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Phosphinic acid-based inhibitors of tubulin polyglutamylases

✍ Scribed by Liu, Yanjie; Garnham, Christopher P.; Roll-Mecak, Antonina; Tanner, Martin E.


Book ID
122940274
Publisher
Elsevier Science
Year
2013
Tongue
English
Weight
870 KB
Volume
23
Category
Article
ISSN
0960-894X

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Phosphinic acid inhibitors of matrix met
✍ Charles G. Caldwell; Soumya P. Sahoo; Scott A. Polo; Randall R. Eversole; Thomas πŸ“‚ Article πŸ“… 1996 πŸ› Elsevier Science 🌐 English βš– 322 KB

The matrix metalloproteinase stromelysin-1 (MMP-3) is inhibited more strongly by peptidyl phosphinic acid 7 than by its corresponding phosphonamidate and phosphonate analogs. Extending a benzyl group at PI' to a phenylethyl group in 8 further increases the potency (Ki = 1.4 nM). Enhanced potency wit