Author/Authors :
Avdhoot D. Velankar، نويسنده , , Gianluca Quintini، نويسنده , , Arati Prabhu، نويسنده , , Alexander Weber، نويسنده , , Gundula Hunaeus، نويسنده , , Britta Voland، نويسنده , , Monika Wuest، نويسنده , , Christian Orjeda، نويسنده , , Dipak Harel، نويسنده , , Shaji Varghese، نويسنده , , Vikas Gore، نويسنده , , Meenal Patil، نويسنده , , Deepak Gayke، نويسنده , , Matthias Herdemann، نويسنده , , Isabelle Heit، نويسنده , , Andrea Zaliani، نويسنده ,
Abstract :
Interleukin-2 inducible T-cell kinase (ITK) is one of five kinases that belong to the Tec kinase family that plays an important role in T-cell and mast cell signaling. Various reports point to a role of ITK in the treatment of allergic asthma. For example, it was shown that mice lacking ITK have reduced airway hyperresponsiveness, inflammation and tracheal responses in an allergic asthma model. In this article, we disclose novel ITK inhibitors based on (4 or 5-aryl)pyrazolyl-indole scaffold that were also found to be selective for ITK over other kinases like IRK, CDK2, GSK3ß and PKA.
Keywords :
ITK , Interleukin-2 inducible T-cell kinase , Tec kinase , Pyrazolyl-indole
