[HTML][HTML] Selective glucocorticoid receptor modulation: New directions with non-steroidal scaffolds

N Sundahl, J Bridelance, C Libert… - Pharmacology & …, 2015 - Elsevier
Glucocorticoids remain the frontline treatment for inflammatory disorders, yet represent a
double-edged sword with beneficial therapeutic actions alongside adverse effects, mainly in …

GR dimerization and the impact of GR dimerization on GR protein stability and half-life

A Louw - Frontiers in immunology, 2019 - frontiersin.org
Pharmacologically, glucocorticoids, which mediate their effects via the glucocorticoid
receptor (GR), are a most effective therapy for inflammatory diseases despite the fact that …

Glucocorticoid signaling and osteoarthritis

O Savvidou, M Milonaki, S Goumenos, D Flevas… - Molecular and cellular …, 2019 - Elsevier
Glucocorticoids are steroid hormones synthesized and released by the adrenal cortex. Their
main function is to maintain cell homeostasis through a variety of signaling pathways …

15-Deoxy-Δ-12, 14-prostaglandin J2 acts cooperatively with prednisolone to reduce TGF-β-induced pro-fibrotic pathways in human osteoarthritis fibroblasts

C Vaamonde-Garcia, O Malaise, E Charlier… - Biochemical …, 2019 - Elsevier
Abstract Background/Aims Synovial fibrosis is a pathological process that is observed in
several musculoskeletal disorders and characterized by the excessive deposition of …

Synovial fibroblasts integrate inflammatory and neuroendocrine stimuli to drive rheumatoid arthritis

T Lowin, RH Straub - Expert review of clinical immunology, 2015 - Taylor & Francis
Rheumatoid arthritis is a chronic inflammatory disease that is characterized by pannus
tissue consisting of synovial fibroblasts (SF), macrophages and lymphocytes. The …

Efficacy and safety of selective glucocorticoid receptor modulators in comparison to glucocorticoids in arthritis, a systematic review

M Safy, MJH De Hair, JWG Jacobs, F Buttgereit… - PLoS …, 2017 - journals.plos.org
Background Long-term treatment with glucocorticoids (GCs) plays an important role in the
management of arthritis patients, although the efficacy/safety balance is unfavorable …

Compound A influences gene regulation of the Dexamethasone-activated glucocorticoid receptor by alternative cofactor recruitment

SJ Desmet, N Bougarne, L Van Moortel… - Scientific reports, 2017 - nature.com
The glucocorticoid receptor (GR) is a transcription factor of which the underlying gene
regulatory mechanisms are complex and incompletely understood. The non-steroidal anti …

Novel role for receptor dimerization in post-translational processing and turnover of the GRα

L Wilkinson, N Verhoog, A Louw - Scientific reports, 2018 - nature.com
Glucocorticoids (GCs), acting via the glucocorticoid receptor (GRα), remain the mainstay
therapeutic choice for the treatment of inflammation. However, chronic GC use, aside from …

Nuclear receptors as potential drug targets in osteoarthritis

MMG Sun, F Beier, A Ratneswaran - Current Opinion in Pharmacology, 2018 - Elsevier
Highlights•Nuclear receptors (NR) are ligand-activated transcription factors.•NRs are well-
characterized pharmacologically and are promising drug targets for OA.•Recent studies …

AB0431 Post-marketing surveillance of tofacitinib in japanese patients with rheumatoid arthritis: an interim report of safety data

T Mimori, M Harigai, T Atsumi, M Kuwana, S Takei… - 2017 - ard.bmj.com
Background Tofacitinib is an oral JAK inhibitor for the treatment of rheumatoid arthritis (RA).
Efficacy and safety of tofacitinib have been shown in RA patients in global Phase 2, Phase 3 …