Mahindra, A., Millard, C. J., Black, I., Archibald, L. J., Schwabe, J. W.R. and Jamieson, A. G. (2019) Synthesis of HDAC substrate peptidomimetic inhibitors (SPIs) using Fmoc amino acids incorporating zinc-binding groups. Organic Letters, 21(9), pp. 3178-3182. (doi: 10.1021/acs.orglett.9b00885) (PMID:30998366) (PMCID:PMC6503537)
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Abstract
Syntheses of Fmoc amino acids having zinc-binding groups were prepared and incorporated into substrate inhibitor H3K27 peptides using Fmoc/tBu solid-phase peptide synthesis (SPPS). Peptide 11, prepared using Fmoc-Asu(NHOtBu)-OH, is a potent inhibitor (IC50 = 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.
| Item Type: | Articles |
|---|---|
| Status: | Published |
| Refereed: | Yes |
| Glasgow Author(s) Enlighten ID: | Archibald, Dr Lewis and Jamieson, Professor Andrew and Mahindra, Dr Amit |
| Authors: | Mahindra, A., Millard, C. J., Black, I., Archibald, L. J., Schwabe, J. W.R., and Jamieson, A. G. |
| College/School: | College of Science and Engineering College of Science and Engineering > School of Chemistry |
| Journal Name: | Organic Letters |
| Publisher: | American Chemical Society |
| ISSN: | 1523-7060 |
| ISSN (Online): | 1523-7052 |
| Published Online: | 18 April 2019 |
| Copyright Holders: | Copyright © 2019 American Chemical Society |
| First Published: | First published in Organic Letters 21(9):3178-3182 |
| Publisher Policy: | Reproduced under a Creative Commons License |
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