Development of small molecule inhibitors/agonists targeting STING for disease

Electronic complementarity permits hindered butenolide heterodimerization and discovery of novel cGAS/STING pathway antagonists

(2020) Benjamin J. Huffman et al.   Nature Chemistry

Homeostatic regulation of STING protein at the resting state by stabilizer TOLLIP

(2020) Vladislav Pokatayev et al.   NATURE IMMUNOLOGY

A defect in COPI-mediated transport of STING causes immune dysregulation in COPA syndrome

(2020) Zimu Deng et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Mutations in COPA lead to abnormal trafficking of STING to the Golgi and interferon signaling

(2020) Alice Lepelley et al.   JOURNAL OF EXPERIMENTAL MEDICINE

cGAS-STING, an important pathway in cancer immunotherapy

(2020) Minlin Jiang et al.   Journal of Hematology & Oncology

C9orf72 in myeloid cells suppresses STING-induced inflammation

(2020) Madelyn E. McCauley et al.   NATURE

Endosomolytic polymersomes increase the activity of cyclic dinucleotide STING agonists to enhance cancer immunotherapy

(2019) Daniel Shae et al.   Nature Nanotechnology

Structural basis of STING binding with and phosphorylation by TBK1

(2019) Conggang Zhang et al.   NATURE

Cryo-EM structures of STING reveal its mechanism of activation by cyclic GMP–AMP

(2019) Guijun Shang et al.   NATURE

Autophagy induction via STING trafficking is a primordial function of the cGAS pathway

(2019) Xiang Gui et al.   NATURE

Association of Aspirin Use for Primary Prevention With Cardiovascular Events and Bleeding Events

(2019) Sean L. Zheng et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Acetylation Blocks cGAS Activity and Inhibits Self-DNA-Induced Autoimmunity

(2019) Jiang Dai et al.   CELL

Modular Architecture of the STING C-Terminal Tail Allows Interferon and NF-κB Signaling Adaptation

(2019) Carina C. de Oliveira Mann et al.   Cell Reports

Function of Green Tea Catechins in the Brain: Epigallocatechin Gallate and its Metabolites

(2019) Monira Pervin et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Innate immunity signalling and membrane trafficking

(2019) Tomohiko Taguchi et al.   CURRENT OPINION IN CELL BIOLOGY

Design, synthesis and biological evaluation of acridone analogues as novel STING receptor agonists

(2019) Shi Hou et al.   BIOORGANIC CHEMISTRY

Design, Synthesis, and Biological Evaluation of Amidobenzimidazole Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists

(2019) Qiumu Xi et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Cytosolic DNA-Sensing cGAS–STING Pathway in Cancer

(2019) John Kwon et al.   Cancer Discovery

Design and synthesis of plant cyclopeptide Astin C analogues and investigation of their immunosuppressive activity

(2018) Fei Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Dynamic Structural Differences between Human and Mouse STING Lead to Differing Sensitivity to DMXAA

(2018) Amy Y. Shih et al.   BIOPHYSICAL JOURNAL

Chromosomal instability drives metastasis through a cytosolic DNA response

(2018) Samuel F. Bakhoum et al.   NATURE

Can innate immune system targets turn up the heat on 'cold' tumours?

(2018) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

Species-specific disruption of STING-dependent antiviral cellular defenses by the Zika virus NS2B3 protease

(2018) Qiang Ding et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A novel anti-malarial drug derivative inhibits cyclic GMP-AMP synthase in Trex1 deficient mice

(2018) Jie An et al.   Arthritis & Rheumatology

A Mutation Outside the Dimerization Domain Causing Atypical STING-Associated Vasculopathy With Onset in Infancy

(2018) Rohit G. Saldanha et al.   Frontiers in Immunology

Radiation-Induced Chromosomal Aberrations and Immunotherapy: Micronuclei, Cytosolic DNA, and Interferon-Production Pathway

(2018) Marco Durante et al.   Frontiers in Oncology

Identification of α-Mangostin as an Agonist of Human STING

(2018) Yibo Zhang et al.   ChemMedChem

Recent advances in small molecule based cancer immunotherapy

(2018) Binbin Cheng et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Induction of necrotic cell death and activation of STING in the tumor microenvironment via cationic silica nanoparticles leading to enhanced antitumor immunity

(2018) Myunggi An et al.   Nanoscale

Parkin and PINK1 mitigate STING-induced inflammation

(2018) Danielle A. Sliter et al.   NATURE

Targeting STING with covalent small-molecule inhibitors

(2018) Simone M. Haag et al.   NATURE

Design, synthesis, and biological evaluation of C7-functionalized DMXAA derivatives as potential human-STING agonists

(2018) Jihyun Hwang et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Nitro-fatty acids are formed in response to virus infection and are potent inhibitors of STING palmitoylation and signaling

(2018) Anne Louise Hansen et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Design of amidobenzimidazole STING receptor agonists with systemic activity

(2018) Joshi M. Ramanjulu et al.   NATURE

G3BP1 promotes DNA binding and activation of cGAS

(2018) Zhao-Shan Liu et al.   NATURE IMMUNOLOGY

Discovery of a Novel cGAMP Competitive Ligand of the Inactive Form of STING

(2018) Tony Siu et al.   ACS Medicinal Chemistry Letters

The Cyclopeptide Astin C Specifically Inhibits the Innate Immune CDN Sensor STING

(2018) Senlin Li et al.   Cell Reports

Medicinal properties of mangosteen ( Garcinia mangostana L.): A comprehensive update

(2017) Berenice Ovalle-Magallanes et al.   FOOD AND CHEMICAL TOXICOLOGY

cGAS/STING Pathway in Cancer: Jekyll and Hyde Story of Cancer Immune Response

(2017) Debojit Bose   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Single Mutations Reshape the Structural Correlation Network of the DMXAA–Human STING Complex

(2017) Xing Che et al.   JOURNAL OF PHYSICAL CHEMISTRY B

Emerging Alphaviruses Are Sensitive to Cellular States Induced by a Novel Small-Molecule Agonist of the STING Pathway

(2017) Bryan Gall et al.   JOURNAL OF VIROLOGY

Mitotic progression following DNA damage enables pattern recognition within micronuclei

(2017) Shane M. Harding et al.   NATURE

Versatile modes of cellular regulation via cyclic dinucleotides

(2017) Petya Violinova Krasteva et al.   Nature Chemical Biology

Role of Aspirin in Breast Cancer Survival

(2017) Wendy Y. Chen et al.   Current Oncology Reports

Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice

(2017) Jessica Vincent et al.   Nature Communications

Trafficking-Mediated STING Degradation Requires Sorting to Acidified Endolysosomes and Can Be Targeted to Enhance Anti-tumor Response

(2017) Vijay K. Gonugunta et al.   Cell Reports

MITA/STING and Its Alternative Splicing Isoform MRP Restrict Hepatitis B Virus Replication

(2017) Shuhui Liu et al.   PLoS One

Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay

(2017) Justin Hall et al.   PLoS One

Familial chilblain lupus due to a gain-of-function mutation in STING

(2016) Nadja König et al.   ANNALS OF THE RHEUMATIC DISEASES

STING Promotes the Growth of Tumors Characterized by Low Antigenicity via IDO Activation

(2016) Henrique Lemos et al.   CANCER RESEARCH

The host STING pathway at the interface of cancer and immunity

(2016) Leticia Corrales et al.   JOURNAL OF CLINICAL INVESTIGATION

cGAS-STING Signaling Regulates Initial Innate Control of Cytomegalovirus Infection

(2016) Chan-Wang J. Lio et al.   JOURNAL OF VIROLOGY

Activation of STING requires palmitoylation at the Golgi

(2016) Kojiro Mukai et al.   Nature Communications

Antitumor Activity of cGAMP via Stimulation of cGAS-cGAMP-STING-IRF3 Mediated Innate Immune Response

(2016) Tiejun Li et al.   Scientific Reports

The Cytosolic Sensor cGAS Detects Mycobacterium tuberculosis DNA to Induce Type I Interferons and Activate Autophagy

(2015) Robert O. Watson et al.   Cell Host & Microbe

Cyclic GMP-AMP Synthase Is an Innate Immune DNA Sensor for Mycobacterium tuberculosis

(2015) Angela C. Collins et al.   Cell Host & Microbe

The Role of Aspirin, Vitamin D, Exercise, Diet, Statins, and Metformin in the Prevention and Treatment of Colorectal Cancer

(2015) Amikar Sehdev et al.   CURRENT TREATMENT OPTIONS IN ONCOLOGY

DNA Damage Primes the Type I Interferon System via the Cytosolic DNA Sensor STING to Promote Anti-Microbial Innate Immunity

(2015) Anetta Härtlova et al.   IMMUNITY

Liposomes loaded with a STING pathway ligand, cyclic di-GMP, enhance cancer immunotherapy against metastatic melanoma

(2015) Takashi Nakamura et al.   JOURNAL OF CONTROLLED RELEASE

DNA-Mediated Cyclic GMP–AMP Synthase–Dependent and –Independent Regulation of Innate Immune Responses

(2015) Kou Motani et al.   JOURNAL OF IMMUNOLOGY

Activation of cyclic GMP-AMP synthase by self-DNA causes autoimmune diseases

(2015) Daxing Gao et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

STING agonist formulated cancer vaccines can cure established tumors resistant to PD-1 blockade

(2015) Juan Fu et al.   Science Translational Medicine

Characterization of a Novel Human-Specific STING Agonist that Elicits Antiviral Activity Against Emerging Alphaviruses

(2015) Tina M. Sali et al.   PLoS Pathogens

Role of DNA/RNA sensors and contribution to autoimmunity

(2014) Siobhán Smith et al.   CYTOKINE & GROWTH FACTOR REVIEWS

STING-Dependent Cytosolic DNA Sensing Mediates Innate Immune Recognition of Immunogenic Tumors

(2014) Seng-Ryong Woo et al.   IMMUNITY

STING-Dependent Cytosolic DNA Sensing Promotes Radiation-Induced Type I Interferon-Dependent Antitumor Immunity in Immunogenic Tumors

(2014) Liufu Deng et al.   IMMUNITY

Inherited STING-activating mutation underlies a familial inflammatory syndrome with lupus-like manifestations

(2014) Nadia Jeremiah et al.   JOURNAL OF CLINICAL INVESTIGATION

The cGAS-cGAMP-STING Pathway of Cytosolic DNA Sensing and Signaling

(2014) Xin Cai et al.   MOLECULAR CELL

Hydrolysis of 2′3′-cGAMP by ENPP1 and design of nonhydrolyzable analogs

(2014) Lingyin Li et al.   Nature Chemical Biology

Activated STING in a Vascular and Pulmonary Syndrome

(2014) Yin Liu et al.   NEW ENGLAND JOURNAL OF MEDICINE

Inflammation-driven carcinogenesis is mediated through STING

(2014) Jeonghyun Ahn et al.   Nature Communications

Binding-Pocket and Lid-Region Substitutions Render Human STING Sensitive to the Species-Specific Drug DMXAA

(2014) Pu Gao et al.   Cell Reports

Anticancer Flavonoids Are Mouse-Selective STING Agonists

(2013) Sujeong Kim et al.   ACS Chemical Biology

Identification of human-selective analogues of the vascular-disrupting agent 5,6-dimethylxanthenone-4-acetic acid (DMXAA)

(2013) S M Tijono et al.   BRITISH JOURNAL OF CANCER

Structure-Function Analysis of STING Activation by c[G(2′,5′)pA(3′,5′)p] and Targeting by Antiviral DMXAA

(2013) Pu Gao et al.   CELL

Oxidative Damage of DNA Confers Resistance to Cytosolic Nuclease TREX1 Degradation and Potentiates STING-Dependent Immune Sensing

(2013) Nadine Gehrke et al.   IMMUNITY

Mouse, but not Human STING, Binds and Signals in Response to the Vascular Disrupting Agent 5,6-Dimethylxanthenone-4-Acetic Acid

(2013) J. Conlon et al.   JOURNAL OF IMMUNOLOGY

Adenovirus Detection by the cGAS/STING/TBK1 DNA Sensing Cascade

(2013) E. Lam et al.   JOURNAL OF VIROLOGY

Cyclic di-GMP: the First 25 Years of a Universal Bacterial Second Messenger

(2013) U. Romling et al.   MICROBIOLOGY AND MOLECULAR BIOLOGY REVIEWS

Cyclic GMP-AMP Containing Mixed Phosphodiester Linkages Is An Endogenous High-Affinity Ligand for STING

(2013) Xu Zhang et al.   MOLECULAR CELL

cGAS produces a 2′-5′-linked cyclic dinucleotide second messenger that activates STING

(2013) Andrea Ablasser et al.   NATURE

Single Nucleotide Polymorphisms of Human STING Can Affect Innate Immune Response to Cyclic Dinucleotides

(2013) Guanghui Yi et al.   PLoS One

Pivotal Roles of cGAS-cGAMP Signaling in Antiviral Defense and Immune Adjuvant Effects

(2013) X.-D. Li et al.   SCIENCE

Cyclic GMP-AMP Synthase Is an Innate Immune Sensor of HIV and Other Retroviruses

(2013) D. Gao et al.   SCIENCE

STING-Dependent Recognition of Cyclic di-AMP Mediates Type I Interferon Responses during Chlamydia trachomatis Infection

(2013) J. R. Barker et al.   mBio

Structural Analysis of the STING Adaptor Protein Reveals a Hydrophobic Dimer Interface and Mode of Cyclic di-GMP Binding

(2012) Songying Ouyang et al.   IMMUNITY

Autoimmunity Initiates in Nonhematopoietic Cells and Progresses via Lymphocytes in an Interferon-Dependent Autoimmune Disease

(2012) Alevtina Gall et al.   IMMUNITY

STING manifests self DNA-dependent inflammatory disease

(2012) J. Ahn et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Cyclic GMP-AMP Is an Endogenous Second Messenger in Innate Immune Signaling by Cytosolic DNA

(2012) J. Wu et al.   SCIENCE

Cyclic GMP-AMP Synthase Is a Cytosolic DNA Sensor That Activates the Type I Interferon Pathway

(2012) L. Sun et al.   SCIENCE

Mitochondria-dependent apoptosis of activated T lymphocytes induced by astin C, a plant cyclopeptide, for preventing murine experimental colitis

(2011) Yan Shen et al.   BIOCHEMICAL PHARMACOLOGY

MPYS Is Required for IFN Response Factor 3 Activation and Type I IFN Production in the Response of Cultured Phagocytes to Bacterial Second Messengers Cyclic-di-AMP and Cyclic-di-GMP

(2011) L. Jin et al.   JOURNAL OF IMMUNOLOGY

STING is a direct innate immune sensor of cyclic di-GMP

(2011) Dara L. Burdette et al.   NATURE

The helicase DDX41 senses intracellular DNA mediated by the adaptor STING in dendritic cells

(2011) Zhiqiang Zhang et al.   NATURE IMMUNOLOGY

Pattern Recognition Receptors and Inflammation

(2010) Osamu Takeuchi et al.   CELL

IFI16 is an innate immune sensor for intracellular DNA

(2010) Leonie Unterholzner et al.   NATURE IMMUNOLOGY

An orthogonal proteomic-genomic screen identifies AIM2 as a cytoplasmic DNA sensor for the inflammasome

(2009) Tilmann Bürckstümmer et al.   NATURE IMMUNOLOGY

Atg9a controls dsDNA-driven dynamic translocation of STING and the innate immune response

(2009) T. Saitoh et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Trex1 Prevents Cell-Intrinsic Initiation of Autoimmunity

(2008) Daniel B. Stetson et al.   CELL