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Stafiba: A STAT5-Selective Small-Molecule Inhibitor.

ABSTRACT: The transcription factors STAT5a and STAT5b are constitutively active in many human tumors. Combined inhibition of both STAT5 proteins is a valuable approach with promising applications in tumor biology. We recently reported resorcinol bisphosphate as a moderately active inhibitor of the protein-protein interaction domains, the SH2 domains, of both STAT5a and STAT5b. Here, we describe the development of resorcinol bisphosphate to Stafiba, a phosphatase-stable inhibitor of STAT5a and STAT5b with activity in the low micromolar concentration range. Our data provide insights into the structure-activity relationships of resorcinol bisphosphates and the corresponding bisphosphonates for use as inhibitors of both STAT5a and STAT5b.

SUBMITTER: Eckhardt KS 

PROVIDER: S-EPMC10099813 | biostudies-literature | 2023 Jan

REPOSITORIES: biostudies-literature

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Stafiba: A STAT5-Selective Small-Molecule Inhibitor.

Eckhardt Katrin S KS   Münzel Theresa T   Gräb Julian J   Berg Thorsten T  

Chembiochem : a European journal of chemical biology 20221124 1

The transcription factors STAT5a and STAT5b are constitutively active in many human tumors. Combined inhibition of both STAT5 proteins is a valuable approach with promising applications in tumor biology. We recently reported resorcinol bisphosphate as a moderately active inhibitor of the protein-protein interaction domains, the SH2 domains, of both STAT5a and STAT5b. Here, we describe the development of resorcinol bisphosphate to Stafiba, a phosphatase-stable inhibitor of STAT5a and STAT5b with  ...[more]