Acefylline activates filaggrin deimination by peptidylarginine deiminases in the upper epidermis

Highlights • Screening of a large chemical library identified xanthines as PAD potential activators. • Deimination of human filaggrin was enhanced by caffeine, theobromine and acefylline. • Topical application of acefylline on reconstructed human epidermis improved deimination. • Acefylline is the f...

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Veröffentlicht in:	Journal of dermatological science 2016-02, Vol.81 (2), p.101-106
Hauptverfasser:	Méchin, Marie-Claire, Cau, Laura, Galliano, Marie-Florence, Daunes-Marion, Sylvie, Poigny, Stéphane, Vidaluc, Jean-Louis, Bessou-Touya, Sandrine, Takahara, Hidenari, Serre, Guy, Duplan, Hélène, Simon, Michel
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Cutaneous Cells, Cultured Computer Simulation Dermatology Dose-Response Relationship, Drug Enzyme Activation Enzyme Activators - administration & dosage Enzyme Activators - chemistry Enzyme Activators - pharmacology Epidermal barrier Epidermal Cells Epidermis / drug effects Epidermis - cytology Epidermis - drug effects Epidermis - enzymology Filaggrin Human health and pathology Humans Humans Hydrolases / metabolism Hydrolases - metabolism Infectious diseases Intermediate Filament Proteins - chemistry Intermediate Filament Proteins - metabolism Keratinocytes - drug effects Keratinocytes - enzymology Life Sciences Models, Molecular Post-translational modification Protein Conformation Protein Processing, Post-Translational Protein-Arginine Deiminases Skin Small Molecule Libraries Structure-Activity Relationship Theophylline - administration & dosage Theophylline - analogs & derivatives Theophylline - chemistry Theophylline - pharmacology Xanthine
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Beschreibung
Zusammenfassung:	Highlights • Screening of a large chemical library identified xanthines as PAD potential activators. • Deimination of human filaggrin was enhanced by caffeine, theobromine and acefylline. • Topical application of acefylline on reconstructed human epidermis improved deimination. • Acefylline is the first identified activator of PAD1 and PAD3.
ISSN:	0923-1811 1873-569X
DOI:	10.1016/j.jdermsci.2015.11.006