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Synthesis of HDAC Substrate Peptidomimetic Inhibitors Using Fmoc Amino Acids Incorporating Zinc-Binding Groups

[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 co...

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Detalles Bibliográficos
Autores principales: Mahindra, Amit, Millard, Christopher J., Black, Iona, Archibald, Lewis J., Schwabe, John W. R., Jamieson, Andrew G.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2019
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6503537/
https://www.ncbi.nlm.nih.gov/pubmed/30998366
http://dx.doi.org/10.1021/acs.orglett.9b00885