- |||||||||| quercetin (LY294002) / Eli Lilly, chlorpromazine / Generic mfg.
Journal: Mediated pathways of exosomes uptake by stem cells of apical papilla (Pubmed Central) - Feb 25, 2020 SCAP could uptake the DPSCs derived exosomes, and low temperature could inhibit this process. The exosomes uptake of SCAP was mediated by the clathrin endocytosis pathway, caveolae-mediated endocytosis and macropinocytosis pathway.
- |||||||||| quercetin (LY294002) / Eli Lilly
Journal: Akirin1 promotes myoblast differentiation by modulating multiple myoblast differentiation factors. (Pubmed Central) - Feb 24, 2020 Similarly, we found that enhanced MEF2B expression by Akirin1 can be abrogated by treatment with LY294002, a PI3K inhibitor. Together, our results indicate that Akirin1 promotes myoblast differentiation by acting on the p38 and PI3K pathways and subsequently inducing the expression of myoblast differentiation factors.
- |||||||||| daunorubicin / Generic mfg., Hikma, quercetin (LY294002) / Eli Lilly
Journal, IO Biomarker: LY294002 Enhaces Chemosensitivity of K562 Cells to Daunorubicin (Pubmed Central) - Feb 23, 2020 Activation of GPER1 attenuated RGCs apoptosis and Müller cells gliosis, indicating GPER1 as a potential treatment target in RGCs degeneration diseases. LY294002 has the sensibilizative effect on DNR chemotherapy, which may be relative with blocking the cell cycle and inducing cell apoptosis.
- |||||||||| quercetin (LY294002) / Eli Lilly
Journal: COX‑2 promotes epithelial‑mesenchymal transition and migration in osteosarcoma MG‑63 cells via PI3K/AKT/NF‑κB signaling. (Pubmed Central) - Feb 21, 2020 A Transwell chamber migration assay was performed to quantify the migration of the COX‑2‑transduced cells, and of cells treated with a COX‑2 inhibitor (NS398) or a PI3K inhibitor (LY294002)...The total protein levels of PI3K, AKT and IKK were not changed among the treatment groups. In summary, COX‑2 overexpression decreased the expression levels of the epithelial protein E‑cadherin and increased the expression levels of the mesenchymal proteins vimentin, MMP‑2 and MMP‑9, as well as promoted cell migration, by activating the PI3K/AKT/NF‑κB signaling pathway.
- |||||||||| MK-2206 / Merck (MSD), quercetin (LY294002) / Eli Lilly, dactolisib (RTB101) / Novartis, PureTech
Journal: Deoxyshikonin isolated from Arnebia euchroma inhibits colorectal cancer by down-regulating the PI3K/Akt/mTOR pathway. (Pubmed Central) - Feb 16, 2020 In vivo study, the weight of tumour tissues at deoxyshikonin groups was significantly reduced compared with the control group, and PI3K, p-PI3K, Akt, p-Akt308 and mTOR expression was decreased. Discussion and We can conclude that deoxyshikonin isolated from Arnebia euchroma inhibited CRC through the PI3K/Akt/mTOR pathway.
- |||||||||| quercetin (LY294002) / Eli Lilly
Journal: MiR-25-3p promotes malignant phenotypes of retinoblastoma by regulating PTEN/Akt pathway. (Pubmed Central) - Feb 15, 2020 Moreover, LY294002 treatment or restoring PTEN expression abolished the effects of miR-25-3p on cell invasion, colony formation and anchorage-independent growth in vitro and tumor xenograft growth in vivo. Taken together, our results suggested that miR-25-3p promotes malignant transformation of retinoblastoma cells by suppressing PTEN.
- |||||||||| quercetin (LY294002) / Eli Lilly
Protective effect of piceatannol against oxidative stress-induced apoptosis in ARPE-19 cells and its mechanism (102B, Pennsylvania Convention Center) - Feb 13, 2020 - Abstract #ACSSp2020ACS_Sp_10101; LY294002 (PI3K inhibitor) dramatically blocked piceatannol-mediated increasing of Nrf2 nuclear translocation, HO-1 expression, and cytoprotective activity, indicating the involvement of PI3K/Akt pathway in the cytoprotective effect of piceatannol. The results from this suggest the potential of piceatannol in reducing the risk of age-related macular degeneration.
- |||||||||| metformin / Generic mfg., sirolimus / Generic mfg.
Journal: MicroRNA‑212 facilitates the motility and invasiveness of esophageal squamous carcinoma cells. (Pubmed Central) - Feb 8, 2020 These data suggest that miR‑212 activates multiple signaling cascades and facilitates ESCC cell motility and invasion by promoting the epithelial‑mesenchymal transition and degrading the ECM. Berberine may be a potential therapeutic agent against metastasis in patients with ESCC, who express high levels of miR‑212.
- |||||||||| quercetin (LY294002) / Eli Lilly
Journal: Orthosilicic Acid Accelerates Bone Formation in Human Osteoblast-Like Cells Through the PI3K-Akt-mTOR Pathway. (Pubmed Central) - Feb 7, 2020 However, with the addition of PI3K-Akt-mTOR pathway-specific inhibitor LY294002, the expression of PI3K, P-Akt, P-mTOR, RUNX2, COL1, ALP, OCN, and P1NP decreased. The results indicated that the PI3K-Akt-mTOR pathway played a positive regulatory role in the process of orthosilicic acid-mediated osteogenesis in vitro.
- |||||||||| doxorubicin hydrochloride / Generic mfg.
Journal: Doxorubicin as a fluorescent reporter identifies novel MRP1 (ABCC1) inhibitors missed by calcein-based high content screening of anticancer agents. (Pubmed Central) - Feb 7, 2020 Six drugs (afatinib, celecoxib, doramapimod, mifepristone, MK-2206 and rosiglitazone) were evaluated for their ability to reverse resistance of MRP1-overexpressing H69AR lung cancer cells against vincristine, doxorubicin and etoposide...Anti-cancer agents that exhibit MRP1 inhibition may be used to reverse multidrug resistance or to improve the efficacy and reduce the toxicity of various cancer chemotherapies. On the other hand, anti-cancer drugs that did not interact with MRP1 carry a low risk for developing MRP1-mediated resistance.
- |||||||||| quercetin (LY294002) / Eli Lilly, Zydelig (idelalisib) / Gilead, SP600125 / BMS
Preclinical, Journal: Echinochrome A Promotes Ex Vivo Expansion of Peripheral Blood-Derived CD34 Cells, Potentially through Downregulation of ROS Production and Activation of the Src-Lyn-p110δ Pathway. (Pubmed Central) - Feb 7, 2020 Moreover, p38-MAPK/JNK inhibitors SB203580 and SP600125 promoted ex vivo expansion of CD34 cells...Furthermore, the Ech A-induced ex vivo expansion of CD34 cells was inhibited by pretreatment with the Src family inhibitor PP1 and p110δ inhibitor CAL-101; PP1 blocked p110δ upregulation and PI3K/Akt activation, whereas CAL-101 and PI3K/Akt pathway inhibitor LY294002 did not block Src/Lyn activation...In conclusion, Ech A promotes the ex vivo expansion of CD34 cells through Src/Lyn-mediated p110δ expression, suppression of ROS generation, and p38-MAPK/JNK activation. Hence, Ech A is a potential candidate modality for the ex vivo, and possibly in vivo, expansion of CD34 cells.
- |||||||||| quercetin (LY294002) / Eli Lilly
Preclinical, Journal, IO Biomarker: Osteopontin promotes rat hepatocyte proliferation both in vitro and in vivo. (Pubmed Central) - Feb 7, 2020 Moreover, LR rate, serum IL-6 and TNF-α, Ki-67 proportion and the phosphorylation of STAT3, AKT and p65 were augmented by rrOPN treatment. OPN promotes hepatocyte proliferation both in vitro and in vivo through STAT3 and AKT signaling pathways.
- |||||||||| quercetin (LY294002) / Eli Lilly
Journal: Calycosin down-regulates c-Met to suppress development of glioblastomas. (Pubmed Central) - Jan 31, 2020 However, an AKT inhibitor (LY294002) only effected on MMP9 and p-AKT, not on c-Met. These data collectively indicated that calycosin possibility targeting on c-Met and exert an anti-tumor role via MMP9 and AKT.
- |||||||||| MK-2206 / Merck (MSD), quercetin (LY294002) / Eli Lilly
Journal: Effect of PI3K/Akt Signaling Pathway on PRAS40Thr246 Phosphorylation in Gastric Cancer Cells. (Pubmed Central) - Jan 30, 2020 The levels of PI3K/Akt signaling pathway related proteins and p-PRAS40Thr246 were significantly increased in gastric cancer cells. p-PRAS40-Thr246 was able to reflect the activation of the PI3K/Akt signaling pathway, reflecting the sensitivity of the PI3K/AKT signaling pathway to inhibitors.
- |||||||||| quercetin (LY294002) / Eli Lilly
Journal: Bombyxin/Akt signaling in relation to the embryonic diapause process of the silkworm, Bombyx mori. (Pubmed Central) - Jan 25, 2020 Results showed that GSK-3β phosphorylation stimulated by dechorionation was blocked by LY294002, a specific phosphatidylinositol 3-kinase (PI3K) inhibitor, indicating involvement of PI3K in GSK-3β phosphorylation in dechorionated eggs...Taken together, our results indicated that PI3K/Akt is an upstream signaling pathway for GSK-3β phosphorylation and is associated with the diapause process of B. mori eggs. To our knowledge, this is the first study to demonstrate the potential correlation between bombyxin/Akt signaling and the embryonic diapause process.
- |||||||||| sirolimus / Generic mfg.
Clinical, Journal: Signaling pathways and inhibitors of cells from patients with kaposiform lymphangiomatosis. (Pubmed Central) - Jan 25, 2020 Our studies using cells from KLA patient lesions demonstrate that these cells are highly proliferative and the PI3K-AKT-mTOR and MAPK pathways are promising therapeutic targets. Development and clinical trials of PI3K, AKT, and MAPK inhibitors for cancer treatment and the data in this study lend support for early clinical trials assessing the efficacy of these inhibitors in KLA patients.
- |||||||||| quercetin (LY294002) / Eli Lilly
Clinical, Journal: Anti-tumor efficacy of phellamurin in osteosarcoma cells: Involvement of the PI3K/AKT/mTOR pathway. (Pubmed Central) - Jan 23, 2020 LY294002 effectively inhibited the PI3K/AKT/mTOR signaling pathway, repressed cell viability and induced apoptosis in OS cells...In conclusion, Phe suppressed the viability and induced apoptosis in OS cells, at least, partially by inhibiting the PI3K/AKT/mTOR pathway. Our study suggested that Phe might be a new and potential chemotherapeutic agent for the treatment of OS.
- |||||||||| quercetin (LY294002) / Eli Lilly, PD98059 / Wayne State University
Biomarker, Journal: RRM2 is a potential prognostic biomarker with functional significance in glioma. (Pubmed Central) - Jan 21, 2020 Moreover, overexpression of RRM2 failed to increase the expression of cyclin B1, cyclin D1, and N-cadherin when phosphorylation of AKT and ERK1/2 was suppressed by LY294002 or PD98059. These findings indicated that RRM2 is a positive regulator of glioma progression which contributes to the migration and proliferation of glioma cells through ERK1/2 and AKT signalings and might be a novel prognostic indicator for glioma patients.
- |||||||||| quercetin (LY294002) / Eli Lilly
Preclinical, Journal: Kaempferol can be used as the single antioxidant in the in vitro culture medium, stimulating sheep secondary follicle development through the phosphatidylinositol 3-kinase signaling pathway. (Pubmed Central) - Jan 21, 2020 In addition, inhibition of PI3K activity was performed through pretreatment in medium supplemented with LY294002...In conclusion, 1 μM kaempferol can be used as the single antioxidant present in the base medium, replacing the addition of transferrin, selenium and ascorbic acid during in vitro culture of ovine secondary follicles, maintaining follicular survival, increasing active mitochondria levels, and promoting the oocyte meiotic resumption. Moreover, the development of the ovine secondary follicle stimulated by kaempferol is mediated by PI3K pathway.
- |||||||||| quercetin (LY294002) / Eli Lilly
Biomarker, Journal, PD(L)-1 Biomarker, IO Biomarker: Cancer-associated fibroblasts promote PD-L1 expression in mice cancer cells via secreting CXCL5. (Pubmed Central) - Jan 19, 2020 Meanwhile, the B16/CT26 xenograft tumor models were used and both CXCR2 and p-AKT were found to be positively correlated with PD-L1 in the xenograft tumor tissues. The immunosuppressive action of CAFs on tumor cells is probably reflective of them being a potential therapeutic biomarker for melanoma and CRC.
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