Missing content? – Request curation!
Request curation for specific Genes, variants, or PubMed publications.
Have questions, comments or suggestions? - Let us know!
Email us at : ckbsupport@jax.org
Ref Type | |
PMID | |
Authors | Francis Burrows, Tao Wu, Linda Kessler, Shuangwei Li, Jingchuan Zhang, Patrick Zarrinkar, Liansheng Li, Tomasz Cierpicki, Jolanta Grembecka, Pingda Ren and Yi Liu |
Title | A novel small molecule menin-MLL inhibitor for potential treatment of MLL-rearranged leukemias and NPM1/DNMT3A-mutant AML |
Journal | Mol Cancer Ther |
Vol | |
Issue | |
Date | |
URL | http://mct.aacrjournals.org/content/17/1_Supplement/LB-A27 |
Abstract Text | Mol Cancer Ther 2018;17(1 Suppl):Abstract nr LB-A27 |
Molecular Profile | Treatment Approach |
---|
Gene Name | Source | Synonyms | Protein Domains | Gene Description | Gene Role |
---|
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
KO-539 | KO539|KO 539 | MEN1-KMT2A Inhibitor 5 | KO-539 is a small molecule inhibitor of MEN1 (menin)-KMT2A (MLL1) complex, which may lead to growth inhibition of KMT2A (MLL1)-positive tumor cells (Mol Cancer Ther 2018;17(1 Suppl):Abstract nr LB-A27). |
Gene | Variant | Impact | Protein Effect | Variant Description | Associated with drug Resistance |
---|
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
KMT2A rearrange | acute myeloid leukemia | predicted - sensitive | KO-539 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, KO-539 inhibited growth of KMT2A (MLL1)-rearranged acute myeloid leukemia cells in culture, and prolonged survival in cell-line xenograft models (AACR; Mol Cancer Ther 2018;17(1 Suppl):Abstract nr LB-A27). | detail... |