Advanced search
1 file | 593.35 KB Add to list

Improved glucocorticoid receptor ligands : fantastic beasts, but how to find them?

Laura Van Moortel (UGent) , Kris Gevaert (UGent) and Karolien De Bosscher (UGent)
Author
Organization
Abstract
Exogenous glucocorticoids are widely used in the clinic for the treatment of inflammatory disorders and hematological cancers. Unfortunately, their use is associated with debilitating side effects, including hyperglycemia, osteoporosis, mood swings, and weight gain. Despite the continued efforts of pharma as well as academia, the search for so-called selective glucocorticoid receptor modulators (SEGRMs), compounds with strong anti-inflammatory or anti-cancer properties but a reduced number or level of side effects, has had limited success so far. Although monoclonal antibody therapies have been successfully introduced for the treatment of certain disorders (such as anti-TNF for rheumatoid arthritis), glucocorticoids remain the first-in-line option for many other chronic diseases including asthma, multiple sclerosis, and multiple myeloma. This perspective offers our opinion on why a continued search for SEGRMs remains highly relevant in an era where small molecules are sometimes unrightfully considered old-fashioned. Besides a discussion on which bottlenecks and pitfalls might have been overlooked in the past, we elaborate on potential solutions and recent developments that may push future research in the right direction.
Keywords
glucocorticoids, glucocorticoid receptor, selective GR modulators, drug discovery, inflammation, assay development, GR, SEGRM, MULTIPLE-SCLEROSIS, INHALED CORTICOSTEROIDS, TOPICAL CORTICOSTEROIDS, DNA-BINDING, AGONIST, MAPRACORAT, EFFICACY, MECHANISMS, MODULATORS, DISCOVERY

Downloads

  • fendo-11-559673.pdf
    • full text (Published version)
    • |
    • open access
    • |
    • PDF
    • |
    • 593.35 KB

Citation

Please use this url to cite or link to this publication:

MLA
Van Moortel, Laura, et al. “Improved Glucocorticoid Receptor Ligands : Fantastic Beasts, but How to Find Them?” FRONTIERS IN ENDOCRINOLOGY, vol. 11, 2020, doi:10.3389/fendo.2020.559673.
APA
Van Moortel, L., Gevaert, K., & De Bosscher, K. (2020). Improved glucocorticoid receptor ligands : fantastic beasts, but how to find them? FRONTIERS IN ENDOCRINOLOGY, 11. https://doi.org/10.3389/fendo.2020.559673
Chicago author-date
Van Moortel, Laura, Kris Gevaert, and Karolien De Bosscher. 2020. “Improved Glucocorticoid Receptor Ligands : Fantastic Beasts, but How to Find Them?” FRONTIERS IN ENDOCRINOLOGY 11. https://doi.org/10.3389/fendo.2020.559673.
Chicago author-date (all authors)
Van Moortel, Laura, Kris Gevaert, and Karolien De Bosscher. 2020. “Improved Glucocorticoid Receptor Ligands : Fantastic Beasts, but How to Find Them?” FRONTIERS IN ENDOCRINOLOGY 11. doi:10.3389/fendo.2020.559673.
Vancouver
1.
Van Moortel L, Gevaert K, De Bosscher K. Improved glucocorticoid receptor ligands : fantastic beasts, but how to find them? FRONTIERS IN ENDOCRINOLOGY. 2020;11.
IEEE
[1]
L. Van Moortel, K. Gevaert, and K. De Bosscher, “Improved glucocorticoid receptor ligands : fantastic beasts, but how to find them?,” FRONTIERS IN ENDOCRINOLOGY, vol. 11, 2020.
@article{8684376,
  abstract     = {{Exogenous glucocorticoids are widely used in the clinic for the treatment of inflammatory disorders and hematological cancers. Unfortunately, their use is associated with debilitating side effects, including hyperglycemia, osteoporosis, mood swings, and weight gain. Despite the continued efforts of pharma as well as academia, the search for so-called selective glucocorticoid receptor modulators (SEGRMs), compounds with strong anti-inflammatory or anti-cancer properties but a reduced number or level of side effects, has had limited success so far. Although monoclonal antibody therapies have been successfully introduced for the treatment of certain disorders (such as anti-TNF for rheumatoid arthritis), glucocorticoids remain the first-in-line option for many other chronic diseases including asthma, multiple sclerosis, and multiple myeloma. This perspective offers our opinion on why a continued search for SEGRMs remains highly relevant in an era where small molecules are sometimes unrightfully considered old-fashioned. Besides a discussion on which bottlenecks and pitfalls might have been overlooked in the past, we elaborate on potential solutions and recent developments that may push future research in the right direction.}},
  articleno    = {{559673}},
  author       = {{Van Moortel, Laura and Gevaert, Kris and De Bosscher, Karolien}},
  issn         = {{1664-2392}},
  journal      = {{FRONTIERS IN ENDOCRINOLOGY}},
  keywords     = {{glucocorticoids,glucocorticoid receptor,selective GR modulators,drug discovery,inflammation,assay development,GR,SEGRM,MULTIPLE-SCLEROSIS,INHALED CORTICOSTEROIDS,TOPICAL CORTICOSTEROIDS,DNA-BINDING,AGONIST,MAPRACORAT,EFFICACY,MECHANISMS,MODULATORS,DISCOVERY}},
  language     = {{eng}},
  pages        = {{11}},
  title        = {{Improved glucocorticoid receptor ligands : fantastic beasts, but how to find them?}},
  url          = {{http://doi.org/10.3389/fendo.2020.559673}},
  volume       = {{11}},
  year         = {{2020}},
}

Altmetric
View in Altmetric
Web of Science
Times cited: