Epimer of amastatin at the 2-position. There are no reports of aminopeptidase inhibition by this epimer; on the contrary, there are suggestions that a 2S-hydroxyl group is important for the stability of an initial collision complex with the enzyme.
Verpackung
Bottomless glass bottle. Contents are inside inserted fused cone.
Journal of medicinal chemistry, 27(4), 417-422 (1984-04-01)
Amastatin [(2S,3R)-3-amino-2-hydroxy-5-methylhexanoyl-L-valyl-L-valyl-L- aspartic acid] and bestatin [(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl-L-leucine] are slow-binding, competitive inhibitors of aminopeptidase M (AP-M) with net inhibition constants (Ki) of 1.9 X 10(-8) and 4.1 X 10(-6) M, respectively. The effect of inhibitor structure on net Ki and on
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