Rapid identification of the pharmacophore in a peptoid inhibitor of the proteasome regulatory particle

Autor:	Young Chan Kim, Troy Hutchens, Hyun-Suk Lim, Chase T. Archer, Thomas Kodadek
Rok vydání:	2008
Předmět:	Models Molecular Proteasome Endopeptidase Complex Cellular activity Indoles Catalysis Structure-Activity Relationship chemistry.chemical_compound Materials Chemistry Enzyme Inhibitors Binding Sites Molecular Structure Chemistry Metals and Alloys Peptoid General Chemistry Surfaces Coatings and Films Electronic Optical and Magnetic Materials 19S Proteasome Regulatory Particle Molecular Weight Rapid identification Biochemistry Purines Ceramics and Composites Pharmacophore Proteasome Inhibitors Proteasome regulatory particle
Zdroj:	Chemical Communications. :1064
ISSN:	1364-548X 1359-7345
Popis:	Here we report a simple and effective method to identify the minimal pharmacophore in the first peptoid inhibitor of the 19S proteasome regulatory particle, which has led to the development of a derivative that exhibits improved cellular activity, presumably due to a reduction in mass of about two-fold and the elimination of positively charged lysine-like residues.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::608f4ca400357df62533285f1b3e6599 https://doi.org/10.1039/b717861a Zobrazit plný text záznamu