ArticleThe Journal of biological chemistry2016
Identifying a Small Molecule Blocking Antigen Presentation in Autoimmune Thyroiditis.
Article in The Journal of biological chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 28 citations in OpenAlex.
- Using HLA-DR3-CBA/J Humanized Mice to Develop a Novel Genetic Model for Autoimmune Thyroiditis.Genes · 2026Article
- Graves' Disease: Is It Time for Targeted Therapy? A Narrative Review.Medicina (Kaunas, Lithuania) · 2025Review
- Promising Role of Alkaloids in the Prevention and Treatment of Thyroid Cancer and Autoimmune Thyroid Disease: A Comprehensive Review of the Current Evidence.International journal of molecular sciences · 2024Review
- A Flexible Mouse Model of Autoimmune Thyroiditis Induced by Immunization with an Adenovirus Containing Full-Length Thyroglobulin cDNA.Current protocols · 2024Article
- The association of common autoimmune diseases with autoimmune thyroiditis: a two-sample Mendelian randomization study.Frontiers in endocrinology · 2024Article
- Research progress on pharmacological effects and mechanisms of cepharanthine and its derivatives.Naunyn-Schmiedeberg's archives of pharmacology · 2023Review
- Pharmacological Activity of Cepharanthine.Molecules (Basel, Switzerland) · 2023Review
- Perturbation of endoplasmic reticulum proteostasis triggers tissue injury in the thyroid gland.JCI insight · 2023Article
- Effective Inhibition of Thyroid Antigen Presentation Using Retro-Inverso Peptides in Experimental Autoimmune Thyroiditis: A Pathway Toward Immune Therapies of Thyroid Autoimmunity.Thyroid : official journal of the American Thyroid Association · 2023Article
- Genetics and epigenetics of autoimmune thyroid diseases: Translational implications.Best practice & research. Clinical endocrinology & metabolism · 2023Review
- Epitope Mapping of Pathogenic Autoantigens on Sjögren's Syndrome-Susceptible Human Leukocyte Antigens Using In Silico Techniques.Journal of clinical medicine · 2022Article
- Blocking IAgLife sciences · 2022Article
- Cepharanthine Blocks Presentation of Thyroid and Islet Peptides in a Novel Humanized Autoimmune Diabetes and Thyroiditis Mouse Model.Frontiers in immunology · 2021Article
- T cell receptor sequencing in autoimmunity.Journal of life sciences (Westlake Village, Calif.) · 2020Article
- A Novel Mouse Model of Autoimmune Thyroiditis Induced by Immunization with Adenovirus Containing Full-Length Thyroglobulin cDNA: Implications to Genetic Studies of Thyroid Autoimmunity.Thyroid : official journal of the American Thyroid Association · 2020Article
- Identification of novel HLA-A0201-restricted T-cell epitopes against thyroid antigens in autoimmune thyroid diseases.Endocrine · 2020Article
- Cepharanthine blocks TSH receptor peptide presentation by HLA-DR3: Therapeutic implications to Graves' disease.Journal of autoimmunity · 2020Article
- Cepharanthine: An update of its mode of action, pharmacological properties and medical applications.Phytomedicine : international journal of phytotherapy and phytopharmacology · 2019Review
- Rationally designed small molecules to prevent type 1 diabetes.Current opinion in endocrinology, diabetes, and obesity · 2019Review
- Structure-based selection of human metabolite binding P4 pocket of DRB1*15:01 and DRB1*15:03, with implications for multiple sclerosis.Genes and immunity · 2019Article
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
We previously showed that an HLA-DR variant containing arginine at position 74 of the DRβ1 chain (DRβ1-Arg74) is the specific HLA class II variant conferring risk for autoimmune thyroid diseases (AITD). We also identified 5 thyroglobulin (Tg) peptides that bound to DRβ1-Arg74. We hypothesized that blocking the binding of these peptides to DRβ1-Arg74 could block the continuous T-cell activation in thyroiditis needed to maintain the autoimmune response to the thyroid. The aim of the current study was to identify small molecules that can block T-cell activation by Tg peptides presented within DRβ1-Arg74 pockets. We screened a large and diverse library of compounds and identified one compound, cepharanthine that was able to block peptide binding to DRβ1-Arg74. We then showed that Tg.2098 is the dominant peptide when inducing experimental autoimmune thyroiditis (EAT) in NOD mice expressing human DRβ1-Arg74. Furthermore, cepharanthine blocked T-cell activation by thyroglobulin peptides, in particular Tg.2098 in mice that were induced with EAT. For the first time we identified a small molecule that can block Tg peptide binding and presentation to T-cells in autoimmune thyroiditis. If confirmed cepharanthine could potentially have a role in treating human AITD.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.