| Structural highlights
2xfk 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: |
| | Related: | 1xn3, 2wf3, 2wf1, 2vnm, 2wf4, 2fdp, 2vj6, 1ym4, 2wf2, 1sgz, 1ujk, 2va7, 2wjo, 2wez, 1ym2, 1py1, 1w50, 2vj7, 2wf0, 1w51, 1tqf, 1m4h, 1xn2, 2viy, 2va6, 2vie, 2viz, 2b8l, 2va5, 2b8v, 1fkn, 1xs7, 2vij, 2vj9, 2vkm, 2vnn, 1ujj, 2xfj, 2xfi |
| 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
Inhibition of the aspartyl protease BACE-1 has the potential to deliver a disease-modifying therapy for Alzheimer's disease. Herein, is described a series of potent inhibitors based on an hydroxyethylamine (HEA) transition state mimetic template. These inhibitors interact with the non prime side of the enzyme using a novel edge-to-face interaction with Arg-296.
BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296.,Clarke B, Cutler L, Demont E, Dingwall C, Dunsdon R, Hawkins J, Howes C, Hussain I, 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 Bioorg Med Chem Lett. 2010 Aug 1;20(15):4639-44. Epub 2010 Jun 8. PMID:20579874[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Clarke B, Cutler L, Demont E, Dingwall C, Dunsdon R, Hawkins J, Howes C, Hussain I, 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. BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4639-44. Epub 2010 Jun 8. PMID:20579874 doi:10.1016/j.bmcl.2010.05.111
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