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  • Title: Synthesis of analogues of the carboxyl protease inhibitor pepstatin. Effect of structure in subsite P3 on inhibition of pepsin.
    Author: Rich DH, Bernatowicz MS.
    Journal: J Med Chem; 1982 Jul; 25(7):791-5. PubMed ID: 6809942.
    Abstract:
    A series of pepstatin analogues having minimum structural requirements for tight-binding inhibition has been synthesized and tested on porcine pepsin. Subtle changes in the geometry and size of side chains at the valine-1 position of pepstatin were found to dramatically affect inhibitor potency as well a the type of kinetic behavior observed. The inhibitors reported here can be grouped into two categories: the more potent inhibitors are slow-binding inhibitors, i.e., exhibit slow, time-dependent inhibition: the weaker inhibitors, with Ki values greater than 10(-8) M, are not time-dependent inhibitors. A minimum kinetic mechanism is proposed to account for the observed kinetic behavior.
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