3u6a

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[[Image:3u6a.png|left|200px]]
 
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{{STRUCTURE_3u6a| PDB=3u6a | SCENE= }}
{{STRUCTURE_3u6a| PDB=3u6a | SCENE= }}
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===Rational Design and Synthesis of Aminopiperazinones as Beta Secretase (BACE) Inhibitors===
===Rational Design and Synthesis of Aminopiperazinones as Beta Secretase (BACE) Inhibitors===
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{{ABSTRACT_PUBMED_22071305}}
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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>
==About this Structure==
==About this Structure==
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==See Also==
==See Also==
*[[Beta secretase|Beta secretase]]
*[[Beta secretase|Beta secretase]]
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==Reference==
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<ref group="xtra">PMID:022071305</ref><references group="xtra"/><references/>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Memapsin 2]]
[[Category: Memapsin 2]]

Revision as of 08:55, 4 September 2013

Template:STRUCTURE 3u6a

Contents

Rational Design and Synthesis of Aminopiperazinones as Beta Secretase (BACE) Inhibitors

Template:ABSTRACT PUBMED 22071305

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

3u6a is a 3 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.

See Also

Reference

  • Tresadern G, Delgado F, Delgado O, Gijsen H, Macdonald GJ, Moechars D, Rombouts F, Alexander R, Spurlino J, Van Gool M, Vega JA, Trabanco AA. Rational design and synthesis of aminopiperazinones as beta-secretase (BACE) inhibitors. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7255-60. doi:, 10.1016/j.bmcl.2011.10.050. Epub 2011 Oct 20. PMID:22071305 doi:10.1016/j.bmcl.2011.10.050
  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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