Synthesis of HDAC Substrate Peptidomimetic Inhibitors Using Fmoc Amino Acids Incorporating Zinc-Binding Groups
| Autor: | Lewis J. Archibald, Andrew G. Jamieson, Amit Mahindra, Iona Black, Christopher J. Millard, John W.R. Schwabe |
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| Rok vydání: | 2019 |
| Předmět: |
Peptidomimetic
Stereochemistry Peptide Stereoisomerism 010402 general chemistry 01 natural sciences Biochemistry chemistry.chemical_compound Coordination Complexes Nickel Solid-Phase Synthesis Techniques Peptide synthesis RBBP4 Amino Acids Physical and Theoretical Chemistry Chelating Agents chemistry.chemical_classification Fluorenes 010405 organic chemistry Organic Chemistry Substrate (chemistry) 0104 chemical sciences 3. Good health Histone Deacetylase Inhibitors Zinc chemistry Peptidomimetics Corepressor |
| Zdroj: | Organic Letters. 21:3178-3182 |
| ISSN: | 1523-7052 1523-7060 |
| Popis: | [Image: see text] Syntheses of Fmoc amino acids having zinc-binding groups were prepared and incorporated into substrate inhibitor H3K27 peptides using Fmoc/(t)Bu solid-phase peptide synthesis (SPPS). Peptide 11, prepared using Fmoc-Asu(NHO(t)Bu)-OH, is a potent inhibitor (IC(50) = 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 for selective HDAC inhibitors. |
| Databáze: | OpenAIRE |
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