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  • ||||||||||  nirogacestat (PF-03084014) / SpringWorks Therap
    Journal:  Membrane-tethered Notch1 exhibits oncogenic property via activation of EGFR-PI3K-AKT pathway in oral squamous cell carcinoma. (Pubmed Central) -  Mar 31, 2020   
    γ-Secretase inhibitor PF-03084014 was utilized to determine the phenotype in the absence of endogenous Notch1 activation...This was the first time that we clearly simulated the mutated Notch1 activities and determined the oncogenic phenotypes of membrane-tethered Notch1. Compared with wild-type Notch1, membrane-tethered Notch1 was strongly associated with activated EGFR-PI3K-AKT signaling pathway.
  • ||||||||||  sirolimus / Generic mfg.
    Preclinical, Journal:  Regulatory role of hippocampal PI3K and mTOR signaling pathway in NMDA-induced infant spasm rats. (Pubmed Central) -  Mar 31, 2020   
    The possible mechanism of mTOR signaling pathway was evaluated by the, inhibitors for mTOR and PI3K, rapamycin and wortmannin, respectively...No obvious neurogenesis was found after IS induction. Results of the present study suggest that hippocampal PI3K may be another potential target for IS treatment.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Critical roles of PI3K/Akt/NF‑κB survival axis in angiotensin II‑induced podocyte injury. (Pubmed Central) -  Mar 31, 2020   
    Cells were treated with 10‑6 mol/l of Ang II and/or LY294002 (inhibitor of Akt) or 740Y‑P (activator of PI3K) for 48 h to detect Akt, phosphorylated (phospho)‑Akt, p65 NF‑κB, and phospho‑p65 NF‑κB, nephrin, podocin and caspase‑9 expression, and podocyte apoptosis...The data suggested that Ang II could regulate the expression of nephrin, podocin and caspase‑9. Collectively, our findings suggested that the PI3K/Akt/NF‑κB survival axis may serve a pivotal role in podocyte injury.
  • ||||||||||  Journal:  14-3-3ζ promotes gliomas cells invasion by regulating Snail through the PI3K/AKT signaling. (Pubmed Central) -  Mar 29, 2020   
    Furthermore, subsequent mechanistic studies showed that 14-3-3ζ could activate PI3K/AKT/Snail signaling pathway to facilitate gliomas cells proliferation, migration, and invasion. This study shows that the overexpression of 14-3-3ζ can promote remarkably gliomas cells proliferation, migration, and invasion by regulating the Snail protein expression through activating PI3K/AKT signaling, and it may serve as a potential prognostic marker and therapeutic target for gliomas.
  • ||||||||||  Journal:  RAB43 Promotes Gastric Cancer Cell Proliferation and Metastasis via Regulating the PI3K/AKT Signaling Pathway. (Pubmed Central) -  Mar 28, 2020   
    In vivo studies confirmed that RAB43 promoted tumor growth. In addition, the knockdown of RAB43 significantly inhibited cell proliferation and metastasis via phosphatidylinositol-3-kinases/protein-serine-threonine kinase (PI3K/AKT) pathway. RAB43 promotes GC cells proliferation and migration in vivo and in vitro and probably served as a novel potential therapeutic biomarker for GC.
  • ||||||||||  Review, Journal:  Signal Transduction Pathways in Breast Cancer: The Important Role of PI3K/Akt/mTOR. (Pubmed Central) -  Mar 28, 2020   
    Despite the existence of selective PI3K/Akt/mTOR pathway inhibitors and current clinical trials, the cellular mechanisms are not yet known. The present review aims to understand the current state of this important disease and the paths that must be forged.
  • ||||||||||  metformin / Generic mfg.
    Preclinical, Journal:  Guava Leaf Extract Attenuates Insulin Resistance via the PI3K/Akt Signaling Pathway in a Type 2 Diabetic Mouse Model. (Pubmed Central) -  Mar 28, 2020   
    Mice were randomly assigned into three groups: diabetic mice (DM), DM + MET (diabetic mice treated with metformin) and DM + GLE (diabetic mice treated with GLE) groups...The results of the DM + MET group were similar to those of the DM + GLE group. GLE plays anti-diabetic roles by ameliorating insulin resistance in KK-Ay diabetic mice and this is related to the activation of PI3K/Akt signaling pathway.
  • ||||||||||  Journal, PARP Biomarker, IO Biomarker:  Cardiac glycoside Cerberin exerts anticancer activity through PI3K/AKT/mTOR signal transduction inhibition. (Pubmed Central) -  Mar 26, 2020   
    Preliminary in silico biopharmaceutical assessment of CR predicted >60% bioavailability and rapid absorption; doses of 1-10 mg/kg CR were predicted to maintain efficacious unbound plasma concentrations (>GI value). CR's potent and selective anti-tumour activity, and its targeting of key signalling mechanisms pertinent to tumourigenesis support further preclinical evaluation of this cardiac glycoside.
  • ||||||||||  Journal:  Loss of PDZK1 expression activates PI3K/AKT signaling via PTEN phosphorylation in gastric cancer. (Pubmed Central) -  Mar 26, 2020   
    Downregulation of PDZK1 was associated with PTEN inactivation, AKT signaling and cell proliferation activation in clinical specimens. Thus, low levels of PDZK1 in gastric cancer specimens lead to increase proliferation of gastric cancer cells via phosphorylation of PTEN at the S380/T382/T383 cluster and constitutively activation of PI3K/AKT signaling, which results in poor prognosis of gastric cancer patients.
  • ||||||||||  tizanidine / Generic mfg.
    Journal:  Tizanidine hydrochloride exhibits a cytotoxic effect on osteosarcoma cells through the PI3K/AKT signaling pathway. (Pubmed Central) -  Mar 26, 2020   
    Thus, low levels of PDZK1 in gastric cancer specimens lead to increase proliferation of gastric cancer cells via phosphorylation of PTEN at the S380/T382/T383 cluster and constitutively activation of PI3K/AKT signaling, which results in poor prognosis of gastric cancer patients. THC may play a novel role in OS cell cytotoxicity, and these findings suggest a potent therapeutic strategy for OS treatment.
  • ||||||||||  Journal:  The evolving role of diet in prostate cancer risk and progression. (Pubmed Central) -  Mar 26, 2020   
    Micronutrients, including the carotenoid lycopene which is found in highest concentrations in tomatoes, may also play a role in prostate cancer prevention and prognosis through complementary metabolic mechanisms. The interplay between genetics, diet, and prostate cancer is an area of emerging focus that might help optimize therapeutic dietary response in the future through personalization.
  • ||||||||||  Journal:  Platelet PI3K Modulates Innate Leukocyte Extravasation during Acid-Induced Acute Lung Inflammation. (Pubmed Central) -  Mar 25, 2020   
    These results provide evidence that apelin-13 attenuates EBI following SAH via suppressing neuronal apoptosis, and that this effect may act partially via the activation of the GLP-1R/PI3K/Akt signaling pathway.  Our data indicate a crucial role of platelet PI3K signaling for leukocyte extravasation upon inflammatory stimuli in various diseases models.
  • ||||||||||  rilotumumab (AMG 102) / Amgen
    Journal, IO Biomarker:  AMG-102 inhibits proliferation and induces apoptosis of laryngeal squamous cell carcinoma cells by regulating c-Met/PI3K/Akt pathway (Pubmed Central) -  Mar 25, 2020   
    The relative expression levels of Bax mRNA were 1.78±0.13, 2.37±0.14 and 3.05±0.13, respectively, and the relative expression levels of caspase-3 mRNA were 1.98±0.14, 2.47±0.14 and 3.15±0.13, respectively, which were significantly higher than those in the control group (all P<0.05). c-Met inhibitor AMG-102 could inhibit the proliferation and induce apoptosis of laryngeal squamous carcinoma Hep-2 cells by regulating the c-Met/PI3K/Akt pathway.
  • ||||||||||  Biomarker, Preclinical, Journal:  Betulinic acid improves insulin sensitivity, hyperglycemia, inflammation and oxidative stress in metabolic syndrome rats via PI3K/Akt pathways. (Pubmed Central) -  Mar 24, 2020   
    High-fructose diet-mediated decrease in activities of antioxidant enzymes (superoxide dismutase, catalase, glutathione peroxidase, glutathione reductase and glucose 6-phosphate dehydrogenase) and increase in oxidative stress biomarkers (reduced glutathione, lipid peroxidation products, protein oxidation and fragmented DNA) were significantly restored by the phenolic acids. Conclusively, betulinic acid improves insulin sensitivity, elevated blood glucose, inflammation and dyslipidaemia and oxidative stress in high-fructose diet-induced metabolic syndrome through the PI#Kand Akt pathways .
  • ||||||||||  Torin1 / InvivoGen
    Journal:  Modulator of the PI3K/Akt oncogenic pathway affects mTOR complex 2 in human adenocarcinoma cells. (Pubmed Central) -  Mar 24, 2020   
    Moreover, the autophosphorylation site on complex mTORC2, S2481, was also significantly reduced with ChK pretreatment, similar to Torin1. This is the first report to illustrate that ChK has a significant effect at mTORC2 S2481 and Akt S473 comparable to Torin1, indicating that it may be a mTOR inhibitor.
  • ||||||||||  Journal:  Targeting the IGF1R/PI3K/AKT pathway sensitizes Ewing sarcoma to BET bromodomain inhibitors. (Pubmed Central) -  Mar 24, 2020   
    Taken together, our results suggest that IGF1R and the downstream PI3K/AKT/mTOR kinase cascade mediate intrinsic resistance to BET inhibitors in Ewing sarcoma. These results provide the proof-of-concept for combining BET inhibitors with agents targeting the IGF1R pathway for treating advanced Ewing sarcoma.
  • ||||||||||  Journal:  The small GTPase ARF6 activates PI3K in melanoma to induce a pro-metastatic state. (Pubmed Central) -  Mar 24, 2020   
    We provide evidence for aberrant ARF6 activation in human melanoma samples, which is associated with reduced survival. Our work reveals a previously unknown ARF6-PI3K-AKT pro-invasive pathway, it demonstrates a critical role for ARF6 in multiple steps of the metastatic cascade, and it illuminates how melanoma cells can acquire an early metastatic phenotype in patients.