Selective estrogen receptor modulators (SERMs): New alternatives for osteoarthritis?

Lugo, L.; Villalvilla, A.; Largo, Raquel; Herrero‐Beaumont, Gabriel; Roman‐Blas, Jorge A.

doi:10.1016/j.maturitas.2014.01.016

Cited by 31 publications

(30 citation statements)

References 36 publications

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“…Several studies report beneficial effects of SERMs on cartilage metabolism, in animal studies and in clinical trials [34]. SERMs had analgesic effect in those with back and knee pain, at least some of which was attributable to OA [35].…”

Section: Type Of Agent and Effect Of Newer Agentsmentioning

confidence: 99%

“…There are several excellent reviews which cover the sometimes conflicting in vitro literature [17,34,[36][37][38]. Estrogen is synthesised by aromatases in most connective tissues [39].…”

Section: Osteoarthritis Pathogenesis Estrogen and Mhtmentioning

confidence: 99%

“…Estrogen is synthesised by aromatases in most connective tissues [39]. Critically, estrogen receptors are present in all joint tissues including articular cartilage, subchondral bone and synovium [34]. In vitro studies suggest that low level estrogens may be pro-chondrogenic and anticatabolic.…”

Section: Osteoarthritis Pathogenesis Estrogen and Mhtmentioning

confidence: 99%

“…Action of estrogen on the joint may not be specific to females: it is notable that male mice treated with estrogen had less OA than untreated mice [46]. In a systematic review of 6 animal studies of SERMs, these agents gave a more consistent positive effect on articular cartilage or appeared to reduce OA changes ( [17,34].…”

Section: Osteoarthritis Pathogenesis Estrogen and Mhtmentioning

confidence: 99%

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Hand osteoarthritis, menopause and menopausal hormone therapy

Watt

2016

Maturitas

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Section: Type Of Agent and Effect Of Newer Agentsmentioning

confidence: 99%

“…There are several excellent reviews which cover the sometimes conflicting in vitro literature [17,34,[36][37][38]. Estrogen is synthesised by aromatases in most connective tissues [39].…”

Section: Osteoarthritis Pathogenesis Estrogen and Mhtmentioning

confidence: 99%

Section: Osteoarthritis Pathogenesis Estrogen and Mhtmentioning

confidence: 99%

Section: Osteoarthritis Pathogenesis Estrogen and Mhtmentioning

confidence: 99%

See 2 more Smart Citations

Hand osteoarthritis, menopause and menopausal hormone therapy

Watt

2016

Maturitas

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“…The effects of oestrogens, SERMs, bisphosphonates, calcitonin, and strontium ranelate in OA were object of different studies (14)(15)(16)44,(78)(79)(80)(81)(82)(83)(84)(85)(86)(87)(88)(89)(90)(91)(92)(93)(94)(95). Oestrogen replacement therapy failed to show a clear reduction of OA progression in postmenopausal women (14,(78)(79)(80)(81)(82)(83).…”

Section: Bone Agents In Oamentioning

confidence: 99%

An update on the up and coming therapies to treat osteoarthritis, a multifaceted disease

Roman‐Blas

Bizzi

Largo

et al. 2016

Expert Opinion on Pharmacotherapy

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Despite the renewed interest in the search of new compounds for treatment of OA, results have been limited. Novel systemic and IA administered agents are in active development. IA drug administration is particularly an attractive approach because can diminish some of the severe side effects associated with systemic drugs. Indeed, one of the most promising fields for pharmacology innovation in OA is joint injected therapy, as suggested by preliminary data from recent studies using IA sprifermin (rhFGF-18), mesenchymal stem cells or TGF-B1 transduced allogenic chondrocytes. Last, the effort to develop new drugs must be accompanied by the interest for establishing well-defined phenotypes, and only then, a more tailored therapy should be practiced in OA.

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Expression and function of the nonclassical estrogen receptor, GPR30, in human cartilage and chondrocytes

Ribeiro

Sousa

Rufino

et al. 2020

Journal Cellular Physiology

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Estrogen hormones are important for cartilage homeostasis, but nothing is known regarding the expression and role of the membrane G protein‐coupled estrogen receptor (GPER), G protein‐coupled receptor 30 (GPR30), in adult articular chondrocytes. Using immunohistochemistry of cartilage sections, quantitative real‐time polymerase chain reaction and Western blot of chondrocyte extracts, we found that these cells express GPR30. Nonetheless, the pattern of bands detected by two distinct antibodies does not overlap, suggesting that the proteins detected represent partially degraded forms of the receptor. Treatment with GPR30 agonists did not induce Akt or ERK1/2 phosphorylation, two known GPR30‐activated signaling pathways, suggesting that GPR30 is not functional in human chondrocytes. Therefore, the protective anti‐osteoarthritic role of estrogen hormones in cartilage homeostasis is likely independent of GPR30. This study was performed using human cartilage collected from the distal femoral condyles of multiorgan donors at the Bone and Tissue Bank of the University and Hospital Center of Coimbra.

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Selective estrogen receptor modulators (SERMs): New alternatives for osteoarthritis?

Cited by 31 publications

References 36 publications

Hand osteoarthritis, menopause and menopausal hormone therapy

Hand osteoarthritis, menopause and menopausal hormone therapy

An update on the up and coming therapies to treat osteoarthritis, a multifaceted disease

Expression and function of the nonclassical estrogen receptor, GPR30, in human cartilage and chondrocytes

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