3ckr: Difference between revisions

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{{STRUCTURE_3ckr|  PDB=3ckr  |  SCENE=  }}  
{{STRUCTURE_3ckr|  PDB=3ckr  |  SCENE=  }}  


'''Crystal structure of BACE-1 in complex with inhibitor'''
===Crystal structure of BACE-1 in complex with inhibitor===




==Overview==
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We describe synthesis and evaluation of a series of cyclic urea derivatives with hydroxylethylamine isostere. Modification of P3, P1, and P2' and combination of SAR display a &gt;100-fold increase in potency with good cellular activity (IC(50)=0.15microM) relative to the previously reported compound 3.
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{{ABSTRACT_PUBMED_18434152}}


==About this Structure==
==About this Structure==
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[[Category: Transmembrane]]
[[Category: Transmembrane]]
[[Category: Zymogen]]
[[Category: Zymogen]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jun  4 09:55:39 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 00:58:28 2008''

Revision as of 00:58, 28 July 2008

File:3ckr.png

Template:STRUCTURE 3ckr

Crystal structure of BACE-1 in complex with inhibitorCrystal structure of BACE-1 in complex with inhibitor

Template:ABSTRACT PUBMED 18434152

About this StructureAbout this Structure

3CKR is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

ReferenceReference

Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives., Park H, Min K, Kwak HS, Koo KD, Lim D, Seo SW, Choi JU, Platt B, Choi DY, Bioorg Med Chem Lett. 2008 May 1;18(9):2900-4. Epub 2008 Apr 8. PMID:18434152

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