Noncovalent tripeptidyl benzyl-and cyclohexyl-amine inhibitors of the cysteine protease caspase-1
…, G Abbenante, PK Madala, M Halili, GT Le…
Index: Le, Giang Thanh; Abbenante, Giovanni; Madala, Praveen K.; Hoang, Huy N.; Fairlie, David P. Journal of the American Chemical Society, 2006 , vol. 128, # 38 p. 12396 - 12397
Full Text: HTML
Citation Number: 17
Abstract
Potent and noncovalent inhibitors of caspase-1 were produced by incorporating a secondary amine (reduced amide) isostere in place of the conventional electrophile (eg, aldehyde) that normally confers high potency to cysteine protease inhibitors. Benzyl-or cyclohexylamines produced potent, reversible, and competitive inhibitors that were selective for caspase-1 (eg, K i= 47 nM) over caspases 3 and 8 with minimal cytotoxicity. Unlike ...
Related Articles:
[Ji, Weidong; Li, Najun; Chen, Dongyun; Qi, Xiuxiu; Sha, Wenwei; Jiao, Yang; Xu, Qingfeng; Lu, Jianmei Journal of Materials Chemistry B, 2013 , vol. 1, # 43 p. 5942 - 5949]
[Vadola, Paul A.; Sames, Dalibor Journal of Organic Chemistry, 2012 , vol. 77, # 18 p. 7804 - 7814,11]
Masking nanoparticle surfaces for sensitive and selective colorimetric detection of proteins
[Zhao, Qiang; Gao, Jie Chemical Communications, 2013 , vol. 49, # 70 p. 7720 - 7722]
A novel fluorometric ultramicro determination of serum. GAMMA.-glutamyltranspeptidase activity.
[Sekine; Itakura; Namihisa; Takahashi; Nakayama; Kanaoka Chemical and Pharmaceutical Bulletin, 1981 , vol. 29, # 11 p. 3286 - 3289]
[Rafiee, Ezzat; Fakhri, Akram; Joshaghani, Mohammad Journal of Heterocyclic Chemistry, 2013 , vol. 50, # 5 p. 1121 - 1128]