Diego
99. BindingDB Entry 50017738: Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
    BindingDB · 2023 · UC San Diego
100. BindingDB Entry 50021651: Perspectives on Nuclear Magnetic Resonance Spectroscopy in Drug Discovery Research.
     BindingDB · 2025 · UC San Diego