Effect of PPADS on achondroplasic chondrocytes: inhibition of FGF receptor type 3 over-activity - PubMed (original) (raw)
. 2008 Apr 14;584(1):72-7.
doi: 10.1016/j.ejphar.2008.02.002. Epub 2008 Feb 12.
Affiliations
- PMID: 18336810
- DOI: 10.1016/j.ejphar.2008.02.002
Effect of PPADS on achondroplasic chondrocytes: inhibition of FGF receptor type 3 over-activity
Ana Guzmán-Aránguez et al. Eur J Pharmacol. 2008.
Abstract
Achondroplasia, results from a mutation in the FGF receptor type 3, leading to receptor hyperactivation and subsequent amplification of FGF receptor type 3 signals. We have tested the ability of pyridoxal-5'-phosphate-6-azophenyl-2', 4'-disulfonate (PPADS) to decrease the overactivation and signalling of FGF receptor type 3 in achondroplasic chondrocytes. PPADS reduced the tyrosine phosphorylation of FGF receptor type 3 triggered by fibroblast growth factor 9 (FGF9) (50% reduction), as well as the activation of extracellular signal-regulated kinases 1 and 2 (ERK1/2) pathway. As a consequence of this inhibitory effect on ERK1/2 activity the loss of extracellular matrix was also reversed by PPADS. The action of PPADS seems to be due to a mechanism independent of P2 receptor antagonism.
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