4ke0

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'''Unreleased structure'''
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{{STRUCTURE_4ke0| PDB=4ke0 | SCENE= }}
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===Crystal structure of BACE1 in complex with hydroxyethylamine-macrocyclic inhibitor 13===
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{{ABSTRACT_PUBMED_23769639}}
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The entry 4ke0 is ON HOLD until Paper Publication
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==Function==
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[[http://www.uniprot.org/uniprot/BACE1_HUMAN BACE1_HUMAN]] Responsible for the proteolytic processing of the amyloid precursor protein (APP). Cleaves at the N-terminus of the A-beta peptide sequence, between residues 671 and 672 of APP, leads to the generation and extracellular release of beta-cleaved soluble APP, and a corresponding cell-associated C-terminal fragment which is later released by gamma-secretase.<ref>PMID:10677483</ref> <ref>PMID:20354142</ref>
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Authors: Whittington, D.A., Long, A.M., Li, V.
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==About this Structure==
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[[4ke0]] is a 3 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4KE0 OCA].
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Description: Crystal structure of BACE1 in complex with hydroxyethylamine-macrocyclic inhibitor 13
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==Reference==
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<ref group="xtra">PMID:023769639</ref><references group="xtra"/><references/>
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[[Category: Homo sapiens]]
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[[Category: Memapsin 2]]
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[[Category: Li, V.]]
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[[Category: Long, A M.]]
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[[Category: Whittington, D A.]]
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[[Category: Alzheimer's disease]]
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[[Category: Aspartic protease]]
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[[Category: Hydrolase-hydrolase inhibitor complex]]

Revision as of 14:01, 3 July 2013

Template:STRUCTURE 4ke0

Contents

Crystal structure of BACE1 in complex with hydroxyethylamine-macrocyclic inhibitor 13

Template:ABSTRACT PUBMED 23769639

Function

[BACE1_HUMAN] Responsible for the proteolytic processing of the amyloid precursor protein (APP). Cleaves at the N-terminus of the A-beta peptide sequence, between residues 671 and 672 of APP, leads to the generation and extracellular release of beta-cleaved soluble APP, and a corresponding cell-associated C-terminal fragment which is later released by gamma-secretase.[1] [2]

About this Structure

4ke0 is a 3 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

  • Pennington LD, Whittington DA, Bartberger MD, Jordan SR, Monenschein H, Nguyen TT, Yang BH, Xue QM, Vounatsos F, Wahl RC, Chen K, Wood S, Citron M, Patel VF, Hitchcock SA, Zhong W. Hydroxyethylamine-based inhibitors of BACE1: P1-P3 macrocyclization can improve potency, selectivity, and cell activity. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4459-64. doi: 10.1016/j.bmcl.2013.05.028., Epub 2013 May 16. PMID:23769639 doi:10.1016/j.bmcl.2013.05.028
  1. ↑ Lin X, Koelsch G, Wu S, Downs D, Dashti A, Tang J. Human aspartic protease memapsin 2 cleaves the beta-secretase site of beta-amyloid precursor protein. Proc Natl Acad Sci U S A. 2000 Feb 15;97(4):1456-60. PMID:10677483
  2. ↑ Okada H, Zhang W, Peterhoff C, Hwang JC, Nixon RA, Ryu SH, Kim TW. Proteomic identification of sorting nexin 6 as a negative regulator of BACE1-mediated APP processing. FASEB J. 2010 Aug;24(8):2783-94. doi: 10.1096/fj.09-146357. Epub 2010 Mar 30. PMID:20354142 doi:10.1096/fj.09-146357

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