gamma-Secretase (a multi-subunit protease complex) inhibitor and indirectly an inhibitor of Notch,
REVIEW DAPT is a gamma-secretase (a multi-subunit protease complex) inhibitor and indirectly an inhibitor of Notch, a gamma-secretase substrate. The most well-known substrate of gamma secretase is amyloid precursor protein, a large integral membrane protein that, when cleaved by both gamma and beta secretase, produces a amyloid beta whose abnormally folded fibrillar form is the primary component of amyloid plaques found in the brains of Alzheimer''s disease patients. As an inhibitor of gamma-secretase, DAPT causes a reduction in Abeta40 and Abeta42 levels in human primary neuronal cultures (IC50 values are 115 and 200 nM for total Abeta and Abeta42 respectively) and in brain extract, cerebrospinal fluid and plasma in vivo. Does not effect APPalpha and APPbeta levels. DAPT blocks Notch signaling in hybrid human-mouse fetal thymus organ culture (FTOC). Activity causes neural cells to commit to neuronal differentiation. DAPT has proved useful in the study of beta-amyloid (Abeta) formation. As an inhibitor of Notch, DAPT has advanced studies of autoimmune and lymphoproliferative diseases, such as ALPS and lupus erythematosus (SLE).
REFERENCES
[1]
H. F. Dovey, V. John, J. P. Anderson, L. Z. Chen, P. De Saint Andrieu, L. Y. Fang, S. B. Freedman, B. Folmer, E. Goldbach, E. J. Holsztynska, K. L. Hu, K. L. Johnson-Wood, S. L. Kennedy, D. Kholodenko, J. E. Knops, L. H. Latimer, M. Lee, Z. Liao, I. M. Lieberburg, R. N. Motter, L. C. Mutter, J. Nietz, K. P. Quinn, K. L. Sacchi, P. A. Seubert, G. M. Shopp, E. D. Thorsett, J. S. Tung, J. Wu, S. Yang, C. T. Yin, D. B. Schenk, P. C. May, L. D. Altstiel, M. H. Bender, L. N. Boggs, T. C. Britton, J. C. Clemens, D. L. Czilli, D. K. Dieckman-McGinty, J. J. Droste, K. S. Fuson, B. D. Gitter, P. A. Hyslop, E. M. Johnstone, W-Y. Li, S. P. Little, T. E. Mabry, F. D. Miller, B. Ni, J. S. Nissen,W. J. Porter, B. D. Potts, J. K. Reel, D. Stephenson, Y. Su, L. A. Shipley, C. A. Whitesitt, T. Yin, J. E. Audia Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain. Journal of Neurochemistry (2001), 76(1), 173-181
[2]
Yagishita, Sousuke; Morishima-Kawashima, Maho; Tanimura, Yu; Ishiura, Shoichi; Ihara, Yasuo; DAPT-Induced Intracellular Accumulations of Longer Amyloid beta-Proteins: Further Implications for the Mechanism of Intramembrane Cleavage by gamma-Secretase. Biochemistry (2006), 45(12), 3952-3960.
[3]
Jakob-Roetne, Roland; Jacobsen, Helmut Alzheimer''s Disease: From Pathology to Therapeutic Approaches Angewandte Chemie, International Edition (2009), 48(17), 3030-3059.
[4]
Palagani V, El Khatib M, Kossatz U, Bozko P, Müller MR, Manns MP, Krech T, Malek NP, Plentz RR.Epithelial mesenchymal transition and pancreatic tumor initiating CD44+/EpCAM+ cells are inhibited by gamma-secretase inhibitor IX. LoS One. 2012;7(10):e46514.
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