2ph6 | pdb_00002ph6

Crystal Structure of Human Beta Secretase Complexed with inhibitor

spinqualitylabelsall models 2ph6, resolution 2.00Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 2ph6 is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: 712, SO4 Related: 1tqf Gene: BACE1, BACE (Homo sapiens) Activity: Memapsin 2, with EC number 3.4.23.46 Resources: FirstGlance, OCA, RCSB, PDBsum Evolutionary Conservation Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf. Publication Abstract from PubMed 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. 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 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Beta secretase

Proteopedia Page Contributors and Editors (what is this?)

OCA