Secretase inhibitor
Original Article -Secretase inhibitor (DAPT) alleviates the inflammation of paraquat-induced ALI mice by regulating the differentiation of Th17 cells
... γ-secretase inhibitor (DAPT) could suppress the expression of RORγt mRNA in mice with PQ-administrated ALI, which suggests that Notch signaling can regulate the differentiation of Th17 cells via RORγ ...
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Effect of γ secretase inhibitor on Th17 cell differentiation and function of mouse psoriasis like skin inflammation
... γ-secretase inhibitor and commonly used to block Notch signaling, which can effectively interrupt presenilin, an important component of the γ-secretase and critical for γ-secretase activity, ...
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γ-secretase inhibitor I inhibits neuroblastoma cells, with NOTCH and the proteasome among its targets
... As high-risk neuroblastoma (NB) has a poor prognosis, new therapeutic modalities are needed. We therefore investigated the susceptibility of NB cells to γ-secretase inhibitor I (GSI-I). NOTCH signaling ...
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Existing plaques and neuritic abnormalities in APP:PS1 mice are not affected by administration of the gamma-secretase inhibitor LY-411575
... γ- secretase inhibitor, N(2)-[(2S)-2-(3,5-difluorophenyl)-2- hydroxyethanoyl]-N(1)-[(7S)-5-methyl-6-oxo-6,7-dihy- dro-5H-dibenzo[b,d]azepin-7-yl]-l-alaninamide (LY- 411575) [21,22] and multiphoton ...
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γ Secretase inhibitor–resistant glioblastoma stem cells require RBPJ to propagate
... γ-secretase inhibitor (GSI) or by induc- ing activation of the bone morphogenetic protein (BMP) pathway with BMP4, has shown some efficacy in preclinical studies (10, 11), bringing hope to improving brain ...
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Gamma-secretase Inhibitor Prevents Proliferation and Migration of Ductus Arteriosus Smooth Muscle Cells through the Notch3-HES1/2/5 Pathway
... γ-secretase inhibitor, Ang II, α-actin and α-smooth muscle actin antibodies, and 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazo- lium bromide (MTT) were obtained from Sigma-Aldrich, ...
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BACE-1 inhibition prevents the γ-secretase inhibitor evoked Aβ rise in human neuroblastoma SH-SY5Y cells
... 12. Burton CR, Meredith JE, Barten DM, Goldstein ME, Krause CM, Kieras CJ, Sisk L, Iben LG, Polson C, Thompson MW, Lin XA, Corsa J, Fiedler T, Pierdomenico M, Cao Y, Roach AH, Cantone JL, Ford MJ, Drexler DM, Olson RE, ...
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Original Article Gamma secretase inhibitor enhances sensitivity to doxorubicin in MDA-MB-231 cells
... Abstract: Deregulated expression of molecular of the Notch signaling pathway is observed in malignant tumor. Notch signaling pathway is activated by a series of catalytic cleavage of the Notch receptor by gamma ...
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The cytotoxicity of γ secretase inhibitor I to breast cancer cells is mediated by proteasome inhibition, not by γ secretase inhibition
... Introduction Notch is a family of transmembrane protein receptors whose activation requires proteolytic cleavage by γ- secretase. Since aberrant Notch signaling can induce mammary carcinomas in transgenic mice and ...
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A phase I trial of the γ-secretase inhibitor MK-0752 in combination with gemcitabine in patients with pancreatic ductal adenocarcinoma
... Groth C, Alvord WG, Quinones OA, Fortini ME (2010) Pharmacological analysis of Drosophila melanogaster gamma-secretase with respect to differential proteolysis of Notch and APP. Mol Pharmacol 77: 567–574. Jones S, ...
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A single dose of the γ-secretase inhibitor semagacestat alters the cerebrospinal fluid peptidome in humans
... APL1β17, a 17-amino acid long peptide located near the transmembrane region of APLP1 (Fig. 4b), also de- creased in response to the treatment (Fig. 3). The peptide showed a maximum decrease 12 h after drug intake, which ...
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Notch pathway activation is essential for maintenance of stem-like cells in early tongue cancer
... gamma secretase inhibitor or shRNA mediated knockdown of NOTCH1 inhibits spheroid forming capacity, transformation, survival and migration of the HNSCC cells suggesting an oncogenic role of NOTCH1 in ...
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Jaeckel, Stephanie (2019): Genetic analysis of Ap4 in the ApcMin mouse model. Dissertation, LMU München: Medizinische Fakultät
... Partial Notch inhibition by the γ -secretase inhibitor Dibenzazepine (DBZ) or by deleting Notch1 (but not Notch2) leads to a decrease of ISCs, an increase in secretory cells such as g[r] ...
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Papillomavirus Infection Requires γ Secretase
... XXI blocks genome localization at ND10 but not capsid uptake or disassembly. We sought to determine at which step during the infectious process ␥ -secretase activity is required. There was no obvious effect upon ...
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QSAR STUDIES & DESIGNING OF POTENT HETEROCYCLIC COMPOUNDS AS γ SECRETASE INHIBITORS
... gamma secretase inhibitor ...gamma secretase inhibitor activity is governed by physicochemical Alignment Independent (AI) descriptors and design new compounds, with more potent ...
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Chemotherapy induces Notch1-dependent MRP1 up-regulation, inhibition of which sensitizes breast cancer cells to chemotherapy
... regulation of MRP1 has not been investigated in non- tumouriogenic cells previously. The well-characterised γ-secretase inhibitor DAPT was used as an inhibitor of Notch1 activation. ...
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The impact of neuronal Notch-1/JNK pathway on intracerebral hemorrhage-induced neuronal injury of rat model
... To determine a role of Notch-1 in the phosphorylation of JNK, blocking Notch signaling activation by a γ-secretase inhibitor, DAPT was applied, and then relevant proteins including p-JNK and active caspase ...
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Induced pluripotent stem cells in Alzheimer’s disease: applications for disease modeling and cell-replacement therapy
... BSI: β -secretase inhibitor; aGSK-3 β : active glycogen synthase kinase-3 β ; AD: Alzheimer ’ s disease; A β : Amyloid- β (A β ); APP: Amyloid precursor protein; APOE: Apolipoprotein E; [r] ...
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Pharmacological Assessment of γ Secretase Activity from Rodent and Human Brain
... γ-secretase inhibitor and the modulatory activity of two classes of γ-secretase modulators were equipotent at affecting the production of Aβ across rodent and human brain membrane ...
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On the origin of vertebrate somites
... -secretase inhibitor that indirectly inhibits Notch) treatment from the late blastula stage reduced late gastrula stage expression of BfFringe in the endodermal archenteron and somite markers BfDelta and ...
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