Abstract
γ-Secretases are a family of intramembrane cleaving aspartyl proteases and important drug targets in Alzheimer's disease. Here, we generated mice deficient for all γ-secretases in the pyramidal neurons of the postnatal forebrain by deleting the three anterior pharynx defective 1 (Aph1) subunits (Aph1abc cKO Cre+). The mice show progressive cortical atrophy, neuronal loss, and gliosis. Interestingly, this is associated with more than 10-fold accumulation of membrane-bound fragments of App, Aplp1, Nrg1, and Dcc, while other known substrates of γ-secretase such as Aplp2, Lrp1, and Sdc3 accumulate to lesser extents. Despite numerous reports linking neurodegeneration to accumulation of membrane-bound App fragments, deletion of App expression in the combined Aph1 knockout does not rescue this phenotype. Importantly, knockout of only Aph1a- or Aph1bc-secretases causes limited and differential accumulation of substrates. This was not associated with neurodegeneration. Further development of selective Aph1-γ-secretase inhibitors should be considered for treatment of Alzheimer's disease.
Keywords
Alzheimer's disease
Aph1 subunit
selective inhibition
side effects
γ‐Secretase
MeSH 主题词
Animals
Blotting, Western
Disease Models, Animal
Endopeptidases/deficiency
Histocytochemistry
Immunohistochemistry
Membrane Proteins
Mice
Mice, Knockout
Microscopy, Fluorescence
Neurodegenerative Diseases/pathology,physiopathology
Prosencephalon/enzymology,pathology
化学物质
Membrane Proteins
Endopeptidases
Aph1C protein, mouse
Aph1a protein, mouse
Aph1b protein, mouse
作者与单位
共 9 位作者,点击展开单位 / ORCID
Acx Hermien
VIB Center for Brain and Disease Research, Leuven, Belgium. | KU Leuven Department for Neurosciences, Leuven Institute for Neurodegenerative Disorders (LIND) and Universitaire Ziekenhuizen Leuven, University of Leuven, Leuven, Belgium.
Serneels Lutgarde
VIB Center for Brain and Disease Research, Leuven, Belgium. | KU Leuven Department for Neurosciences, Leuven Institute for Neurodegenerative Disorders (LIND) and Universitaire Ziekenhuizen Leuven, University of Leuven, Leuven, Belgium.
Radaelli Enrico
VIB Center for Brain and Disease Research, Leuven, Belgium. | KU Leuven Department for Neurosciences, Leuven Institute for Neurodegenerative Disorders (LIND) and Universitaire Ziekenhuizen Leuven, University of Leuven, Leuven, Belgium.
Muyldermans Serge
Cellular and Molecular Immunology, Vrije Universiteit Brussel, Brussels, Belgium.
Vincke Cécile
Cellular and Molecular Immunology, Vrije Universiteit Brussel, Brussels, Belgium.
Pepermans Elise
VIB Center for Brain and Disease Research, Leuven, Belgium. | KU Leuven Department for Neurosciences, Leuven Institute for Neurodegenerative Disorders (LIND) and Universitaire Ziekenhuizen Leuven, University of Leuven, Leuven, Belgium.
Müller Ulrike
Institute for Pharmacy and Molecular Biotechnology (IPMB), University of Heidelberg, Heidelberg, Germany.
Chávez-Gutiérrez Lucía
ORCID
VIB Center for Brain and Disease Research, Leuven, Belgium lucia.chavezGutierrez@cme.vib-kuleuven.be bart.destrooper@cme.vib-kuleuven.be. | KU Leuven Department for Neurosciences, Leuven Institute for Neurodegenerative Disorders (LIND) and Universitaire Ziekenhuizen Leuven, University of Leuven, Leuven, Belgium.
De Strooper Bart
ORCID
VIB Center for Brain and Disease Research, Leuven, Belgium lucia.chavezGutierrez@cme.vib-kuleuven.be bart.destrooper@cme.vib-kuleuven.be. | KU Leuven Department for Neurosciences, Leuven Institute for Neurodegenerative Disorders (LIND) and Universitaire Ziekenhuizen Leuven, University of Leuven, Leuven, Belgium. | UCL Dementia Research Institute (DRI-UK), London, UK.