Synthesis and Evaluation of Macrocyclic Peptide Aldehydes as Potent and Selective Inhibitors of the 20S Proteasome

[Image: see text] This research explores the first design and synthesis of macrocyclic peptide aldehydes as potent inhibitors of the 20S proteasome. Two novel macrocyclic peptide aldehydes based on the ring-size of the macrocyclic natural product TMC-95 were prepared and evaluated as inhibitors of t...

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Udgivet i:ACS Med Chem Lett
Main Authors: Wilson, David L., Meininger, Isabel, Strater, Zack, Steiner, Stephanie, Tomlin, Frederick, Wu, Julia, Jamali, Haya, Krappmann, Daniel, Götz, Marion G.
Format: Artigo
Sprog:Inglês
Udgivet: American Chemical Society 2016
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4789680/
https://ncbi.nlm.nih.gov/pubmed/26985310
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.5b00401
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