Novel STAT3 Inhibitors Targeting STAT3 Dimerization by Binding to the STAT3 SH2 Domain

• Main Authors: Yaping Hua (Author), Xing Yuan (Author), Yun-heng Shen (Author), Jinxin Wang (Author), Waqas Azeem (Author), Shuo Yang (Author), Alexandra Gade (Author), Seyed Mohammad Lellahi (Author), Anne Margrete Øyan (Author), Xisong Ke (Author), Wei-dong Zhang (Author), Karl-Henning Kalland (Author)
• Format: Book
• Published: Frontiers Media S.A., 2022-05-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Our drug discovery model has identified two novel STAT3 SH2 domain inhibitors 323-1 and 323-2 (delavatine A stereoisomers) in a series of experiments. In silico computational modeling, drug affinity responsive target stability (DARTS), and fluorescence polarization (FP) assays altogether determined...