2p83: Difference between revisions

Revision as of 12:34, 4 May 2008

Potent and selective isophthalamide S2 hydroxyethylamine inhibitor of BACE1

OverviewOverview

The design and synthesis of a novel series of potent BACE1 hydroxyethylamine inhibitors. These inhibitors feature hydrogen bonding substituents at the C-5 position of the isophthalamide ring with improved selectivity over cathepsin D.

About this StructureAbout this Structure

2P83 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

ReferenceReference

Potent and selective isophthalamide S2 hydroxyethylamine inhibitors of BACE1., Kortum SW, Benson TE, Bienkowski MJ, Emmons TL, Prince DB, Paddock DJ, Tomasselli AG, Moon JB, LaBorde A, TenBrink RE, Bioorg Med Chem Lett. 2007 Jun 15;17(12):3378-83. Epub 2007 Apr 3. PMID:17434734 Page seeded by OCA on Sun May 4 12:34:54 2008

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

OCA

@@ Line 1: / Line 1: @@
 [[Image:2p83.jpg|left|200px]]
- {{Structure
+<!--
-|PDB= 2p83 |SIZE=350|CAPTION= <scene name='initialview01'>2p83</scene>, resolution 2.500&Aring;
+The line below this paragraph, containing "STRUCTURE_2p83", creates the "Structure Box" on the page.
-|SITE=
+You may change the PDB parameter (which sets the PDB file loaded into the applet)
-|LIGAND= <scene name='pdbligand=MR0:N~3~-{(1S,2R)-1-(3,5-DIFLUOROBENZYL)-2-HYDROXY-3-[(3-METHOXYBENZYL)AMINO]PROPYL}-N~1~,N~1~-DIPROPYLBENZENE-1,3,5-TRICARBOXAMIDE'>MR0</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene>
+or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-|ACTIVITY= <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>
+or leave the SCENE parameter empty for the default display.
-|GENE= BACE1, BACE ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
+-->
-|DOMAIN=
+{{STRUCTURE_2p83|  PDB=2p83  |  SCENE=  }}
-|RELATEDENTRY=
-|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2p83 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2p83 OCA], [http://www.ebi.ac.uk/pdbsum/2p83 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2p83 RCSB]</span>
-}}
 '''Potent and selective isophthalamide S2 hydroxyethylamine inhibitor of BACE1'''
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 [[Category: Prince, D B.]]
 [[Category: Tomasselli, A G.]]
-[[Category: protein-inhibitor complex]]
+[[Category: Protein-inhibitor complex]]
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 12:34:54 2008''
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:32:10 2008''