2qzk: Difference between revisions

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{{STRUCTURE_2qzk|  PDB=2qzk  |  SCENE=  }}  
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'''Crystal structure of human Beta Secretase complexed with I21'''
===Crystal structure of human Beta Secretase complexed with I21===




==Overview==
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This letter describes replacements for the P3 amide moiety present in previously reported tertiary carbinamine macrolactones. Although P-gp efflux issues associated with these amide-macrolactones were solved and full brain penetration was measured in one case, potency was compromised in the process.
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{{ABSTRACT_PUBMED_17827011}}


==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 Apr 30 13:18:52 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 19:56:34 2008''

Revision as of 19:56, 28 July 2008

File:2qzk.png

Template:STRUCTURE 2qzk

Crystal structure of human Beta Secretase complexed with I21Crystal structure of human Beta Secretase complexed with I21

Template:ABSTRACT PUBMED 17827011

About this StructureAbout this Structure

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

ReferenceReference

Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors., Moore KP, Zhu H, Rajapakse HA, McGaughey GB, Colussi D, Price EA, Sankaranarayanan S, Simon AJ, Pudvah NT, Hochman JH, Allison T, Munshi SK, Graham SL, Vacca JP, Nantermet PG, Bioorg Med Chem Lett. 2007 Nov 1;17(21):5831-5. Epub 2007 Aug 23. PMID:17827011

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