Design, synthesis, and structure–activity relationship study of epoxysuccinyl–peptide derivatives as cathepsin B inhibitors
Cathepsin B is a lysosomal cysteine protease involved in many diseases. The present research demonstrates that derivatives of epoxysuccinyl–peptide are effective and selective cathepsin B inhibitors. We synthesized a series of epoxysuccinyl–peptide deriva
Zhang, Xiaoye,Yang, Xiaohong,Wang, Hongqiang,Li, Song,Guo, Kun,Jiang, Dan,Xiao, Junhai,Liang, Di
p. 1240 - 1246
(2017/08/09)
COMPOSITIONS AND METHODS FOR SYNTHESIZING (2S,3S)-TRANS-EPOXYSUCCINYL-L-LEUCYL-AMIDO-3-METHYLBUTANE ETHYL ESTER
In alternative embodiments the invention provides methods for synthesizing AB-007 (also called loxistatin, E64d, EST or ((2S,3S)-trans-epoxysuccinyl-L-leucyl-amido-3-methylbutane ethyl ester) and its acid form E64c (loxistatin acid), and various synthetic
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Paragraph 0057
(2017/07/06)
An improved preparation of the activity-based probe JPM-OEt and in situ applications
A short, stereoselective synthesis of the general, cell permeable cathepsin probe JPM-OEt, is presented. The synthetic route is improved and described in more detail than previous reports for related compounds. This serves as a facile method for the synth
Chehade, Kareem A. H.,Baruch, Amos,Verhelst, Steven H. L.,Bogyo, Matthew
p. 240 - 244
(2007/10/03)
Efficient synthetic method for ethyl (+)-(2S,3S)-3-[(S)-3-methyl-1-(3-methylbutylcarbamoyl)butylcarbam oyl]-2-oxiranecarboxylate (EST), a new inhibitor of cysteine proteinases
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Tamai,Yokoo,Murata,Oguma,Sota,Sato,Kanaoka
p. 1098 - 1104
(2007/10/02)
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