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1w51

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Revision as of 07:10, 4 April 2018

BACE (Beta Secretase) in complex with a nanomolar non-peptidic inhibitor

Structural highlights

1w51 is a 1 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:	,
Related:	1fkn, 1m4h, 1py1, 1sgz, 1ujj, 1ujk, 1w50
Activity:	Memapsin 2, with EC number 3.4.23.46
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

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]

Evolutionary Conservation

Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.

Publication Abstract from PubMed

Human BACE, also known as beta-secretase, shows promise as a potential therapeutic target for Alzheimer's disease. We determined the apo structure of BACE to 1.75 A, and a structure of a hydroxyethylamine inhibitor complex derived by soaking. These show significant active-site movements compared to previously described BACE structures. Additionally, the structures reveal two pockets that could be targeted by structure-based drug design.

Apo and inhibitor complex structures of BACE (beta-secretase).,Patel S, Vuillard L, Cleasby A, Murray CW, Yon J J Mol Biol. 2004 Oct 15;343(2):407-16. PMID:15451669^[3]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ 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
↑ Patel S, Vuillard L, Cleasby A, Murray CW, Yon J. Apo and inhibitor complex structures of BACE (beta-secretase). J Mol Biol. 2004 Oct 15;343(2):407-16. PMID:15451669 doi:10.1016/j.jmb.2004.08.018

1 Structural highlights
2 Function
3 Evolutionary Conservation
4 Publication Abstract from PubMed
5 See Also
6 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/1w51"

@@ Line 1: / Line 1: @@
-==BACE (BETA SECRETASE) IN COMPLEX WITH A NANOMOLAR NON-PEPTIDIC INHIBITOR==
+==BACE (Beta Secretase) in complex with a nanomolar non-peptidic inhibitor==
 <StructureSection load='1w51' size='340' side='right' caption='[[1w51]], [[Resolution|resolution]] 2.55&Aring;' scene=''>
 == Structural highlights ==
@@ Line 6: / Line 7: @@
 <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1fkn|1fkn]], [[1m4h|1m4h]], [[1py1|1py1]], [[1sgz|1sgz]], [[1ujj|1ujj]], [[1ujk|1ujk]], [[1w50|1w50]]</td></tr>
 <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Memapsin_2 Memapsin 2], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.46 3.4.23.46] </span></td></tr>
-<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1w51 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1w51 OCA], [http://pdbe.org/1w51 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=1w51 RCSB], [http://www.ebi.ac.uk/pdbsum/1w51 PDBsum]</span></td></tr>
+<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1w51 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1w51 OCA], [http://pdbe.org/1w51 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=1w51 RCSB], [http://www.ebi.ac.uk/pdbsum/1w51 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=1w51 ProSAT]</span></td></tr>
 </table>
 == Function ==
@@ Line 14: / Line 15: @@
 Check<jmol>
   <jmolCheckbox>
-    <scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/w5/1w51_consurf.spt"</scriptWhenChecked>
+    <scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/w5/1w51_consurf.spt"</scriptWhenChecked>
     <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
     <text>to colour the structure by Evolutionary Conservation</text>
@@ Line 43: / Line 44: @@
 [[Category: Vuillard, L]]
 [[Category: Yon, J]]
+[[Category: Alternative splicing]]
 [[Category: Alzheimer's disease]]
 [[Category: Aspartic protease]]

1w51

From Proteopedia

Revision as of 07:10, 4 April 2018

BACE (Beta Secretase) in complex with a nanomolar non-peptidic inhibitor

Structural highlights

Function

Evolutionary Conservation

Publication Abstract from PubMed

See Also

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

Views

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