peptide-like structure.
Heterocyclicaminoacids and related compounds have been used to prepare synthetic DNA-encoded compound libraries for the discovery of small molecule protein ligands [23][24][25]. Recently, a highly specific and potent p38α kinase inhibitor containing a 3-amino-1-phenyl-1H-pyrazole
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Graphical Abstract
Figure 1:
Examples of amino-functionalized 1,2-oxazole derivatives I–VIII.
Beilstein J. Org. Chem.2020,16, 60–70, doi:10.3762/bjoc.16.8
systematically increased the number of binding motifs, and thus achieved sequence-specific binding [6][7][8][9]. Selectively binding polyamides adopt an antiparallel hairpin structure where a base pair of the DNA is addressed by a pair of the heterocyclicaminoacids in the hairpin assembly. Overall, specific
required because this allowed for an alignment between hydrogen-bonding groups in long polyamides and in the minor groove of DNA [41].
The Fmoc-protected heterocyclicaminoacids 2 were obtained from N-methylpyrrole and N-methylimidazole, respectively (Scheme 2A). The N-terminal N-methylpyrrole and N
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Graphical Abstract
Scheme 1:
Pyrrole–imidazole–azobenzene polyamides and the dsDNA target sequences employed in this study.