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Modulation of the inhibitor properties of dipeptidyl (acyloxy)methyl ketones toward the CaaX proteases

โœ Scribed by Anne-Marie R. Dechert; James P. MacNamara; Sarah R. Breevoort; Emily R. Hildebrandt; Ned W. Hembree; Adam C. Rea; Duncan E. McLain; Stephen B. Porter; Walter K. Schmidt; Timothy M. Dore


Book ID
108072901
Publisher
Elsevier Science
Year
2010
Tongue
English
Weight
442 KB
Volume
18
Category
Article
ISSN
0968-0896

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A weak inhibitor means faster exchange! Since the methyl ketone MK2 is a weak noncovalent peptidyl inhibitor of the human cytomegalovirus protease, exchange between the free and enzyme-bound forms is rapid. This allows for the use of transferred NOE NMR methods and molecular modeling, which show tha