2b8l | pdb_00002b8l
Crystal structure of human beta secretase complexed with inhibitor
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| 2b8l, resolution 1.7Å | |||||||||||||
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| Ligands: | 5HA | ||||||||||||
| Gene: | BACE1, BACE (Homo sapiens) | ||||||||||||
| Activity: | Memapsin 2, with EC number 3.4.23.46 | ||||||||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
Overview
We have synthesized and evaluated a series of conformationally biased P3 amide replacements based on an isophthalamide lead structure. The studies resulted in the identification of the beta-secretase inhibitor 7m which has an in vitro IC(50)=35 nM. The synthesis and biological activities of these compounds are described.
About this Structure
2B8L is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Conformationally biased P3 amide replacements of beta-secretase inhibitors., Stachel SJ, Coburn CA, Steele TG, Crouthamel MC, Pietrak BL, Lai MT, Holloway MK, Munshi SK, Graham SL, Vacca JP, Bioorg Med Chem Lett. 2006 Feb;16(3):641-4. Epub 2005 Nov 2. PMID:16263281
Page seeded by OCA on Mon Mar 31 02:02:53 2008
