2ph6

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[[Image:2ph6.jpg|left|200px]]
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{{STRUCTURE_2ph6| PDB=2ph6 | SCENE= }}
{{STRUCTURE_2ph6| PDB=2ph6 | 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 the design and synthesis of tertiary carbinamine macrocyclic inhibitors of the beta-secretase (BACE-1) enzyme. These macrocyclic inhibitors, some of which incorporate novel P2 substituents, display a 2- to 100-fold increase in potency relative to the previously described acyclic analogs while affording greater stability.
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(as it appears on PubMed at http://www.pubmed.gov), where 17482814 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17482814}}
==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 Sun May 4 13:06:10 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 05:52:44 2008''

Revision as of 02:52, 28 July 2008

Image:2ph6.png

Template:STRUCTURE 2ph6

Crystal Structure of Human Beta Secretase Complexed with inhibitor

Template:ABSTRACT PUBMED 17482814

About this Structure

2PH6 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors., Lindsley SR, Moore KP, Rajapakse HA, Selnick HG, Young MB, Zhu H, Munshi S, Kuo L, McGaughey GB, Colussi D, Crouthamel MC, Lai MT, Pietrak B, Price EA, Sankaranarayanan S, Simon AJ, Seabrook GR, Hazuda DJ, Pudvah NT, Hochman JH, Graham SL, Vacca JP, Nantermet PG, Bioorg Med Chem Lett. 2007 Jul 15;17(14):4057-61. Epub 2007 Apr 27. PMID:17482814

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