Ontology highlight
ABSTRACT:
SUBMITTER: Mahindra A
PROVIDER: S-EPMC6503537 | biostudies-literature | 2019 May
REPOSITORIES: biostudies-literature
Mahindra Amit A Millard Christopher J CJ Black Iona I Archibald Lewis J LJ Schwabe John W R JWR Jamieson Andrew G AG
Organic letters 20190418 9
Syntheses of Fmoc amino acids having zinc-binding groups were prepared and incorporated into substrate inhibitor H3K27 peptides using Fmoc/<sup>t</sup>Bu solid-phase peptide synthesis (SPPS). Peptide 11, prepared using Fmoc-Asu(NHO<sup>t</sup>Bu)-OH, is a potent inhibitor (IC<sub>50</sub> = 390 nM) of the core NuRD corepressor complex (HDAC1-MTA1-RBBP4). The Fmoc amino acids have the potential to facilitate the rapid preparation of substrate peptidomimetic inhibitor (SPI) libraries in the search ...[more]