A Novel Potent and Selective GCN2 Inhibitor, APL-4098, Has Antileukemic Activity through Dysregulation of Mitochondrial Function
APL-4098 is a novel, potent and selective GCN2 inhibitor with strong preclinical efficacy against AML cells, including LSCs. Our findings support APL-4098 as a promising candidate for AML treatment.
Authors
- Bianca Perfler (ORCID: https://orcid.org/0009-0007-2302-301X)
- Mónica Román-Trufero
- Matthew John Fuchter (ORCID: https://orcid.org/0000-0002-1767-7072)
- Armin Zebisch (ORCID: https://orcid.org/0000-0002-4861-7021)
- Kevin Blighe (ORCID: https://orcid.org/0000-0002-6322-6571)
- Claire Seydoux (ORCID: https://orcid.org/0000-0003-3263-086X)
- Gavin A. Whitlock
- Holger W. Auner (ORCID: https://orcid.org/0000-0003-4040-0642)
- Richard Butt
- Nadine Clemo
Institutions
- Nissan (United Kingdom) (GB)
- BioClinica (United States) (US)
- Medical University of Graz (AT)
- Centre Hospitalier Universitaire Vaudois (CH)
- University of Oxford (GB)
- Mission Therapeutics (United Kingdom) (GB)
- NIHR Imperial Biomedical Research Centre (GB)
- Imperial College London (GB)
- University of Lausanne (CH)
Publication Details
- Journal
- Clinical Cancer Research
- Published
- 2026-02-23
- DOI
- https://doi.org/10.1158/1078-0432.ccr-25-1444
- Primary Topic
- Protein Degradation and Inhibitors
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- Jazz Pharmaceuticals
- Astellas Pharma
- Karl-Franzens-Universität Graz
- Medizinische Universität Graz
- Servier
- Daiichi Sankyo Europe