2vnn
From Proteopedia
HUMAN BACE-1 IN COMPLEX WITH 7-ETHYL-N-((1S,2R)-2-HYDROXY-1-(PHENYLMETHYL)-3-(((3-(TRIFLUOROMETHYL)PHENYL)METHYL)AMINO) PROPYL)-1-METHYL-3,4-DIHYDRO-1H-(1,2,5)THIADIAZEPINO(3,4,5-HI)INDOLE-9-CARBOXAMIDE 2,2-DIOXIDE
Overview
BACE-1 inhibition has the potential to provide a disease-modifying therapy for the treatment of Alzheimer's disease. Optimization of a first generation of BACE-1 inhibitors led to the discovery of novel hydroxyethylamines (HEAs) bearing a tricyclic nonprime side. These derivatives have nanomolar cell potency and are orally bioavailable.
About this Structure
2VNN is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Second Generation of Hydroxyethylamine BACE-1 Inhibitors: Optimizing Potency and Oral Bioavailability., Charrier N, Clarke B, Cutler L, Demont E, Dingwall C, Dunsdon R, East P, Hawkins J, Howes C, Hussain I, Jeffrey P, Maile G, Matico R, Mosley J, Naylor A, O'Brien A, Redshaw S, Rowland P, Soleil V, Smith KJ, Sweitzer S, Theobald P, Vesey D, Walter DS, Wayne G, J Med Chem. 2008 May 6;. PMID:18457381 Page seeded by OCA on Thu May 22 21:41:55 2008
Categories: Homo sapiens | Memapsin 2 | Single protein | Charrier, N. | Clarke, B. | Cutler, L. | Demont, E. | Dingwall, C. | Dunsdon, R. | East, P. | Hawkins, J. | Howes, C. | Hussain, I. | Jeffrey, P. | Maile, G. | Matico, R. | Mosley, J. | Naylor, A. | Obrien, A. | Redshaw, S. | Rowland, P. | Smith, K J. | Soleil, V. | Sweitzer, S. | Theobald, P. | Vesey, D. | Walter, D S. | Wayne, G. | Alternative splicing | Asp-2 | Aspartyl protease | Bace-1 | Beta-secretase | Beta-site app cleaving enzyme | Glycoprotein | Hydrolase | Memapsin-2 | Membrane | Protease | Transmembrane | Zymogen
