Related Experiment Video
Updated: May 22, 2026

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries
Published on: January 22, 2019
A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation
Giovanna Bergamini1, Kathryn Bell, Satoko Shimamura
1Cellzome AG, Heidelberg, Germany.
Abstract:
We devised a high-throughput chemoproteomics method that enabled multiplexed screening of 16,000 compounds against native protein and lipid kinases in cell extracts. Optimization of one chemical series resulted in CZC24832, which is to our knowledge the first selective inhibitor of phosphoinositide 3-kinase γ (PI3Kγ) with efficacy in in vitro and in vivo models of inflammation. Extensive target- and cell-based profiling of CZC24832 revealed regulation of interleukin-17-producing T helper cell (T(H)17) differentiation by PI3Kγ, thus reinforcing selective inhibition of PI3Kγ as a potential treatment for inflammatory and autoimmune diseases.
Related Concept Videos
PI3K/mTOR/AKT Signaling Pathway
The JAK-STAT Signaling Pathway

