دورية أكاديمية
Androgen receptor mutations modulate activation by 11-oxygenated androgens and glucocorticoids.
| العنوان: | Androgen receptor mutations modulate activation by 11-oxygenated androgens and glucocorticoids. |
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| المؤلفون: | Snaterse G; Department of Internal Medicine, Section of Endocrinology, Erasmus MC, University Medical Center Rotterdam, Rotterdam, the Netherlands., Mies R; Department of Internal Medicine, Section of Endocrinology, Erasmus MC, University Medical Center Rotterdam, Rotterdam, the Netherlands., van Weerden WM; Department of Urology, Erasmus MC, University Medical Center Rotterdam, Rotterdam, The Netherlands., French PJ; Cancer Treatment Screening Facility, Department of Neurology, Erasmus MC, University Medical Center Rotterdam, Rotterdam, The Netherlands., Jonker JW; Section of Molecular Metabolism and Nutrition, Department of Pediatrics, University of Groningen, University Medical Center Groningen, Groningen, The Netherlands., Houtsmuller AB; Department of Pathology, Erasmus MC, University Medical Center Rotterdam, Rotterdam, The Netherlands., van Royen ME; Department of Pathology, Erasmus MC, University Medical Center Rotterdam, Rotterdam, The Netherlands., Visser JA; Department of Internal Medicine, Section of Endocrinology, Erasmus MC, University Medical Center Rotterdam, Rotterdam, the Netherlands., Hofland J; Department of Internal Medicine, Section of Endocrinology, Erasmus MC, University Medical Center Rotterdam, Rotterdam, the Netherlands. j.hofland@erasmusmc.nl. |
| المصدر: | Prostate cancer and prostatic diseases [Prostate Cancer Prostatic Dis] 2023 Jun; Vol. 26 (2), pp. 293-301. Date of Electronic Publication: 2022 Jan 19. |
| نوع المنشور: | Meta-Analysis; Journal Article; Research Support, Non-U.S. Gov't |
| اللغة: | English |
| بيانات الدورية: | Publisher: Nature Publishing Group Country of Publication: England NLM ID: 9815755 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1476-5608 (Electronic) Linking ISSN: 13657852 NLM ISO Abbreviation: Prostate Cancer Prostatic Dis Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: <2002->: London : Nature Publishing Group Original Publication: Houndmills, Basingstoke, UK : Stockton Press, c1997- |
| مواضيع طبية MeSH: | Androgens*/genetics , Androgens*/metabolism , Prostatic Neoplasms, Castration-Resistant*/drug therapy , Prostatic Neoplasms, Castration-Resistant*/genetics , Prostatic Neoplasms, Castration-Resistant*/metabolism, Male ; Humans ; Receptors, Androgen/genetics ; Receptors, Androgen/metabolism ; Glucocorticoids/pharmacology ; Ligands ; Testosterone/metabolism ; Steroids/metabolism ; Mutation ; Prednisolone/pharmacology ; Dexamethasone/pharmacology |
| مستخلص: | Background: Androgen receptor (AR) ligand-binding domain (LBD) mutations occur in ~20% of all castration-resistant prostate cancer (CRPC) patients. These mutations confer ligand promiscuity, but the affinity for many steroid hormone pathway intermediates is unknown. In this study, we investigated the stimulation of clinically relevant AR-LBD mutants by endogenous and exogenous steroid hormones present in CRPC patients to unravel their potential contribution to AR pathway reactivation. Methods: A meta-analysis of studies reporting untargeted analysis of AR mutants was performed to identify clinically relevant AR-LBD mutations. Using luciferase reporter and quantitative fluorescent microscopy, these AR mutants were screened for sensitivity for various endogenous steroids and synthetic glucocorticoids used in the treatment of CRPC. Results: The meta-analysis revealed that AR Conclusion: Both testosterone and 11KT effectively contribute to AR (© 2022. The Author(s), under exclusive licence to Springer Nature Limited.) |
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| المشرفين على المادة: | 0 (Androgens) 0 (Receptors, Androgen) 0 (Glucocorticoids) 0 (Ligands) 3XMK78S47O (Testosterone) 0 (Steroids) 9PHQ9Y1OLM (Prednisolone) 7S5I7G3JQL (Dexamethasone) |
| تواريخ الأحداث: | Date Created: 20220120 Date Completed: 20230609 Latest Revision: 20230614 |
| رمز التحديث: | 20230615 |
| DOI: | 10.1038/s41391-022-00491-z |
| PMID: | 35046557 |
| قاعدة البيانات: | MEDLINE |
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Full Text Finder | تدمد: | 1476-5608 |
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| DOI: | 10.1038/s41391-022-00491-z |