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BibTeX
JLK isocoumarin inhibitors: Selective γ-secretase inhibitors that do not interfere with notch pathway in vitro or in vivo
Journal of neuroscience research, 2003-11, Vol.74 (3), p.370-377
Petit, A.
Pasini, A.
Alves da Costa, C.
Ayral, E.
Hernandez, J.F.
Dumanchin-Njock, C.
Phiel, C.J.
Marambaud, P.
Wilk, S.
Farzan, M.
Fulcrand, P.
Martinez, J.
Andrau, D.
Checler, F.
2003
Details
Autor(en) / Beteiligte
Petit, A.
Pasini, A.
Alves da Costa, C.
Ayral, E.
Hernandez, J.F.
Dumanchin-Njock, C.
Phiel, C.J.
Marambaud, P.
Wilk, S.
Farzan, M.
Fulcrand, P.
Martinez, J.
Andrau, D.
Checler, F.
Titel
JLK isocoumarin inhibitors: Selective γ-secretase inhibitors that do not interfere with notch pathway in vitro or in vivo
Ist Teil von
Journal of neuroscience research, 2003-11, Vol.74 (3), p.370-377
Ort / Verlag
Hoboken: Wiley Subscription Services, Inc., A Wiley Company
Erscheinungsjahr
2003
Link zum Volltext
Quelle
Alma/SFX Local Collection
Beschreibungen/Notizen
γ‐Secretase activity is involved in the generation of Aβ and therefore likely contributes to the pathology of Alzheimer's disease. Blocking this activity was seen as a major therapeutic target to slow down or arrest Aβ‐related AD progression. This strategy seemed more doubtful when it was established that γ‐secretase also targets other substrates including Notch, a particularly important transmembrane protein involved in vital functions, at both embryonic and adulthood stages. We have described previously new non‐peptidic inhibitors able to selectively inhibit Aβ cellular production in vitro without altering Notch pathway. We show here that in vivo, these inhibitors do not alter the Notch pathway responsible for somitogenesis in the zebrafish embryo. In addition, we document further the selectivity of JLK inhibitors by showing that, unlike other described γ‐secretase inhibitors, these agents do not affect E‐cadherin processing. Finally, we establish that JLKs do not inhibit β‐site APP cleaving enzymes (BACE) 1 and BACE2, α‐secretase, the proteasome, and GSK3β kinase. Altogether, JLK inhibitors are the sole agents to date that are able to prevent Aβ production without triggering unwanted cleavages of other proteins. © 2003 Wiley‐Liss, Inc.
Sprache
Englisch
Identifikatoren
ISSN: 0360-4012
eISSN: 1097-4547
DOI: 10.1002/jnr.10747
Titel-ID: cdi_proquest_miscellaneous_71366833
Format
–
Schlagworte
Alzheimer's disease
,
Amyloid beta-Peptides - metabolism
,
Amyloid Precursor Protein Secretases
,
amyloid β peptide
,
Animals
,
Anticoagulants - pharmacology
,
Aspartic Acid Endopeptidases - metabolism
,
BACE
,
Blotting, Western
,
cadherins
,
Cadherins - metabolism
,
Carbamates - analysis
,
Carbamates - pharmacology
,
Cell Line - drug effects
,
Cysteine Endopeptidases - metabolism
,
Danio rerio
,
Dipeptides - analysis
,
Dipeptides - pharmacology
,
Dose-Response Relationship, Drug
,
Embryo, Mammalian - drug effects
,
Embryo, Nonmammalian
,
Endopeptidases - metabolism
,
gamma-Aminobutyric Acid - analogs & derivatives
,
gamma-Aminobutyric Acid - pharmacology
,
Glycogen Synthase Kinase 3 - metabolism
,
Glycogen Synthase Kinase 3 beta
,
GSK3β
,
Humans
,
In Situ Hybridization
,
In Vitro Techniques
,
inhibitors
,
Kidney
,
Membrane Proteins - metabolism
,
Multienzyme Complexes - metabolism
,
Mutation
,
NICD
,
notch
,
Peptide Fragments - metabolism
,
Precipitin Tests
,
presenilins
,
processing
,
proteasome
,
Proteasome Endopeptidase Complex
,
Receptors, Notch
,
Time Factors
,
Transfection - methods
,
Triglycerides - pharmacology
,
Zebrafish
,
γ-secretase
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