Importance of the novel organic cation transporter 1 for tyrosine kinase inhibition by saracatinib in rheumatoid arthritis synovial fibroblasts

• Published in: Scientific reports Vol. 7; no. 1; pp. 1258 - 9
• Main Authors: Harrach, Saliha, Edemir, Bayram, Schmidt-Lauber, Christian, Pap, Thomas, Bertrand, Jessica, Ciarimboli, Giuliano
• Format: Journal Article
• Language: English
• Published: London Nature Publishing Group UK 28.04.2017; Nature Publishing Group; Nature Portfolio
• Subjects: 13; 13/21; 13/89; 13/95; 14/34; 692/308/153; 692/4023/1670/498; 82/80; Arthritis, Rheumatoid - pathology; Benzodioxoles - metabolism; Cations; Cell Proliferation - drug effects; Cells, Cultured; Enzyme Inhibitors - metabolism; Fibroblasts; Fibroblasts - drug effects; Fibroblasts - physiology; Humanities and Social Sciences; Humans; Inflammatory diseases; Intracellular; multidisciplinary; Organic Cation Transport Proteins - metabolism; Organic cation transporter; pH effects; Protein-Tyrosine Kinases - antagonists & inhibitors; Quinazolines - metabolism; Rheumatoid arthritis; Science; Science (multidisciplinary); Side effects; Src protein; Tumor necrosis factor-α; Tyrosine kinase inhibitors

Recent therapeutic approaches of rheumatoid arthritis (RA) address the use of small molecules such as tyrosine kinase inhibitors (TKIs). However, the TKIs developed to date have important side effects and/or scarce efficacy in inflammatory diseases such as RA. Since intracellular effective TKIs must...