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Role of HCA2 (GPR109A) in nicotinic acid and fumaric acid ester-induced effects on the skin

Nicotinic acid (NA) and fumaric acid esters (FAE) such as monomethyl fumarate or dimethyl fumarate are drugs that elicit a cutaneous reaction called flushing as a side effect. NA is used to reduce progression of atherosclerosis through its anti-dyslipidemic activity and lipid-independent mechanisms i...

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Bibliographische Detailangaben
Hauptverfasser: Hanson, Julien (VerfasserIn) , Gille, Andreas (VerfasserIn) , Offermanns, Stefan (VerfasserIn)
Dokumenttyp: Article (Journal)
Sprache:Englisch
Veröffentlicht: 26 June 2012
In: Pharmacology & therapeutics
Year: 2012, Jahrgang: 136, Heft: 1, Pages: 1-7
ISSN:1879-016X
DOI:10.1016/j.pharmthera.2012.06.003
Online-Zugang:Verlag, Volltext: http://dx.doi.org/10.1016/j.pharmthera.2012.06.003
Verlag, Volltext: http://linkinghub.elsevier.com/retrieve/pii/S0163725812001210
Volltext
Verfasserangaben:Julien Hanson, Andreas Gille, Stefan Offermanns
Beschreibung
Zusammenfassung:Nicotinic acid (NA) and fumaric acid esters (FAE) such as monomethyl fumarate or dimethyl fumarate are drugs that elicit a cutaneous reaction called flushing as a side effect. NA is used to reduce progression of atherosclerosis through its anti-dyslipidemic activity and lipid-independent mechanisms involving immune cells, whereas FAE are used to treat psoriasis via largely unknown mechanisms. Both, NA and FAE, induce flushing by the activation of the G-protein-coupled receptor (GPCR) Hydroxy-carboxylic acid receptor 2 (HCA2, GPR109A) in cells of the epidermis. While the wanted effects of NA are at least in part also mediated by HCA2, it is currently not clear whether this receptor is also involved in the anti-psoriatic effects of FAE. The HCA2‐mediated flushing response to these drugs involves the formation of prostaglandins D2 and E2 by Langerhans cells and keratinocytes via COX-1 in Langerhans cells and COX-2 in keratinocytes. This review summarizes recent progress in the understanding of the mechanisms underlying HCA2-mediated flushing, describes strategies to mitigate it and discusses the potential link between flushing, HCA2 and the anti-psoriatic effects of FAE.
Beschreibung:Im Titel ist die Zahl 2 tiefgestellt
Available online 26 June 2012
Gesehen am 26.07.2018
Beschreibung:Online Resource
ISSN:1879-016X
DOI:10.1016/j.pharmthera.2012.06.003

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