Title of article
Design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 1
Author/Authors
Hong Liu، نويسنده , , David C. Tully، نويسنده , , Robert Epple، نويسنده , , Badry Bursulaya، نويسنده , , Jun Li، نويسنده , , Jennifer L. Harris، نويسنده , , Jennifer A. Williams، نويسنده , , Ross Russo، نويسنده , , Christine Tumanut، نويسنده , , Michael J. Roberts، نويسنده , , Phil B. Alper، نويسنده , , Yun He، نويسنده , , Donald S. Karanewsky، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
6
From page
4979
To page
4984
Abstract
A series of Nα-acyl-α-amino acid-(arylaminoethyl)amides were found to be potent and noncovalent cathepsin S inhibitors. Compound 20 possessed high cathepsin S affinity (Ki = 3.3 nM) and showed excellent selectivity over cathepsin K, L, F, and V. Molecular modeling, design, synthesis, and in vitro activity are described.
Keywords
Cathepsin S , cathepsin , peptidomimetics , Noncovalent inhibitors , Cysteine protease inhibitor
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796113
Link To Document