(R)‐PFI‐2 Analogues as Substrates and Inhibitors of Histone Lysine Methyltransferase SETD7
Miriam R. B. Porzberg,
Danny C. Lenstra,
Eddy Damen
et al.
Abstract:(R)‐PFI‐2 is a histone substrate‐competitive inhibitor of the human histone lysine monomethyltransferase SETD7. Aimed at developing potent inhibitors of SETD7 that can also act as small molecule substrates, we replaced the pyrrolidine ring of (R)‐PFI‐2 with several side chains bearing nucleophilic functional groups. We explored the inhibitory activity of 20 novel (R)‐PFI‐2 analogues, and found that the most potent analogue has a hydroxyethyl side chain (7). SETD7’s ability to catalyse methylation of (R)‐PFI‐2‐… Show more
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