[Nle20] H4 peptide (16−23) is a peptide with strong inhibitory activity against histone methyltransferase SETD8 ( K d =0.14 μM), which inhibits SETD8 's methylation of histone H4 by competing with SETD8 's substrate binding site. [Nle20] H4 peptide (16−23) can be used as a lead compound for anticancer therapy.
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