Targeting interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) using a novel covalent inhibitor PRN694

Abstract

Background: ITK and RLK are unique to effector lymphocytes and critical for immune activation. Results: A novel selective covalent ITK/RLK inhibitor called PRN694 was discovered, which blocks T-cell and NK cell activation. Conclusion: PRN694 provides an effective tool to elucidate the roles of ITK and RLK in immune cell signaling. Significance: PRN694 could be an effective therapy for T-cell- or NK cell-driven autoimmune, inflammatory, and malignant diseases.