LY294002 / Eli Lilly 
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  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Urotensin II promotes secretion of LTB through 5-lipoxygenase via the UT-ROS-Akt pathway in RAW264.7 macrophages. (Pubmed Central) -  Jul 31, 2019   
    ...Leukotriene B4 production and 5-lipoxygenase expression were decreased by blocking the UII receptor (UT) with urantide, eliminating ROS with N-acetylcysteine and diphenyliodonium, and inhibiting Akt phosphorylation with LY294002...Urotensin II may promote 5-lipoxygenase expression and LTB release in RAW264.7 macrophages via UT-ROS-Akt pathways. These results indicate that UII may participate in macrophage activation and suggest a potential new mechanism underlying atherosclerosis.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Wound Healing Potential of Spirulina Protein on CCD-986sk Cells. (Pubmed Central) -  Jul 24, 2019   
    However, the phosphorylation of Akt was significantly blocked by PI3K inhibitor (LY294002), which in turn reduced the SPCP-induced proliferation and migration of CCD-986sk cells. Therefore, the results presenting in this study suggested that SPCP can promote the proliferation and migration of CCD-986sk cells; the PI3K/Akt signaling pathway play a positive and important role in these processes.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Lipopolysaccharide-Induced Autophagy Mediates Retinal Pigment Epithelium Cells Survival. Modulation by the Phospholipase D Pathway. (Pubmed Central) -  Jul 23, 2019   
    ...MTT reduction assays showed that early autophagy inhibitors, 3-methyladenin (3-MA) or LY294002, enhanced the loss in cell viability induced by LPS exposure for 48 h. On the contrary, the inhibition of PLD1 and PLD2 prevented the loss in cell viability induced by LPS...In addition, we demonstrate that the PLD pathway modulates the autophagic process in RPE cells. Our findings contribute to the knowledge of the molecular basis of retinal inflammatory and degenerative diseases and open new avenues for potential therapeutic exploration.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  GCN5 inhibition prevents IL-6-induced prostate cancer metastases by inactivating Egr-1. (Pubmed Central) -  Jul 21, 2019   
    Besides, knockdown of GCN5 resulted in the down-regulation of p-Akt and up-regulation of PTEN, which was partly impeded by Egr-1 overexpression. The effects of GCN5 overexpression on cell proliferation and invasion were suppressed by LY294002, In conclusion, these data demonstrated the negative effect of upregulated GCN5 in IL-6-induced metastasis and EMT in PCa cells through PI3K/PTEN/Akt sigaling pathway down-regulating Egr-1 expression.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, ipatasertib (GDC-0068) / Roche, Ipatasertib (RG7440, GDC / 0068)
    Journal:  FGFR mutation promotes chemoresistance by activating Akt signaling in bladder cancer cells. (Pubmed Central) -  Jul 19, 2019   
    The results of the present study demonstrated that the FGFR3 mutation promotes chemoresistance in BCa cells by activating the Akt signaling pathway. The FGFR3 mutation may therefore be used as a predictor of chemosensitivity in patients with BCa.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, CCT128930 / Otsuka
    Preclinical, Journal:  High-concentration hydrogen protects mouse heart against ischemia/reperfusion injury through activation of thePI3K/Akt1 pathway. (Pubmed Central) -  Jul 19, 2019   
    ...C57BL/6 mice were randomly divided into the following groups: sham, I/R, I/R + HCH, I/R + HCH + LY294002 (PI3K inhibitor), I/R + HCH + wortmannin (PI3K inhibitor), I/R + LY294002, and I/R + wortmannin...To investigate the role of Akt1 in the protective effects of HCH, mice were divided into the following groups: I/R + A-674563 (Akt1 selective inhibitor), I/R + HCH + A-674563, I/R + CCT128930 (Akt2 selective inhibitor), and I/R + HCH + CCT128930...HCH resulted in the phosphorylation of Akt1 but not Akt2, and Akt1 inhibition markedly abolished HCH-induced cardioprotection. Our findings reveal that HCH may exert cardioprotective effects through a PI3K-Akt1-dependent mechanism.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, PD98059 / Wayne State University
    Journal:  The role of oxidative stress in the crosstalk between leptin and mineralocorticoid receptor in the cardiac fibrosis associated with obesity. (Pubmed Central) -  Jul 19, 2019   
    Likewise, the MEK/ERK inhibitor, PD98059, and the PI3/Akt inhibitor, LY294002, showed a similar pattern...However, the cardiac fibrosis and enhanced O2.-levels observed in HFD rats were attenuated by MitoTempo, which also prevented the increased circulating leptin and aldosterone levels in HFD fed animals. This study supports a role of mineralocorticoid receptor in the cardiac fibrosis induced by leptin in the context of obesity and highlights the role of the mitochondrial ROS in this process.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Ginsenoside Rb1 increases macrophage phagocytosis through p38 mitogen-activated protein kinase/Akt pathway. (Pubmed Central) -  Jul 18, 2019   
    ...Rb1 also increased Akt phosphorylation, which was suppressed by LY294002, a phosphoinositide 3-kinase inhibitor...These results suggest that ginsenoside Rb1 enhances the phagocytic capacity of macrophages for bacteria via activation of the p38/Akt pathway. Rb1 may be a useful pharmacological adjuvant for the treatment of bacterial infections in clinically relevant conditions.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Preclinical, Journal:  TREM2 inhibits inflammatory responses in mouse microglia by suppressing the PI3K/NF-κB signaling. (Pubmed Central) -  Jul 17, 2019   
    ...The BV2 cells were pre-treated with the PI3 K inhibitor of LY294002 for 1 h and stimulated with LPS for 24 h...Thus, we concluded that TREM2 inhibited neuroinflammation by down-regulating PI3K/AKT and NF-kB signaling in BV2 microglia. Above all, therapeutic enhanced TREM2 expression may be a new strategy for intervention of neuroinflammatory diseases.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Elongator promotes the migration and invasion of hepatocellular carcinoma cell by the phosphorylation of AKT. (Pubmed Central) -  Jul 17, 2019   
    ...Elongator-driven migration and invasion and the expression of MMP-2 and MMP-9 were reduced in HCC cells treated with AKT inhibitor LY294002...Collectively, these results suggested that Elongator activated migration and invasion of HCC cells by promoting the expression of MMP-2 and MMP-9 through the PI3K/AKT signaling pathway. Our work suggests that Elongator might be a potential marker which promotes the metastasis of HCC.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Biomarker, Clinical, Journal:  Identification of serum β-catenin as a biomarker in patients with HBV-related liver diseases. (Pubmed Central) -  Jul 17, 2019   
    Serum β-catenin levels are correlated with necroinflammation parameters but not with viral load. Serum β-catenin has potential to discriminate the phase of HBV-related disorders, particularly predicts the patients with CHB from HHCs and also predicting HCC form chronic HBV infection.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, AZD8055 / AstraZeneca
    Journal:  PI3K inhibitors protect against glucocorticoid-induced skin atrophy. (Pubmed Central) -  Jul 13, 2019   
    Our results built a strong foundation for development of safer GR-targeted therapies for inflammatory skin diseases using combination of glucocorticoids with PI3K/mTOR/Akt inhibitors. FUND: Work is supported by NIH grants R01GM112945, R01AI125366, and HESI-THRIVE foundation.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Brain-derived neurotrophic factor induces thioredoxin-1 expression through TrkB/Akt/CREB pathway in SH-SY5Y cells. (Pubmed Central) -  Jul 11, 2019   
    ...We first demonstrated that cell viability and the expression of Trx-1 were increased by BDNF in SH-SY5Y cells, which were inhibited by the tyrosine kinase B (TrkB) inhibitor, K252a, and the phosphatidylinositol 3-kinase (PI3-K) inhibitor, LY294002...Whereas the expression of Trx-1 induced by BDNF was suppressed by CREB siRNA. Thus, our data suggest that BDNF induces the expression of Trx-1 through the TrkB/Akt/CREB pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Exosomes Derived from Mesenchymal Stem Cells Ameliorate Hypoxia/Reoxygenation-Injured ECs via Transferring MicroRNA-126. (Pubmed Central) -  Jul 10, 2019   
    ...The PI3K inhibitor (LY294002) was used in pathway analysis...Downregulation of miR-126 in MSC-EXs inhibited these effects of MSC-EXs. The results suggest that MSC-EXs could enhance the survival and angiogenic function of H/R-injured ECs via delivering miR-126 to ECs and subsequently activate the PI3K/Akt/eNOS pathway, decrease cleaved caspase-3 expression, and increase angiogenic and growth factors.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  CCDC85B promotes non-small cell lung cancer cell proliferation and invasion. (Pubmed Central) -  Jul 6, 2019   
    In conclusion, CCDC85B was associated with NSCLC progression as it promoted the proliferation and invasion of lung cancer cells through activated AKT/GSK3?/?-catenin oncogenic signaling pathway. Therefore, CCDC85B might serve as a novel target for NSCLC treatment.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Dopamine D2 receptor up-regulates leptin and IL-6 in adipocytes. (Pubmed Central) -  Jul 4, 2019   
    The quinpirole treatment in C57Bl/6J mice increased serum leptin concentration and leptin mRNA in visceral adipocyte tissue but not in subcutaneous adippocytes confirming the stimulatory effect of D2R on leptin in vivo. Our results suggest that the stimulation of D2R increases leptin production and may have tissue specific pro-inflammatory effect in adipocytes.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, U0126 / Promega
    Journal:  Liquiritin and Liquiritigenin Induce Melanogenesis via Enhancement of p38 and PKA Signaling Pathways. (Pubmed Central) -  Jun 27, 2019   
    Furthermore, LQ- or LQG-mediated melanin synthesis was partially blocked by p38 inhibitor (SB203580) and protein kinase A (PKA) inhibitor (H-89); however, ERK kinase (MEK) inhibitor (U0126) and phosphatidylinositol-3-kinase (PI3K) inhibitor (LY294002) had no effect. The results suggest that LQ and LQG enhance melanin synthesis by upregulating the expression of melanogenic enzymes, which were activated by p38 and PKA signaling pathways, leading to MITF expression and CREB phosphorylation.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  miR-188-5p regulates proliferation and invasion via PI3K/Akt/MMP-2/9 signaling in keloids. (Pubmed Central) -  Jun 26, 2019   
    The upregulation of MMP-2 and MMP-9 by miR-188-5p inhibitor could be abolished by LY294002. These findings together demonstrate a tumor-suppressive role of miR-188-5p in KD proliferation and invasion via PI3K/Akt/MMP-2/9 signaling, indicating that miR-188-5p may be a potential prognostic marker and therapeutic target for KDs.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  An essential role of PI3K in the control of West Nile virus infection. (Pubmed Central) -  Jun 24, 2019   
    ...Inhibition of PI3K activity by 3-methyl adenine (3-MA), Wortmannin (WM) and LY294002 (LY) increased viral titers by 3-16 folds in primary mouse macrophages, embryonic fibroblasts and human cell lines...Lastly translocation of interferon regulatory factor 7(IRF7) from the cytosol to the nuclei was effectively blocked in the presence of PI3K inhibitors. Our results clearly define an antiviral role of PI3K by modulating immune responses and demonstrate differential mode of action of three PI3K inhibitors on IFN-I.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, SB202190 / Amgen
    Biomarker, Journal:  Circular RNA regulatory network reveals cell-cell crosstalk in acute myeloid leukemia extramedullary infiltration. (Pubmed Central) -  Jun 22, 2019   
    This study was supported by The National Key Basic Research Program(2018YFC1002500), National Nature Science Foundation of China (81571443 to JW, 81801451 to JG). Taken together, this study reveals the overall alterations of circRNA and mRNA involved in EMI and suggests potential circRNAs may act as biomarkers and targets for early diagnosis and treatment of EMI.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Preclinical, Journal:  C89 Induces Autophagy of Female Germline Stem Cells via Inhibition of the PI3K-Akt Pathway In Vitro. (Pubmed Central) -  Jun 21, 2019   
    ...Western blot confirmed that levels of p-PI3K and p-Akt were significantly reduced in the C89- or LY294002 (PI3K inhibitor)-treated groups compared with controls...Furthermore, C89 induced FGSC autophagy by inhibiting the activity of PI3K and Akt. The PI3K-Akt pathway may be a target to regulate FGSC proliferation and death.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, PD98059 / Wayne State University
    Journal:  The muscarinic antagonist gallamine induces proliferation of airway smooth muscle cells regardless of the cell phenotype. (Pubmed Central) -  Jun 19, 2019   
    In conclusion, this study demonstrated that SIRT1/AMPK and Akt/eNOS signaling pathways are involved in endothelial protection of TASAES against atherosclerotic mice, suggesting that TASAES is a candidate drug for atherosclerosis treatment. Gallamine, in the absence of any agonist, has a transient mitogenic effect on ASMCs, regardless of the cell phenotype, mediated by the PI3K and the MAPK signaling pathways.