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- W3165731556 abstract "SETD3 was recently identified as the histidine methyltransferase responsible for N3 -methylation of His73 of β-actin in humans. Overexpression of SETD3 is associated with several diseases, including breast cancer. Here, we report a development of actin-based peptidomimetics as inhibitors of recombinantly expressed human SETD3. Substitution of His73 by simple natural and unnatural amino acids led to selected β-actin peptides with high potency against SETD3 in MALDI-TOF MS assays. The selenomethionine-containing β-actin peptide was found to be the most potent SETD3 inhibitor (IC50 =161 nM). Supporting our inhibition assays, a combination of computational docking and molecular dynamics simulations revealed that the His73 binding pocket for β-actin in SETD3 is rigid and accommodates the inhibitor peptides with similar binding modes. Collectively, our work demonstrates that actin-based peptidomimetics can act as potent SETD3 inhibitors and provide a basis for further development of highly potent and selective inhibitors of SETD3." @default.
- W3165731556 created "2021-06-07" @default.
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- W3165731556 date "2021-06-22" @default.
- W3165731556 modified "2023-10-16" @default.
- W3165731556 title "β‐Actin Peptide‐Based Inhibitors of Histidine Methyltransferase SETD3" @default.
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- W3165731556 doi "https://doi.org/10.1002/cmdc.202100296" @default.
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