L-Phenylalaninamide, N-[(2R,4R,5S)-5-[[(1,1-dimethylethoxy)carbonyl]amino]-4-hydroxy-1-oxo-6-phenyl-2-(phenylmethyl)hexyl]-L-leucyl-
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Biological significance and therapeutic implication of resveratrol-inhibited Wnt, Notch and STAT3 signaling in cervical cancer cells. | Genes & cancer 20140501 |
Dopamine induces apoptosis in APPswe-expressing Neuro2A cells following Pepstatin-sensitive proteolysis of APP in acid compartments. | Brain research 20120830 |
Development of clickable active site-directed photoaffinity probes for γ-secretase. | Bioorganic & medicinal chemistry letters 20120415 |
First and second generation γ-secretase modulators (GSMs) modulate amyloid-β (Aβ) peptide production through different mechanisms. | The Journal of biological chemistry 20120406 |
Inhibition of the Notch-Hey1 axis blocks embryonal rhabdomyosarcoma tumorigenesis. | Clinical cancer research : an official journal of the American Association for Cancer Research 20111201 |
Presenilin-1 regulates neural progenitor cell differentiation in the adult brain. | The Journal of neuroscience : the official journal of the Society for Neuroscience 20110216 |
Surface expression and limited proteolysis of ADAM10 are increased by a dominant negative inhibitor of dynamin. | BMC cell biology 20110101 |
Characterization of a Drosophila Alzheimer's disease model: pharmacological rescue of cognitive defects. | PloS one 20110101 |
Human ROBO1 is cleaved by metalloproteinases and gamma-secretase and migrates to the nucleus in cancer cells. | FEBS letters 20100702 |
Design, synthesis, and biological evaluation of a novel class of gamma-secretase modulators with PPARgamma activity. | Journal of medicinal chemistry 20100624 |
A GPCR/secretase complex regulates beta- and gamma-secretase specificity for Abeta production and contributes to AD pathogenesis. | Cell research 20100201 |
Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. | Journal of medicinal chemistry 20091022 |
Nitrous oxide plus isoflurane induces apoptosis and increases beta-amyloid protein levels. | Anesthesiology 20091001 |
The common inhalational anesthetic sevoflurane induces apoptosis and increases beta-amyloid protein levels. | Archives of neurology 20090501 |
Nutlin-3 up-regulates the expression of Notch1 in both myeloid and lymphoid leukemic cells, as part of a negative feedback antiapoptotic mechanism. | Blood 20090430 |
Plasmodium falciparum signal peptide peptidase is a promising drug target against blood stage malaria. | Biochemical and biophysical research communications 20090313 |
Suppression of Notch signaling in the neonatal mouse ovary decreases primordial follicle formation. | Endocrinology 20090201 |
The cytotoxicity of gamma-secretase inhibitor I to breast cancer cells is mediated by proteasome inhibition, not by gamma-secretase inhibition. | Breast cancer research : BCR 20090101 |
The inhalation anesthetic desflurane induces caspase activation and increases amyloid beta-protein levels under hypoxic conditions. | The Journal of biological chemistry 20080502 |
In vitro validation of gamma-secretase inhibitors alone or in combination with other anti-cancer drugs for the treatment of T-cell acute lymphoblastic leukemia. | Haematologica 20080401 |
Identification of gamma-secretase inhibitor potency determinants on presenilin. | The Journal of biological chemistry 20080201 |
Abeta46 is processed to Abeta40 and Abeta43, but not to Abeta42, in the low density membrane domains. | The Journal of biological chemistry 20080111 |
Signal peptide peptidase and gamma-secretase share equivalent inhibitor binding pharmacology. | The Journal of biological chemistry 20071221 |
Gamma-secretase inhibitors exerts antitumor activity via down-regulation of Notch and Nuclear factor kappa B in human tongue carcinoma cells. | Oral diseases 20071101 |
Insensitivity to Abeta42-lowering nonsteroidal anti-inflammatory drugs and gamma-secretase inhibitors is common among aggressive presenilin-1 mutations. | The Journal of biological chemistry 20070824 |
The same gamma-secretase accounts for the multiple intramembrane cleavages of APP. | Journal of neurochemistry 20070301 |
Novel processing of Notch 1 within its intracellular domain by a cysteine protease. | Neuro-degenerative diseases 20070101 |
A novel tricyclic pyrone compound ameliorates cell death associated with intracellular amyloid-beta oligomeric complexes. | Journal of neurochemistry 20060701 |
C-terminal fragment of presenilin is the molecular target of a dipeptidic gamma-secretase-specific inhibitor DAPT (N-[N-(3,5-difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl ester). | The Journal of biological chemistry 20060526 |
Up-regulation of the Notch ligand Delta-like 4 inhibits VEGF-induced endothelial cell function. | Blood 20060201 |
A presenilin-independent aspartyl protease prefers the gamma-42 site cleavage. | Journal of neurochemistry 20060101 |
Eosinophilic differentiation is promoted by blockage of Notch signaling with a gamma-secretase inhibitor. | European journal of immunology 20051001 |
Cell-autonomous notch signaling regulates endothelial cell branching and proliferation during vascular tubulogenesis. | FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20050601 |
Inhibition of angiogenesis and tumor growth by beta and gamma-secretase inhibitors. | European journal of pharmacology 20050502 |
Transition-state analogue gamma-secretase inhibitors stabilize a 900 kDa presenilin/nicastrin complex. | Biochemistry 20050322 |
Presenilin-dependent processing and nuclear function of gamma-protocadherins. | The Journal of biological chemistry 20050311 |
Presenilin attenuates receptor-mediated signaling and synaptic function. | The Journal of neuroscience : the official journal of the Society for Neuroscience 20050209 |
Stereoselective synthesis of photoreactive peptidomimetic gamma-secretase inhibitors. | The Journal of organic chemistry 20041015 |
PEN-2 enhances gamma-cleavage after presenilin heterodimer formation. | Journal of neurochemistry 20040901 |
JLK isocoumarin inhibitors: selective gamma-secretase inhibitors that do not interfere with notch pathway in vitro or in vivo. | Journal of neuroscience research 20031101 |
The mechanism of gamma-secretase: multiple inhibitor binding sites for transition state analogs and small molecule inhibitors. | The Journal of biological chemistry 20030801 |
Catalytic site-directed gamma-secretase complex inhibitors do not discriminate pharmacologically between Notch S3 and beta-APP cleavages. | Biochemistry 20030624 |
Presenilin-dependent gamma-secretase activity mediates the intramembranous cleavage of CD44. | Oncogene 20030313 |
Distinct mechanisms by mutant presenilin 1 and 2 leading to increased intracellular levels of amyloid beta-protein 42 in Chinese hamster ovary cells. | Biochemistry 20030204 |
Synthesis and gamma-secretase activity of APP substrate-based hydroxyethylene dipeptide isosteres. | Bioorganic & medicinal chemistry letters 20030106 |
Presenilin-dependent intramembrane proteolysis of CD44 leads to the liberation of its intracellular domain and the secretion of an Abeta-like peptide. | The Journal of biological chemistry 20021122 |
Linear non-competitive inhibition of solubilized human gamma-secretase by pepstatin A methylester, L685458, sulfonamides, and benzodiazepines. | The Journal of biological chemistry 20020830 |
Presenilin-dependent gamma-secretase activity modulates neurite outgrowth. | Neurobiology of disease 20020201 |
gamma-Secretase: characterization and implication for Alzheimer disease therapy. | Neurobiology of aging 20020101 |
gamma -Secretase cleavage and nuclear localization of ErbB-4 receptor tyrosine kinase. | Science (New York, N.Y.) 20011207 |
Gamma-secretase: a catalyst of Alzheimer disease and signal transduction. | Molecular interventions 20011001 |
Endoproteolysis of the ER stress transducer ATF6 in the presence of functionally inactive presenilins. | Neurobiology of disease 20010801 |
Secretase targets for Alzheimer's disease: identification and therapeutic potential. | Journal of medicinal chemistry 20010621 |
L-685,458, an aspartyl protease transition state mimic, is a potent inhibitor of amyloid beta-protein precursor gamma-secretase activity. | Biochemistry 20000801 |