1fkn

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(New page: 200px<br /> <applet load="1fkn" size="450" color="white" frame="true" align="right" spinBox="true" caption="1fkn, resolution 1.90&Aring;" /> '''STRUCTURE OF BETA-S...)
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'''STRUCTURE OF BETA-SECRETASE COMPLEXED WITH INHIBITOR'''<br />
'''STRUCTURE OF BETA-SECRETASE COMPLEXED WITH INHIBITOR'''<br />
==Overview==
==Overview==
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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.
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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==
==About this Structure==
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1FKN is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. The following page contains interesting information on the relation of 1FKN with [[http://pdb.rcsb.org/pdb/static.do?p=education_discussion/molecule_of_the_month/pdb79_1.html Amyloid-beta Precursor Protein]]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1FKN OCA].
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1FKN is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. The following page contains interesting information on the relation of 1FKN with [[http://pdb.rcsb.org/pdb/static.do?p=education_discussion/molecule_of_the_month/pdb79_1.html Amyloid-beta Precursor Protein]]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1FKN OCA].
==Reference==
==Reference==
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[[Category: Terzyan, S.]]
[[Category: Terzyan, S.]]
[[Category: Wu, S.]]
[[Category: Wu, S.]]
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[[Category: Zhang, X.C.]]
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[[Category: Zhang, X C.]]
[[Category: alzheimer's disease]]
[[Category: alzheimer's disease]]
[[Category: aspartic protease]]
[[Category: aspartic protease]]
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[[Category: memapsin 2]]
[[Category: memapsin 2]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 16:54:23 2007''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 12:39:41 2008''

Revision as of 10:39, 21 February 2008


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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