Synthesis and Profiling of Highly Selective Inhibitors of Methyltransferase DOT1L Based on Carbocyclic C-Nucleosides.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c02228
Abstract: Histone methyltransferase DOT1L is an attractive therapeutic target for the treatment of hematological malignancies. Here, we report the design, synthesis, and profiling of new DOT1L inhibitors based on nonroutine carbocyclic C-nucleoside scaffolds. The experimentally observed… read more here.
Keywords: inhibitors methyltransferase; profiling highly; selective inhibitors; methyltransferase dot1l ... See more keywords
Inhibition of histone methyltransferase DOT1L silences ERα gene and blocks proliferation of antiestrogen-resistant breast cancer cells
Sign Up to like & getrecommendations! Published in 2019 at "Science Advances"
DOI: 10.1126/sciadv.aav5590
Abstract: Pharmacological inhibition of DOT1L blocks estrogen receptor signaling in breast cancer. Breast cancer (BC) resistance to endocrine therapy results from constitutively active or aberrant estrogen receptor α (ERα) signaling, and ways to block ERα pathway… read more here.
Keywords: methyltransferase dot1l; gene; dot1l; breast cancer ... See more keywords
Histone Methyltransferase DOT1L as a Promising Epigenetic Target for Treatment of Solid Tumors
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Genetics"
DOI: 10.3389/fgene.2022.864612
Abstract: The histone lysine methyltransferase DOT1L (DOT1-like histone lysine methyltransferase) is responsible for the epigenetic regulation of gene expression through specific methylation of lysine79 residue of histone H3 (H3K79) in actively transcribed genes. Its normal activity… read more here.
Keywords: cell; dot1l; methyltransferase dot1l; solid tumors ... See more keywords