Biaryl Phosphates and Phosphonates as Selective Inhibitors of the Transcription Factor STAT4.

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Tác giả: Angela Berg, Thorsten Berg, Nadiya Brovchenko, Julian Gräb, Theresa Münzel, Kalaiselvi Natarajan, Christoph Protzel, Sabine Schubert

Ngôn ngữ: eng

Ký hiệu phân loại:

Thông tin xuất bản: Germany : Angewandte Chemie (International ed. in English) , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 694798

The transcription factor STAT4 has been implicated in the pathogenesis of autoimmune diseases including inflammatory bowel disease, multiple sclerosis, rheumatoid arthritis and diabetes mellitus. Here, we report p-biaryl phosphates and phosphonates as the first small-molecule inhibitors of STAT4. The most potent p-biaryl phosphate inhibited the protein-protein interaction domain of STAT4, the SH2 domain, with submicromolar potency (Ki = 0.35 µM) and 14-fold selectivity over the closely related family member STAT3, which has the same core peptide binding motif as STAT4. Further development resulted in the phosphatase-stable inhibitor Stafori-1, which protected STAT4, but not STAT3, against thermal denaturation in cell lysates. Its cell-permeable prodrug Pomstafori-1 selectively inhibited STAT4 phosphorylation in cultured human cells at low micromolar concentrations. Our data open up the possibility of exploring STAT4 as a target protein for small molecules in the treatment of unmet medical needs.
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