2ph6

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Image:2ph6.jpg

2ph6, resolution 2.00Å

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Crystal Structure of Human Beta Secretase Complexed with inhibitor

Overview

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.

About this Structure

2PH6 is a Single protein structure of sequence from Homo sapiens with and as ligands. Active as Memapsin 2, with EC number 3.4.23.46 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 Apr 27;. PMID:17482814

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