Title of article
Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: Heterocyclic P3
Author/Authors
David C. Tully، نويسنده , , Hong Liu، نويسنده , , Phil B. Alper، نويسنده , , Arnab K. Chatterjee، نويسنده , , Robert Epple، نويسنده , , Michael J. Roberts، نويسنده , , Jennifer A. Williams، نويسنده , , KhanhLinh T. Nguyen، نويسنده , , David H. Woodmansee، نويسنده , , Christine Tumanut، نويسنده , , Jun Li، نويسنده , , Glen Spraggon، نويسنده , , Jonathan Chang، نويسنده , , Tove Tuntland، نويسنده , , Jennifer L. Harris، نويسنده , , Donald S. Karanewsky، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
6
From page
1975
To page
1980
Abstract
A series of Nα-2-benzoxazolyl-α-amino acid-(arylaminoethyl)amides were identified as potent, selective, and noncovalent inhibitors of cathepsin S. Structure–activity relationships including strategies for modulating the selectivities among cathepsins S, K, and L, and in vivo pharmacokinetics are discussed. A X-ray structure of compound 3 bound to the active site of cathepsin S is also reported.
Keywords
Cathepsin S , cathepsin , Cysteine protease inhibitor , Noncovalent inhibitor , peptidomimetics
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796705
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