2ph8

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{{STRUCTURE_2ph8| PDB=2ph8 | SCENE= }}
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'''Crystal Structure of Human Beta Secretase Complexed with inhibitor'''
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===Crystal Structure of Human Beta Secretase Complexed with inhibitor===
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==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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==About this Structure==
==About this Structure==
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[[Category: Bace]]
[[Category: Bace]]
[[Category: Hydrolase]]
[[Category: Hydrolase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Apr 24 09:39:05 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 13:20:04 2008''

Revision as of 10:20, 28 July 2008

Image:2ph8.png

Template:STRUCTURE 2ph8

Crystal Structure of Human Beta Secretase Complexed with inhibitor

Template:ABSTRACT PUBMED 17827011

About this Structure

2PH8 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

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

Page seeded by OCA on Mon Jul 28 13:20:04 2008

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