- |||||||||| irinotecan / Generic mfg.
Journal: Nitidine chloride exerts anti-inflammatory action by targeting Topoisomerase I and enhancing IL-10 production. (Pubmed Central) - Jul 2, 2020 In LPS-stimulated RAW264.7 cells and in peritoneal macrophages from endotoxemic mice, NC and TOP1 inhibitors significantly enhanced the activation of Akt, a critical signal transducer for IL-10 production, and inhibition of Akt prevented these compounds from enhancing IL-10 production and ameliorating endotoxemia. These data indicated that NC and TOP1 inhibitors are able to exert anti-inflammatory action through enhancing Akt-mediated IL-10 production and may assist with the treatment of inflammatory diseases.
- |||||||||| quercetin (LY294002) / Eli Lilly
[VIRTUAL] 5-(3’, 4’-Dihydroxyphenyl-valerolactone) regulates DNA methylation in UVB-irradiated keratinocytes () - Jul 1, 2020 - Abstract #SID2020SID_542; Overall, our results indicate that DHPV regulates DNA methylation by suppression of AKT1 phosphorylation and DNMT1 stabilization, and suggest the protective role of DHPV on keratinocytes from UVB-induced epigenetic changes. Considering that DNA methylation changes are frequently observed in skin cancers, we suggest that DHPV could be a potential substance that can protect our skin from UVB-cancer initiation.
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Journal: C-Terminus of E1A Binding Protein 1 Stimulates Malignant Phenotype in Human Hepatocellular Carcinoma. (Pubmed Central) - Jun 28, 2020 The phosphatidylinositol-3-kinase (PI3K) inhibitor LY294002 was utilized to treat hepatic astrocyte cells, and the impact of CTBP1 on proliferation and metastasis of hepatic astrocytes and HCC cells was accessed by CCK-8, clone-forming, Transwell chamber, and cell scratch assays...Moreover, genetic loss of CTBP1 significantly reduced the metastatic activity of HCC cells in vitro. CONCLUSIONS Our data suggest that the loss of CTBP1 suppresses cell proliferative and invasive activity of HCC cells via the PI3K/Akt pathway.
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Journal: Resveratrol Attenuates Oxidative Stress-Induced Intestinal Barrier Injury through PI3K/Akt-Mediated Nrf2 Signaling Pathway. (Pubmed Central) - Jun 28, 2020 Consistent with Nrf2 knockdown, the PI3K/Akt inhibitor LY294002 significantly suppressed RSV-induced Nrf2 phosphorylation and RSV-induced increase of TJ protein levels and antioxidant gene expression under HO treatment (P < 0.05). Collectively, these results demonstrate that RSV can directly protect IPEC-J2 cells against oxidative stress through the PI3K/Akt-mediated Nrf2 signaling pathway, suggesting that RSV may be an effective feed additive against intestinal damage in livestock production.
- |||||||||| doxorubicin hydrochloride / Generic mfg.
Journal: Shenmai Injection Protects Against Doxorubicin-Induced Cardiotoxicity via Maintaining Mitochondrial Homeostasis. (Pubmed Central) - Jun 27, 2020 SMI increased ratio of L-OPA1 to S-OPA1, levels of AMPK phosphorylation, and DRP1 phosphorylation (Ser637) in order to prevent DOX-induced excessive mitochondrial fission and insufficient mitochondrial fusion. In conclusion, SMI prevents DOX-induced cardiotoxicity, inhibits mitochondrial oxidative stress and mitochondrial fragmentation through activation of AMPK and PI3K/Akt/GSK-3β signaling pathway.
- |||||||||| quercetin (LY294002) / Eli Lilly, U0126 / Promega, SP600125 / BMS
Preclinical, Journal: Ochratoxin A suppresses proliferation of Sertoli and Leydig cells in mice. (Pubmed Central) - Jun 26, 2020 In conclusion, the results of the present study demonstrate the mechanism underlying the antiproliferative effects of OTA in mouse testicular cells. Exposure to OTA may result in abnormal sperm maturation and the failure of spermatogenesis, which leads to male infertility.
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Journal: Neuregulin-1β attenuates sepsis-induced diaphragm atrophy by activating the PI3K/Akt signaling pathway. (Pubmed Central) - Jun 26, 2020 In addition, NRG-1β could activate the PI3K/Akt signaling pathway in L6 myotubes treated with LPS, while the PI3K inhibitor LY294002 blocked the effects of NRG-1β. NRG-1 expression in the diaphragm was reduced during sepsis, and exogenously administered recombinant human NRG-1β could attenuate sepsis-induced diaphragm atrophy by activating the PI3K/Akt signaling pathway.
- |||||||||| quercetin (LY294002) / Eli Lilly, selisistat (SEN-196) / AOP Orphan Pharma
Journal: Resveratrol increase myocardial Nrf2 expression in type 2 diabetic rats and alleviate myocardial ischemia/reperfusion injury (MIRI). (Pubmed Central) - Jun 25, 2020 NRG-1 expression in the diaphragm was reduced during sepsis, and exogenously administered recombinant human NRG-1β could attenuate sepsis-induced diaphragm atrophy by activating the PI3K/Akt signaling pathway. Resveratrol can enhance the expression of Nrf2 in a diabetic heart by stimulating SIRT1 or inhibiting GSK3β, alleviating myocardial oxidative stress, and improving ischemia-reperfusion injury.
- |||||||||| Journal, IO Biomarker: Polyphyllin VI, a saponin from Trillium tschonoskii Maxim. induces apoptotic and autophagic cell death via the ROS triggered mTOR signaling pathway in non-small cell lung cancer. (Pubmed Central) - Jun 19, 2020
The apoptotic cell death induced by PPVI was confirmed, and it was significantly suppressed by the overexpression of AKT, ERK and mTOR, and the induced autophagic cell death which was depended on the Atg7 was decreased by the inhibitors, such as LY294002 (LY), Bafilomycin A1 (Baf), Compound C (CC) and SBI-0206965 (SBI)...Finally, the anti-tumor growth activity of PPVI in vivo was validated in A549 bearing athymicl nude mice. Taken together, our data have firstly demonstrated that PPVI is the main component in TTM that exerts the anti-proliferative effect by inducing apoptotic and autophagic cell death in NSCLC via the ROS-triggered mTOR signaling pathway, and PPVI may be a promising candidate for the treatment of NSCLC in future.
- |||||||||| sirolimus / Generic mfg.
Journal: Long-term arsenite exposure decreases autophagy by increased release of Nrf2 in transformed human keratinocytes. (Pubmed Central) - Jun 19, 2020 In conclusion, our data suggest that long-term exposure to arsenite promotes Nrf2 upregulation via the PI3K/Akt pathway and, along with upregulation of downstream mTOR and Bcl2, contributes to autophagy dysfunction in transformed HaCaT cells. This work provides new insights into the mechanisms underlying arsenite-induced autophagy dysfunction in cancer promotion and malignancy progression.
- |||||||||| quercetin (LY294002) / Eli Lilly
Journal: MiR-92b-3p promotes neurite growth and functional recovery via the PTEN/AKT pathway in acute spinal cord injury. (Pubmed Central) - Jun 15, 2020 The PTEN/AKT pathway-related proteins and their roles in miR-92b-3p regulation were also identified using western blotting and immunofluorescence in vitro through LY294002, an AKT inhibitor...Moreover, miR-92b-3p could also improve the BBB scale as well as GAP43 and NF-200 expression levels in vivo. Collectively, these results indicate that miR-92b-3p promotes neurite growth and functional recovery through the PTEN/AKT pathway in ASCI.
- |||||||||| quercetin (LY294002) / Eli Lilly
Journal, IO Biomarker: Angiotensin II induces apoptosis of cardiac microvascular endothelial cells via regulating PTP1B/PI3K/Akt pathway. (Pubmed Central) - Jun 14, 2020 Furthermore, cotreatment with PTP1B inhibitor significantly decreased the number of apoptotic CMECs induced by Ang II, along with increased PI3K expression, phosphorylation of Akt and the ratio of Bcl-2/Bax, decreased caspase-3 activity, and a cleaved caspase-3/caspase-3 ratio, while treatment with LY294002 partly inhibited the anti-apoptotic effect of the PTP1B inhibitor. Ang II induces apoptosis of primary rat CMECs via regulating the PTP1B/PI3K/Akt pathway.
- |||||||||| quercetin (LY294002) / Eli Lilly
Journal, PARP Biomarker: NANOG Attenuates Hair Follicle-Derived Mesenchymal Stem Cell Senescence by Upregulating PBX1 and Activating AKT Signaling. (Pubmed Central) - Jun 14, 2020 Moreover, blocking AKT with the PI3K/AKT inhibitor LY294002 or knocking down AKT via RNA interference significantly decreased PBX1 expression, while increasing p16 and p21 expression and the number of SA-β-gal-positive cells. In conclusion, our findings show that NANOG delays HF-MSC senescence by upregulating PBX1 and activating AKT signaling and that a feedback loop likely exists between PBX1 and AKT signaling.
- |||||||||| quercetin (LY294002) / Eli Lilly
Journal: Ginsenoside Re Attenuates High Glucose-Induced RF/6A Injury via Regulating PI3K/AKT Inhibited HIF-1α/VEGF Signaling Pathway. (Pubmed Central) - Jun 13, 2020 Afterwards, the effects of Re on the regulation of apoptotic related proteins, VEGF and HIF-1α nuclear transcription was partially reversed. These findings suggested the exerting protective effects of ginsenoside Re were associated with regulating of PI3K/AKT and HIF-1α/VEGF signaling pathway, which indicates that ginsenoside Re may ameliorates HG-induced retinal angiogenesis and suggests the potential for the development of Re as a therapeutic for DR.
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Journal: Negative correlation between serum levels of homocysteine and apolipoprotein M. (Pubmed Central) - Jun 12, 2020 These findings suggested the exerting protective effects of ginsenoside Re were associated with regulating of PI3K/AKT and HIF-1α/VEGF signaling pathway, which indicates that ginsenoside Re may ameliorates HG-induced retinal angiogenesis and suggests the potential for the development of Re as a therapeutic for DR. Present study demonstrates that Hcy downregulates the expression of apoM by mechanisms involving the PI3K signal pathway.
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Journal: Epidermal growth factor upregulates expression of MUC5AC via TMEM16A, in chronic rhinosinusitis with nasal polyps. (Pubmed Central) - Jun 11, 2020 Cultures pretreated for 30 min with T16Ainh-A01 (a specific TMEM16A inhibitor) or LY294002 (a phosphoinositide 3-kinase (PI3K) inhibitor) were also assessed similarly following EGF treatment...This study demonstrated that EGF upregulates the expression of MUC5AC in HNECs from CRSwNP patients. Furthermore, the EGF-mediated regulation of MUC5AC expression is likely to involve a PI3K-TMEM16A signalling pathway in CRSwNP.
- |||||||||| quercetin (LY294002) / Eli Lilly
Journal: Apelin shorten QT interval by inhibiting Kir2.1/I via a PI3K way in acute myocardial infarction. (Pubmed Central) - Jun 10, 2020 In cultured neonatal mouse cardiomyocytes, Apelin (1 μmol/L) restored hypoxia-induced Kir2.1 down-regulation, which was abolished by IP3K inhibitor LY-294002...These results showed that Apelin enhanced I/Kir2.1 currents via IP3K pathway as by rescue ischemia- and hypoxia-induced RMP depolarization and prolongation of QT interval, which may prevent or cure acute ischemic-mediated arrhythmias. This study brings new information to anti-arrhythmic theories and provides a potential target for the clinical management of acute ischemia-related arrhythmias.
- |||||||||| quercetin (LY294002) / Eli Lilly, U0126 / Promega
Preclinical, Journal: Leukotriene B induces proliferation of rat pulmonary arterial smooth muscle cells via modulating GSK-3β/β-catenin pathway. (Pubmed Central) - Jun 9, 2020 In addition, inactivation or lack of GSK-3β up-regulated β-catenin and cyclin D1 in PASMCs. Taken together, our study indicates that activation of PI3K/Akt and ERK1/2 pathways mediate LTB-induced PASMCs proliferation by modulating GSK-3β/β-catenin/cyclin D1 axis and suggests that targeting this pathway might have potential value in alleviating vascular remodeling and benefit PAH.
- |||||||||| quercetin (LY294002) / Eli Lilly
Preclinical, Journal: Effect of Bmi-1 Silencing on the Proliferation of K562/ADM Cells in vitro and in vivo (Pubmed Central) - Jun 9, 2020 Taken together, our study indicates that activation of PI3K/Akt and ERK1/2 pathways mediate LTB-induced PASMCs proliferation by modulating GSK-3β/β-catenin/cyclin D1 axis and suggests that targeting this pathway might have potential value in alleviating vascular remodeling and benefit PAH. Bmi-1 can mediate the proliferation of K562/ADM cell, the PTEN/p-AKT might be involved in this pathway.
- |||||||||| quercetin (LY294002) / Eli Lilly
Journal, IO Biomarker: Sodium Tanshinone II Sulfonate A Ameliorates Hypoxia-Induced Pulmonary Hypertension. (Pubmed Central) - Jun 9, 2020 In addition, hypoxia-induced increases in PAP, cardiac hypertrophy, and lung expression of the proteins PI3K/Akt/mTOR/autophagy pathway were partially reversed by treatment with LY294002. STS alleviates hypoxia-induced PH by promoting apoptosis, inhibiting PI3K/AKT/mTOR pathway, up-regulating autophagy, and inhibiting inflammatory responses.
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