4lxk: Difference between revisions
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{{STRUCTURE_4lxk| PDB=4lxk | SCENE= }} | |||
===Crystal Structure of Human Beta Secretase in Complex with compound 11d=== | |||
{{ABSTRACT_PUBMED_22380629}} | |||
==Function== | |||
[[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== | |||
[[4lxk]] is a 3 chain structure with sequence from [http://en.wikipedia.org/wiki/Ochroconis_lascauxensis Ochroconis lascauxensis]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4LXK OCA]. | |||
==Reference== | |||
<ref group="xtra">PMID:022380629</ref><references group="xtra"/><references/> | |||
[[Category: Memapsin 2]] | |||
[[Category: Ochroconis lascauxensis]] | |||
[[Category: Bourgier, E.]] | |||
[[Category: Rondeau, J M.]] | |||
[[Category: Aspartyl protease]] | |||
[[Category: Hydrolase-hydrolase inhibitor complex]] | |||
[[Category: Membrane]] | |||
[[Category: Structure-based drug design]] | |||
Revision as of 10:33, 28 August 2013
Crystal Structure of Human Beta Secretase in Complex with compound 11dCrystal Structure of Human Beta Secretase in Complex with compound 11d
Template:ABSTRACT PUBMED 22380629
FunctionFunction
[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 StructureAbout this Structure
4lxk is a 3 chain structure with sequence from Ochroconis lascauxensis. Full crystallographic information is available from OCA.
ReferenceReference
- ↑ Rueeger H, Lueoend R, Rogel O, Rondeau JM, Mobitz H, Machauer R, Jacobson L, Staufenbiel M, Desrayaud S, Neumann U. Discovery of cyclic sulfone hydroxyethylamines as potent and selective beta-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure-based design and in vivo reduction of amyloid beta-peptides. J Med Chem. 2012 Apr 12;55(7):3364-86. Epub 2012 Mar 21. PMID:22380629 doi:10.1021/jm300069y
- ↑ 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
- ↑ 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