| Structural highlights
2qzl 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: | 2qzk |
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
A series of beta-site amyloid precursor protein cleaving enzyme (BACE-1) inhibitors containing a psi(CH2NH) reduced amide bond were synthesized. Incorporation of this reduced amide isostere as a non-cleavable peptide surrogate afforded inhibitors possessing low nanomolar potencies in both an enzymatic and cell-based assay.
BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres.,Coburn CA, Stachel SJ, Jones KG, Steele TG, Rush DM, DiMuzio J, Pietrak BL, Lai MT, Huang Q, Lineberger J, Jin L, Munshi S, Katharine Holloway M, Espeseth A, Simon A, Hazuda D, Graham SL, Vacca JP Bioorg Med Chem Lett. 2006 Jul 15;16(14):3635-8. Epub 2006 May 11. PMID:16690314[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Coburn CA, Stachel SJ, Jones KG, Steele TG, Rush DM, DiMuzio J, Pietrak BL, Lai MT, Huang Q, Lineberger J, Jin L, Munshi S, Katharine Holloway M, Espeseth A, Simon A, Hazuda D, Graham SL, Vacca JP. BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3635-8. Epub 2006 May 11. PMID:16690314 doi:10.1016/j.bmcl.2006.04.076
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