Alkynyl phosphates are potent inhibitors of serine enzyme
Open Access
- 26 August 1996
- journal article
- Published by Wiley in FEBS Letters
- Vol. 392 (2) , 117-120
- https://doi.org/10.1016/0014-5793(96)00795-8
Abstract
Propynyl, hexynyl and t‐butylethynyl diethyl phosphates were found to be very powerful covalent inhibitors of serine enzymes. Esterases were inhibited with second‐order rate constants of 107–108 M−1 min−1. Most proteases were inhibited with a rate constant of 104–105 M−1 min−1. By inhibiting chymotrypsin with (3‐14C)‐1‐propynyl diethyl phosphate, it was established that inhibition was caused by binding of the phosphate group to the enzyme active site.Keywords
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