ArticleMolecular pharmacology2018
Carboxylic Acid Derivatives of Amlexanox Display Enhanced Potency toward TBK1 and IKK
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Article in Molecular pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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24citing papers in PubMed
2.0field-weighted citation impact, top 12% of its field
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Who cites it
24 citing papers in PubMed, 50 citations in OpenAlex.
- Targeting the cGAS-STING Pathway to Modulate Immune Inflammation in Diabetes and Cardiovascular Complications: Mechanisms and Therapeutic Insights.Current issues in molecular biology · 2025Review
- TBK1 inhibitor amlexanox exerts anti-cancer effects against endometrial cancer by regulating AKT/NF-κB signaling.International journal of biological sciences · 2025Article
- In Silico Insights: QSAR Modeling of TBK1 Kinase Inhibitors for Enhanced Drug Discovery.Journal of chemical information and modeling · 2024Article
- Review
- Article
- Role of TBK1 Inhibition in Targeted Therapy of Cancer.Mini reviews in medicinal chemistry · 2024Review
- Identification of TBK1 inhibitors against breast cancer using a computational approach supported by machine learning.Frontiers in pharmacology · 2024Article
- Tetrazoles and Related Heterocycles as Promising Synthetic Antidiabetic Agents.International journal of molecular sciences · 2023Review
- TRAF7 negatively regulates the RLR signaling pathway by facilitating the K48-linked ubiquitination of TBK1.Virologica Sinica · 2023Article
- Beyond DNA sensing: expanding the role of cGAS/STING in immunity and diseases.Archives of pharmacal research · 2023Review
- The NF-κB Pharmacopeia: Novel Strategies to Subdue an Intractable Target.Biomedicines · 2022Review
- Role of IKKε in the Metabolic Diseases: Physiology, Pathophysiology, and Pharmacology.Frontiers in pharmacology · 2022Review
- Inhibitory targeting cGAS-STING-TBK1 axis: Emerging strategies for autoimmune diseases therapy.Frontiers in immunology · 2022Review
- Role of nucleic acid sensing in the pathogenesis of type 1 diabetes.World journal of diabetes · 2021Review
- Recent Advances in Pain Management: Relevant Protein Kinases and Their Inhibitors.Molecules (Basel, Switzerland) · 2021Review
- Amlexanox Enhances Temozolomide-Induced Antitumor Effects in Human Glioblastoma Cells by Inhibiting IKBKE and the Akt-mTOR Signaling Pathway.ACS omega · 2021Article
- Signaling by cGAS-STING in Neurodegeneration, Neuroinflammation, and Aging.Trends in neurosciences · 2021Review
- Amlexanox: A Novel Therapeutic for Atopic, Metabolic, and Inflammatory Disease.The Yale journal of biology and medicine · 2020Review
- Small molecules targeting the innate immune cGAS‒STING‒TBK1 signaling pathway.Acta pharmaceutica Sinica. B · 2020Review
- A concise synthesis of 3-substituted-7-amino-6-carboxyl-8-azachromones.Tetrahedron letters · 2019Article
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Authors and funding
8 authors at 1 institution in 1 country.
Tyler S BeyettProgram in Chemical Biology (T.S.B.), Life Sciences Institute (T.S.B., L.C., J.J.G.T.), Departments of Medicinal Chemistry (X.G., H.D.S., J.J.G.T.), Pharmacology (J.J.G.T.), Biological Chemistry (J.J.G.T.), and Vahlteich Medicinal Chemistry Core, College of Pharmacy (X.G., H.D.S.), University of Michigan, Ann Arbor, Michigan; Institute for Diabetes and Metabolic Health (S.M.R., A.V.G., A.R.S.), Departments of Medicine (S.M.R., A.R.S.) and Pharmacology (A.V.G., A.R.S.), University of California, San Diego, La Jolla, California; and Departments of Biological Sciences and of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, Indiana (J.J.G.T.).ORCID 0000-0001-5509-7004
Xinmin GanProgram in Chemical Biology (T.S.B.), Life Sciences Institute (T.S.B., L.C., J.J.G.T.), Departments of Medicinal Chemistry (X.G., H.D.S., J.J.G.T.), Pharmacology (J.J.G.T.), Biological Chemistry (J.J.G.T.), and Vahlteich Medicinal Chemistry Core, College of Pharmacy (X.G., H.D.S.), University of Michigan, Ann Arbor, Michigan; Institute for Diabetes and Metabolic Health (S.M.R., A.V.G., A.R.S.), Departments of Medicine (S.M.R., A.R.S.) and Pharmacology (A.V.G., A.R.S.), University of California, San Diego, La Jolla, California; and Departments of Biological Sciences and of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, Indiana (J.J.G.T.).
Shannon M ReillyProgram in Chemical Biology (T.S.B.), Life Sciences Institute (T.S.B., L.C., J.J.G.T.), Departments of Medicinal Chemistry (X.G., H.D.S., J.J.G.T.), Pharmacology (J.J.G.T.), Biological Chemistry (J.J.G.T.), and Vahlteich Medicinal Chemistry Core, College of Pharmacy (X.G., H.D.S.), University of Michigan, Ann Arbor, Michigan; Institute for Diabetes and Metabolic Health (S.M.R., A.V.G., A.R.S.), Departments of Medicine (S.M.R., A.R.S.) and Pharmacology (A.V.G., A.R.S.), University of California, San Diego, La Jolla, California; and Departments of Biological Sciences and of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, Indiana (J.J.G.T.).
Louise ChangProgram in Chemical Biology (T.S.B.), Life Sciences Institute (T.S.B., L.C., J.J.G.T.), Departments of Medicinal Chemistry (X.G., H.D.S., J.J.G.T.), Pharmacology (J.J.G.T.), Biological Chemistry (J.J.G.T.), and Vahlteich Medicinal Chemistry Core, College of Pharmacy (X.G., H.D.S.), University of Michigan, Ann Arbor, Michigan; Institute for Diabetes and Metabolic Health (S.M.R., A.V.G., A.R.S.), Departments of Medicine (S.M.R., A.R.S.) and Pharmacology (A.V.G., A.R.S.), University of California, San Diego, La Jolla, California; and Departments of Biological Sciences and of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, Indiana (J.J.G.T.).
Andrew V GomezProgram in Chemical Biology (T.S.B.), Life Sciences Institute (T.S.B., L.C., J.J.G.T.), Departments of Medicinal Chemistry (X.G., H.D.S., J.J.G.T.), Pharmacology (J.J.G.T.), Biological Chemistry (J.J.G.T.), and Vahlteich Medicinal Chemistry Core, College of Pharmacy (X.G., H.D.S.), University of Michigan, Ann Arbor, Michigan; Institute for Diabetes and Metabolic Health (S.M.R., A.V.G., A.R.S.), Departments of Medicine (S.M.R., A.R.S.) and Pharmacology (A.V.G., A.R.S.), University of California, San Diego, La Jolla, California; and Departments of Biological Sciences and of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, Indiana (J.J.G.T.).
Alan R SaltielProgram in Chemical Biology (T.S.B.), Life Sciences Institute (T.S.B., L.C., J.J.G.T.), Departments of Medicinal Chemistry (X.G., H.D.S., J.J.G.T.), Pharmacology (J.J.G.T.), Biological Chemistry (J.J.G.T.), and Vahlteich Medicinal Chemistry Core, College of Pharmacy (X.G., H.D.S.), University of Michigan, Ann Arbor, Michigan; Institute for Diabetes and Metabolic Health (S.M.R., A.V.G., A.R.S.), Departments of Medicine (S.M.R., A.R.S.) and Pharmacology (A.V.G., A.R.S.), University of California, San Diego, La Jolla, California; and Departments of Biological Sciences and of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, Indiana (J.J.G.T.).
Hollis D ShowalterProgram in Chemical Biology (T.S.B.), Life Sciences Institute (T.S.B., L.C., J.J.G.T.), Departments of Medicinal Chemistry (X.G., H.D.S., J.J.G.T.), Pharmacology (J.J.G.T.), Biological Chemistry (J.J.G.T.), and Vahlteich Medicinal Chemistry Core, College of Pharmacy (X.G., H.D.S.), University of Michigan, Ann Arbor, Michigan; Institute for Diabetes and Metabolic Health (S.M.R., A.V.G., A.R.S.), Departments of Medicine (S.M.R., A.R.S.) and Pharmacology (A.V.G., A.R.S.), University of California, San Diego, La Jolla, California; and Departments of Biological Sciences and of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, Indiana (J.J.G.T.).
John J G TesmerProgram in Chemical Biology (T.S.B.), Life Sciences Institute (T.S.B., L.C., J.J.G.T.), Departments of Medicinal Chemistry (X.G., H.D.S., J.J.G.T.), Pharmacology (J.J.G.T.), Biological Chemistry (J.J.G.T.), and Vahlteich Medicinal Chemistry Core, College of Pharmacy (X.G., H.D.S.), University of Michigan, Ann Arbor, Michigan; Institute for Diabetes and Metabolic Health (S.M.R., A.V.G., A.R.S.), Departments of Medicine (S.M.R., A.R.S.) and Pharmacology (A.V.G., A.R.S.), University of California, San Diego, La Jolla, California; and Departments of Biological Sciences and of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, Indiana (J.J.G.T.) jtesmer@purdue.edu.
Girls Incorporated · US
Funding
INTERDEPARTMENTAL TRAINING IN PHARMACOLOGICAL SCIENCEST32GM007767 · NIGMS · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI ISOM, LORI L. · 1985 to 2019
$10.2MStructure, function, and inhibition of G protein-coupled receptor kinasesR01HL071818 · NHLBI · UNIVERSITY OF TEXAS AUSTIN · PI TESMER, JOHN · 2004 to 2023
$7.1MSignaling Pathways in Insulin ActionR01DK060591 · NIDDK · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI SALTIEL, ALAN R. · 2002 to 2016
$4.9MHormonal Regulation of Glycogen SynthesisR01DK060597 · NIDDK · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI SALTIEL, ALAN R. · 2002 to 2010
$2.8MIKKepsilon/TBK1 Inhibitors for the Treatment of Obesity and Type 2 DiabetesR01DK100319 · NIDDK · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI SALTIEL, ALAN R. · 2014 to 2017
$2.3MStructure and Function of the LPLA2/LCAT Acyltransferase FamilyR01HL122416 · NHLBI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI TESMER, JOHN · 2015 to 2018
$1.9MIl-6 and metabolic crosstalk between tissuesK01DK105075 · NIDDK · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI REILLY, SHANNON MARIE · 2015 to 2017
$488kAn Il-6/Stat3 Autocrine Axis in Adipose TissueR03DK118195 · NIDDK · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI REILLY, SHANNON MARIE · 2018 to 2019
$233kNHLBI NIH HHS R01 HL071818NHLBI NIH HHS R01 HL122416NIDDK NIH HHS K01 DK105075NIDDK NIH HHS R01 DK060591NIDDK NIH HHS R01 DK060597NIDDK NIH HHS R01 DK100319NIDDK NIH HHS R03 DK118195NIGMS NIH HHS T32 GM007767
Abstract
Chronic low-grade inflammation is a hallmark of obesity, which is a risk factor for the development of type 2 diabetes. The drug amlexanox inhibits I
Indexed as
3T3-L1 CellsAdipocytesAminopyridinesAnimalsCarboxylic AcidsCell LineDiabetes Mellitus, Type 2Energy MetabolismHumansI-kappa B KinaseInflammationMiceProtein Kinase InhibitorsProtein Serine-Threonine KinasesStructure-Activity RelationshipAminopyridinesamlexanoxCarboxylic AcidsI-kappa B KinaseIKBKE protein, humanProtein Kinase InhibitorsProtein Serine-Threonine KinasesTBK1 protein, human
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