Yeni Oral Küçük Molekül İnhibitörü RO9021 ın Dalak Tirozin Kinazı Selektif İnhibisyonuna Bağlı Doğuştan ve Adaptif İmmün Yanıt Üzerinde Ortaya Çıkan Etkiler: Otoimmün Hastalık Tedavisinde SYK Etkileri
Arthritis Research and Therapy 2013 15:R146
Spleen tyrosine kinase (SYK) has already been described as a potential therapeutic target for the treatment of autoimmune diseases. Previously the SYK inhibitor fostamatinib was in clinical development for the treatment of rheumatoid arthritis, but has since been suspended. However, investigation into SYK inhibition continues with RO2091, a novel ATP-competitive inhibitor of SYK with reasonable selectivity, potency and oral bioavailability which has been shown to suppress various innate and adaptive immune responses in vitro and in mCIA models. Following investigation in this study, including selectivity tests indicating no overlap into the JAK/STAT pathway, the authors conclude that RO2091 could serve as a promising medical lead for the design of SYK inhibitors, and could complement the current therapeutic agents in the treatment of inflammation-related and autoimmune disorders.
