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   Articles with "menin mll" as a keyword



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A Menin-MLL Inhibitor Induces Specific Chromatin Changes and Eradicates Disease in Models of MLL-Rearranged Leukemia.

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recommendations! Published in 2019 at "Cancer cell"

DOI: 10.1016/j.ccell.2019.11.001

Abstract: Inhibition of the Menin (MEN1) and MLL (MLL1, KMT2A) interaction is a potential therapeutic strategy for MLL-rearranged (MLL-r) leukemia. Structure-based design yielded the potent, highly selective, and orally bioavailable small-molecule inhibitor VTP50469. Cell lines carrying… read more here.

Keywords: mll; mll rearranged; menin mll; mll inhibitor ... See more keywords
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Discovery of M-1121 as an Orally Active Covalent Inhibitor of Menin-MLL Interaction Capable of Achieving Complete and Long-Lasting Tumor Regression.

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recommendations! Published in 2021 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.1c00789

Abstract: Targeting the menin-MLL protein-protein interaction is being pursued as a new therapeutic strategy for the treatment of acute leukemia carrying MLL-rearrangements (MLLr leukemia). Herein, we report M-1121, a covalent and orally active inhibitor of the… read more here.

Keywords: orally active; menin; covalent; interaction ... See more keywords
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Menin-MLL protein-protein interaction inhibitors: a patent review (2014–2021)

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recommendations! Published in 2022 at "Expert Opinion on Therapeutic Patents"

DOI: 10.1080/13543776.2022.2045947

Abstract: ABSTRACT Introduction Chromosomal translocations involving the mixed-lineage leukemia (MLL, KMT2A, MLL1) genes result in the production of MLL fusion proteins, which cause abnormal transcriptional regulation leading to acute leukemia (AL). Menin (MEN1) protein is essential… read more here.

Keywords: interaction inhibitors; menin mll; leukemia; mll ... See more keywords
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Synergistic Targeting of FLT3 Mutations in AML via Combined Menin-MLL and FLT3 Inhibition.

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recommendations! Published in 2020 at "Blood"

DOI: 10.1182/blood.2020005037

Abstract: The interaction of Menin (MEN1) and MLL (MLL1, KMT2A) is a dependency and potential therapeutic opportunity against NPM1-mutant (NPM1mut) and MLL-rearranged (MLL-r) leukemias. Concomitant activating driver mutations in the gene encoding the tyrosine kinase FLT3… read more here.

Keywords: inhibition; flt3; combined menin; menin mll ... See more keywords