1fkn

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1fkn, resolution 1.90Å

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STRUCTURE OF BETA-SECRETASE COMPLEXED WITH INHIBITOR

Overview

Memapsin 2 (beta-secretase) is a membrane-associated aspartic protease, involved in the production of beta-amyloid peptide in Alzheimer's disease, and is a major target for drug design. We determined the crystal structure, of the protease domain of human memapsin 2 complexed to an eight-residue, inhibitor at 1.9 angstrom resolution. The active site of memapsin 2 is, more open and less hydrophobic than that of other human aspartic, proteases. The subsite locations from S4 to S2' are well defined. A kink, of the inhibitor chain at P2' and the change of chain direction of P3' and, P4' may be mimicked to provide inhibitor selectivity.

About this Structure

1FKN is a Single protein structure of sequence from Homo sapiens. The following page contains interesting information on the relation of 1FKN with [Amyloid-beta Precursor Protein]. Full crystallographic information is available from OCA.

Reference

Structure of the protease domain of memapsin 2 (beta-secretase) complexed with inhibitor., Hong L, Koelsch G, Lin X, Wu S, Terzyan S, Ghosh AK, Zhang XC, Tang J, Science. 2000 Oct 6;290(5489):150-3. PMID:11021803

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