Rational hopping of a peptidic scaffold into non-peptidic scaffolds: structurally novel potent proteasome inhibitors derived from a natural product, belactosin A


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Please use this identifier to cite or link to this item:http://hdl.handle.net/2115/57671

Title:	Rational hopping of a peptidic scaffold into non-peptidic scaffolds: structurally novel potent proteasome inhibitors derived from a natural product, belactosin A
Authors:	Kawamura, Shuhei Browse this author
	Unno, Yuka Browse this author
	Hirokawa, Takatsugu Browse this author
	Asai, Akira Browse this author
	Arisawa, Mitsuhiro Browse this author →KAKEN DB
	Shuto, Satoshi Browse this author →KAKEN DB
Issue Date:	7-Mar-2014
Publisher:	Royal soc chemistry
Journal Title:	Chemical communications
Volume:	50
Issue:	19
Start Page:	2445
End Page:	2447
Publisher DOI:	10.1039/c3cc48818g
PMID:	24452398
Abstract:	Rational scaffold hopping of a natural product belactosin A derivative was successfully achieved based on the pharmacophore model constructed. The peptidic scaffold was replaced by significantly simplified non- peptidic scaffolds, bywhich weak belactosin A (IC50= 1440nM) was converted into highly potent non- peptidic inhibitors (IC50 = 26-393 nM).
Type:	article (author version)
URI:	http://hdl.handle.net/2115/57671
Appears in Collections:	薬学研究院 (Faculty of Pharmaceutical Sciences) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)

Submitter: 周東智

OAI-PMH ( junii2 , jpcoar_1.0 )

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