Document Detail

Role of HCA(2) (GPR109A) in nicotinic acid and fumaric acid ester-induced effects on the skin.
MedLine Citation:
PMID:  22743741     Owner:  NLM     Status:  Publisher    
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) HCA(2) (GPR109A) in cells of the epidermis. While the wanted effects of NA are at least in part also mediated by HCA(2), it is currently not clear whether this receptor is also involved in the anti-psoriatic effects of FAE. The HCA(2)-mediated flushing response to these drugs involves the formation of prostaglandin D(2) and E(2) 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 HCA(2)-mediated flushing, describes strategies to mitigate it and discusses the potential link between flushing, HCA(2) and the antipsoriatic effects of FAE.
Julien Hanson; Andreas Gille; Stefan Offermanns
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-6-25
Journal Detail:
Title:  Pharmacology & therapeutics     Volume:  -     ISSN:  1879-016X     ISO Abbreviation:  -     Publication Date:  2012 Jun 
Date Detail:
Created Date:  2012-6-29     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7905840     Medline TA:  Pharmacol Ther     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2012. Published by Elsevier Inc.
Molecular Pharmacology, GIGA Signal Transduction Unit, University of Liège, CHU, B34 (+4), 4000 Liège, Belgium; Medicinal Chemistry, Drug Research Center-CIRM, University of Liège, Belgium.
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