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UnknownEvaluation of VTP-50469, a menin-MLL1 inhibitor, against Ewing sarcoma xenograft models by the pediatric preclinical testing consortium.
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S-EPMC10286575 | biostudies-literature
TranscriptomicsA novel Menin-MLL inhibitor induces specific chromatin changes and eradicates disease in models of MLL-rearranged leukemia [RNA-seq]
Cells carrying MLL-rearrangements are sensitive to treatment with VTP-50469 with IC50 in 20-60 nM. We treated MOLM13 or RS4;11 cells with DMSO (0.33%) or VTP-50469 (100-330nM), followed by digital gene expression analyses of 3'end RNA-seq data. We found that very few genes significantly change expre...
ORGANISM(S): Homo sapiens 
2019-11-06 | GSE127506 | GEO
GenomicsA novel Menin-MLL inhibitor induces specific chromatin changes and eradicates disease in models of MLL-rearranged leukemia [ChIP-seq]
Treatment of cells carrying MLL-rearrangements with VTP-50469 (specific Menin-MLL1 inhibitor) displaces Menin from high molecular weight complexes and chromatin genome-wide. Since VTP-50469 block Menin interaction with MLL1 we tested using chip-seq if treatment with VTP-50469 also displaces MLL1 or ...
ORGANISM(S): Homo sapiens 
2019-11-06 | GSE127507 | GEO
TranscriptomicsA novel Menin-MLL inhibitor induces specific chromatin changes and eradicates disease in models of MLL-rearranged leukemia
Inhibition of the Menin (encoded by MEN1) and MLL1 (KMT2A) protein-protein interaction has been proposed as a potential targeted therapeutic strategy for MLL-rearranged (MLL-r) leukemia. We sought to develop more potent and selective Menin-MLL1 interaction inhibitors that are effective in vitro and ...
ORGANISM(S): Homo sapiens 
2019-02-28 | GSE127298 | GEO
GenomicsIKAROS and MENIN are Functionally Cooperative Therapeutic Targets in Acute Myeloid Leukemia [CUT&RUN]
Using CUT&RUN-seq we examined the chromatin occupancy of IKAROS, H3K27-acetylation and CTCF in steady-state growth conditions. IKAROS chromatin occupancy was also assessed after drug-treatment with CC220, VTP-50469 or the drug combination and compared to a DMSO-vehicle treated control.
ORGANISM(S): Homo sapiens 
2022-03-10 | GSE168460 | GEO
ProteomicsIKAROS and MENIN are Functionally Cooperative Therapeutic Targets in Acute Myeloid Leukemia
Genome-scale functional genetic screening was utilized to identify resistance mechanisms and synthetic lethal interactions during small molecule targeting of MENIN and DOT1L in MLL1-rearranged AML. Chromatin regulatory complexes are found to modulate the therapeutic response to these inhibitors, and...
ORGANISM(S): Homo sapiens (Human) 
2022-03-11 | PXD025229 | Pride
Ikzf1 Kmt2a Menin Mll1 Ikaros Acute myeloid leukemia Dot1l Imid Lenalidomide Men1 
ProteomicsIKAROS and MENIN are Functionally Cooperative Therapeutic Targets in Acute Myeloid Leukemia
Genome-scale functional genetic screening was utilized to identify resistance mechanisms and synthetic lethal interactions during small molecule targeting of MENIN and DOT1L in MLL1-rearranged AML. Chromatin regulatory complexes are found to modulate the therapeutic response to these inhibitors, and...
ORGANISM(S): Homo sapiens (Human) 
2022-03-11 | PXD025228 | Pride
Ikzf1 Kmt2a Menin Mll1 Ikaros Acute myeloid leukemia Dot1l Imid Lenalidomide Men1 
ProteomicsIKAROS and MENIN are Functionally Cooperative Therapeutic Targets in Acute Myeloid Leukemia
Genome-scale functional genetic screening was utilized to identify resistance mechanisms and synthetic lethal interactions during small molecule targeting of MENIN and DOT1L in MLL1-rearranged AML. Chromatin regulatory complexes are found to modulate the therapeutic response to these inhibitors, and...
ORGANISM(S): Homo sapiens (Human) 
2022-03-11 | PXD025227 | Pride
Ikzf1 Kmt2a Menin Mll1 Ikaros Acute myeloid leukemia Dot1l Imid Lenalidomide Men1 
ProteomicsIKAROS and MENIN are Functionally Cooperative Therapeutic Targets in Acute Myeloid Leukemia
Genome-scale functional genetic screening was utilized to identify resistance mechanisms and synthetic lethal interactions during small molecule targeting of MENIN and DOT1L in MLL1-rearranged AML. Chromatin regulatory complexes are found to modulate the therapeutic response to these inhibitors, and...
ORGANISM(S): Homo sapiens (Human) 
2022-03-11 | PXD025231 | Pride
Ikzf1 Kmt2a Menin Mll1 Ikaros Acute myeloid leukemia Dot1l Imid Lenalidomide Men1 
ProteomicsIKAROS and MENIN are Functionally Cooperative Therapeutic Targets in Acute Myeloid Leukemia
Genome-scale functional genetic screening was utilized to identify resistance mechanisms and synthetic lethal interactions during small molecule targeting of MENIN and DOT1L in MLL1-rearranged AML. Chromatin regulatory complexes are found to modulate the therapeutic response to these inhibitors, and...
ORGANISM(S): Homo sapiens (Human) 
2022-03-11 | PXD025230 | Pride
Ikzf1 Kmt2a Menin Mll1 Ikaros Acute myeloid leukemia Dot1l Imid Lenalidomide Men1 
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