| Autor: |
Bakshi P; Center for Neurologic Disease, Brigham and Women's Hospital, Harvard Medical School, Boston, Massachusetts 02115, USA., Wolfe MS |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2004 Dec 16; Vol. 47 (26), pp. 6485-9. |
| DOI: |
10.1021/jm049566e |
| Abstrakt: |
(Hydroxyethyl)urea peptidomimetics systematically altered at positions P2-P3' with hydrophobic D-amino acids were synthesized. An all D-amino acid containing analogue was identified that effectively blocked gamma-secretase activity in a cell-free system (IC50 = 30 nM). Systematic alteration of the stereocenters of a potent compound revealed interdependence between the various positions. Although typically less potent than their L-peptidomimetic counterparts, selected all D-amino acid containing analogues were equipotent to their counterparts in a cell-based assay when incubated for extended times. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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