2qzk
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Revision as of 10:19, 30 April 2008
Crystal structure of human Beta Secretase complexed with I21
Overview
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.
About this Structure
2QZK 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 Wed Apr 30 13:18:52 2008
