- Titel
- Stafiba: A STAT5-Selective Small-Molecule Inhibitor
- Zitierfähige Url:
- https://nbn-resolving.org/urn:nbn:de:bsz:15-qucosa2-987972
- Quellenangabe
- ChemBioChem
Erscheinungsjahr: 2023
Jahrgang: 24
Heft: 1
Artikelnummer: e202200553 - Erstveröffentlichung
- 2022
- Abstract (EN)
- 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.
- Andere Ausgabe
- Link zur Erstveröffentlichung
DOI: 10.1002/cbic.202200553 - Freie Schlagwörter (EN)
- SH2 domains, biological activity, inhibitors, protein-protein interactions, transcription factors
- Klassifikation (DDC)
- 540
- Verlag
- Wiley-VCH, Weinheim
- Version / Begutachtungsstatus
- publizierte Version / Verlagsversion
- URN Qucosa
- urn:nbn:de:bsz:15-qucosa2-987972
- Veröffentlichungsdatum Qucosa
- 01.09.2025
- Dokumenttyp
- Artikel
- Sprache des Dokumentes
- Englisch
- Lizenz / Rechtehinweis
CC BY 4.0