NFE2 and PF4 as biomarkers for BET inhibition-induced thrombocytopenia in preclinical and clinical studies
The consistent downregulation of GATA1, NFE2, and PF4 transcription within hours post-BMS-986158 treatment in both preclinical and clinical studies demonstrates that BET inhibitors induce thrombocytopenia by altering GATA1 gene expression and its downstream genes, NFE2 and PF4, which regulate megakaryopoiesis and thrombopoiesis. Early detection of transcriptional changes in blood samples during treatment courses positions NFE2 and PF4 as promising biomarkers for proactively monitoring and mitigating treatment-emergent thrombocytopenia.
Authors
- Oriana Esposito (ORCID: https://orcid.org/0000-0003-0751-3389)
- Jennifer L. Price
- Karen Augustine‐Rauch
- Shodeinde Coker (ORCID: https://orcid.org/0000-0003-2263-5923)
- Cindy Zhang (ORCID: https://orcid.org/0000-0002-0243-7842)
- Richard A. Westhouse
- Ke Xu (ORCID: https://orcid.org/0000-0002-2796-6177)
- Faye Wang
- Danielle M. Greenawalt
- Julie Panzica
Institutions
- Bristol-Myers Squibb (Sweden) (SE)
Publication Details
- Journal
- Frontiers in Medicine
- Published
- 2025-08-27
- DOI
- https://doi.org/10.3389/fmed.2025.1592693
- Primary Topic
- Protein Degradation and Inhibitors
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- Bristol-Myers Squibb