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Updated: Dec 12, 2025

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries
Published on: January 22, 2019
Research advances on selective phosphatidylinositol 3 kinase δ (PI3Kδ) inhibitors
Jiajia Sun1, Yifan Feng1, Yuan Huang1
1Department of Medicinal Chemistry, School of Pharmacy, Health Science Center, Xi'an Jiaotong University, 76 West Yanta Road, Xi'an, Shaanxi 710061, PR China.
Abstract:
PI3Kδ in B cells mediates antigen receptor signaling and promote neutrophil chemotaxis. The activation of PI3Kδ can cause mast cell maturation and degranulation, myeloid cell dysfunction, and cytokine release. As a key signal molecule, PI3Kδ interacts with the lipid binding domain of a variety of cellular proteins as a secondary messenger, ultimately affecting a series of significant cellular pathways in disease pathology. Therefore, many research organizations and pharmaceutical companies have studied it to develop effectively selective PI3Kδ inhibitors as therapeutics. This review summarizes research advances in varying chemical classes of selective PI3Kδ inhibitors and the structure-activity relationship, and it mainly focuses on the propeller- versus flat-type class of inhibitors.
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