التفاصيل البيبلوغرافية
| العنوان: |
Potent dipeptidylketone inhibitors of the cysteine protease cathepsin K |
| المؤلفون: |
Ward W. Smith, Thaddeus A. Tomaszek, Cheryl A. Janson, Baoguang Zhao, Mark Alan Levy, Dennis S. Yamashita, Sherin S. Abdel-Meguid, Ru Yu, Yen Jack Hwekwo, Daniel F. Veber, Scott K. Thompson, Thomas Joseph Carr, Robert W. Marquis, Karla J. D'Alessio, Carl F. Ijames, Michael S. McQueney, Hye-Ja Oh |
| المصدر: |
Bioorganic & Medicinal Chemistry. 7:581-588 |
| بيانات النشر: |
Elsevier BV, 1999. |
| سنة النشر: |
1999 |
| مصطلحات موضوعية: |
Models, Molecular, Stereochemistry, Cathepsin L, Cathepsin K, Clinical Biochemistry, Pharmaceutical Science, Cysteine Proteinase Inhibitors, Biochemistry, Cathepsin A, Cathepsin B, Cathepsin C, Cathepsin O, Cathepsin H, Cathepsin L1, Endopeptidases, Drug Discovery, Molecular Biology, Cathepsin S, Chemistry, Organic Chemistry, Ketones, Cathepsins, Cysteine Endopeptidases, Kinetics, Models, Chemical, Molecular Medicine |
| الوصف: |
Cathepsin K (EC 3.4.22.38) is a cysteine protease of the papain superfamily which is selectively expressed within the osteoclast. Several lines of evidence have pointed to the fact that this protease may play an important role in the degradation of the bone matrix. Potent and selective inhibitors of cathepsin K could be important therapeutic agents for the control of excessive bone resorption. Recently a series of peptide aldehydes have been shown to be potent inhibitors of cathepsin K. In an effort to design more selective and metabolically stable inhibitors of cathepsin K, a series of electronically attenuated alkoxymethylketones and thiomethylketones inhibitors have been synthesized. The X-ray co-crystal structure of one of these analogues in complex with cathepsin K shows the inhibitor binding in the primed side of the enzyme active site with a covalent interaction between the active site cysteine 25 and the carbonyl carbon of the inhibitor. © |
| تدمد: |
0968-0896 |
| DOI: |
10.1016/s0968-0896(99)00011-5 |
| URL الوصول: |
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::982f16a2419ee5ecc999e28f282ce276
https://doi.org/10.1016/s0968-0896(99)00011-5 |
| Rights: |
CLOSED |
| رقم الانضمام: |
edsair.doi.dedup.....982f16a2419ee5ecc999e28f282ce276 |
| قاعدة البيانات: |
OpenAIRE |