ArticleMolecular therapy : the journal of the American Society of Gene Therapy2012
Targeting the hemoglobin scavenger receptor CD163 in macrophages highly increases the anti-inflammatory potency of dexamethasone.
Article in Molecular therapy : the journal of the American Society of Gene Therapy, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 65 papers.
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Who cites it
65 citing papers in PubMed, 139 citations in OpenAlex.
- Polymer-mRNA complexes for monocyte-trafficked, lymph node-targeted cancer vaccination.Nature biomedical engineering · 2026Article
- CD74-Targeting Antibody-Drug Conjugate Enhances Immunosuppression of Glucocorticoid in Systemic Lupus Erythematosus.International journal of molecular sciences · 2025Article
- The next frontier in antibody-drug conjugates: challenges and opportunities in cancer and autoimmune therapy.Cancer drug resistance (Alhambra, Calif.) · 2025Review
- Granulomas in Common Variable Immunodeficiency Display Different Histopathological Features Compared to Other Granulomatous Diseases.Journal of clinical immunology · 2024Article
- Supramolecular assembly of polycation/mRNA nanoparticles and in vivo monocyte programming.Proceedings of the National Academy of Sciences of the United States of America · 2024Article
- Glucocorticoids-based prodrug design: Current strategies and research progress.Asian journal of pharmaceutical sciences · 2024Review
- Minimising the payload solvent exposed hydrophobic surface area optimises the antibody-drug conjugate properties.RSC medicinal chemistry · 2024Article
- The medicinal chemistry evolution of antibody-drug conjugates.RSC medicinal chemistry · 2024Review
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- Drug Delivery System Approaches for Rheumatoid Arthritis Treatment: A Review.Mini reviews in medicinal chemistry · 2024Review
- Anti-Obesity Drug Delivery Systems: Recent Progress and Challenges.Pharmaceutics · 2023Review
- ValCitGlyPro-dexamethasone antibody conjugates selectively suppress the activation of human monocytes.RSC medicinal chemistry · 2023Article
- The Evolving Landscape of Antibody-Drug Conjugates: In Depth Analysis of Recent Research Progress.Bioconjugate chemistry · 2023Review
- Development of Apoptotic-Cell-Inspired Antibody-Drug Conjugate for Effective Immune Modulation.International journal of molecular sciences · 2023Article
- An Overview of the Development and Preclinical Evaluation of Antibody-Drug Conjugates for Non-Oncological Applications.Pharmaceutics · 2023Review
- Targeting macrophages in atherosclerosis using nanocarriers loaded with liver X receptor agonists: A narrow review.Frontiers in molecular biosciences · 2023Review
- Evaluation of an ester-linked immunosuppressive payload: A case study in understanding the stability and cleavability of ester-containing ADC linkers.Bioorganic & medicinal chemistry letters · 2022Article
- Renaissance of glucocorticoids in critical care in the era of COVID-19: ten urging questions.Critical care (London, England) · 2022Review
- Scavenger Receptors: Novel Roles in the Pathogenesis of Liver Inflammation and Cancer.Seminars in liver disease · 2022Review
5 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
Synthetic glucocorticoids are potent anti-inflammatory drugs but serious side effects such as bone mobilization, muscle mass loss, immunosuppression, and metabolic alterations make glucocorticoid therapy a difficult balance. The therapeutic anti-inflammatory effect of glucocorticoids relies largely on the suppressed release of tumor-necrosis factor-α and other cytokines by macrophages at the sites of inflammation. We have now developed a new biodegradable anti-CD163 antibody-drug conjugate that specifically targets the glucocorticoid, dexamethasone to the hemoglobin scavenger receptor CD163 in macrophages. The conjugate, that in average contains four dexamethasone molecules per antibody, exhibits retained high functional affinity for CD163. In vitro studies in rat macrophages and in vivo studies of Lewis rats showed a strong anti-inflammatory effect of the conjugate measured as reduced lipopolysaccharide-induced secretion of tumor-necrosis factor-α. The in vivo potency of conjugated dexamethasone was about 50-fold that of nonconjugated dexamethasone. In contrast to a strong systemic effect of nonconjugated dexamethasone, the equipotent dose of the conjugate had no such effect, measured as thymus lymphocytes apoptosis, body weight loss, and suppression of endogenous cortisol levels. In conclusion, the study shows antibody-drug conjugates as a future approach in anti-inflammatory macrophage-directed therapy. Furthermore, the data demonstrate CD163 as an excellent macrophage target for anti-inflammatory drug delivery.
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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.