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Design of substrate-based inhibitors of human beta-secretase.

Abstract：

:By use of the effectively cleaved beta-secretase (BACE) substrate (1), incorporation of a statine in P(1) resulted in a weak inhibitor 13 of the enzyme. Further substitution of P(1)'-Asp by P(1)'-Val in 13 results in a potent inhibitor 22 of BACE. Removal of the P(10)-P(5) residues on the N-terminal part of inhibitor 22 resulted in no loss of potency (23). C-terminal truncations of inhibitor 22 generally led to significant loss of potency.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Tung JS,Davis DL,Anderson JP,Walker DE,Mamo S,Jewett N,Hom RK,Sinha S,Thorsett ED,John V

doi

10.1021/jm0155695

keywords:

subject

Has Abstract

pub_date

2002-01-17 00:00:00

pages

259-62

issue

2

eissn

0022-2623

issn

1520-4804

pii

jm0155695

journal_volume

45

pub_type

杂志文章

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