Yeatman.Gamma-secretase inhibition attenuates oxaliplatin-induced apoptosis through increased Mcl-1 and/or Bcl-xL in human colon cancer cells[J].Apoptosis.2013(10)Timme CR, Gruidl M, Yeatman TJ. Gamma-secretase inhibition attenuates oxaliplatin- induced apoptosis through increased Mcl-1 and/or Bcl...
Explores the potency of pharmacological gamma-secretase in the inhibition of thymocyte development. Significance of gamma-secretase for the management of Alzheimer's disease; Functions of Notch signal transduction pathway; Employment of fetal thymus organ cultures.Hadland...
specifically reduce gamma-secretase activity in the central nervous system, and those with the appropriate properties are being utilized in on-going proof-of-concept studies in animals and humans, to determine the extent and duration of gamma-secretase inhibition required to elicit therapeutic benefits...
29 Tumors did not recur in any treated mice up to 1 year after administration, suggesting γ-secretase/Notch inhibition as a potential strategy for treating breast cancer. Similar effects were seen in in vitro models of multiple myeloma and non-Hodgkin's lymphoma30 and combination therapy with ...
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Targeted gamma-secretase inhibition of Notch signaling activation in acute renal injury The Notch pathway has been reported to control tissue damage in acute kidney diseases. To investigate potential beneficial nephroprotective effects of targeting Notch, we developed chemically functionalized -secretase inhib...
Gamma Secretase Inhibition by BMS-906024 Enhances Efficacy of Paclitaxel in Lung Adenocarcinoma. Mol Cancer Ther. 2017 Dec;16(12):2759-2769.2.Gavai AV, et al. Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors. ACS Med ...
Trials in both healthy volunteers and patients with AD have demonstrated a dose-dependent inhibition of plasma A beta levels, and a recent trial in healthy volunteers demonstrated a robust, dose-dependent inhibition of newly generated A beta in the CSF after single oral doses. The main adverse ...
Inhibition of gamma-secretase presents a direct target for lowering Aβ production in the brain as a therapy for Alzheimer's disease (AD). However, gamma-secretase is known to process multiple substrates in addition to amyloid precursor protein (APP), mo
active site, (5) substrate processing after endoproteolysis, and (6) inhibition and modulation of γ-secretase. We conclude with still open questions and suggest further investigations in order to advance our understanding on how γ-secretase selects and processes substrates. This knowledge will ...