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.
- Standort
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Deutsche Nationalbibliothek Frankfurt am Main
- Umfang
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Online-Ressource
- Sprache
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Englisch
- Erschienen in
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Stafiba: A STAT5‐Selective Small‐Molecule Inhibitor ; day:24 ; month:11 ; year:2022 ; extent:1
ChemBioChem ; (24.11.2022) (gesamt 1)
- Urheber
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Eckhardt, Katrin S.
Münzel, Theresa
Gräb, Julian
Berg, Thorsten
- DOI
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10.1002/cbic.202200553
- URN
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urn:nbn:de:101:1-2022112414484665854862
- Rechteinformation
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Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Letzte Aktualisierung
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15.08.2025, 07:29 MESZ
Datenpartner
Deutsche Nationalbibliothek. Bei Fragen zum Objekt wenden Sie sich bitte an den Datenpartner.
Beteiligte
- Eckhardt, Katrin S.
- Münzel, Theresa
- Gräb, Julian
- Berg, Thorsten
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