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  • ||||||||||  Aliqopa (copanlisib) / Bayer, Rituxan (rituximab) / Biogen, Zenyaku Kogyo, Roche
    Clinical, Journal:  Copanlisib for the treatment of adults with relapsed follicular lymphoma. (Pubmed Central) -  Jan 29, 2021   
    Further investigations of copanlisib within combination regimens will potentially allow to move copanlisib to an earlier line of therapy for FL. However, results of the CHRONOS-4 clinical trial evaluating copanlisib with standard chemoimmunotherapy (rituximab with bendamustine or CHOP) are not yet available.
  • ||||||||||  Review, Journal:  Class I phosphoinositide 3-kinase (PI3K) regulatory subunits and their roles in signaling and disease. (Pubmed Central) -  Jan 28, 2021   
    Given the overwhelming evidence for the involvement of PI3Ks in diseases such as cancer, inflammation, immunodeficiency and diabetes, an understanding of how these regulatory proteins influence PI3K function is essential. This article highlights research deciphering the role of regulatory subunits in PI3K signaling and their involvement in human disease.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal, PARP Biomarker:  Akt/survivin pathway inhibition enhances the apoptotic cell death-induced by alpha-santalol in human prostate cancer cells. (Pubmed Central) -  Jan 28, 2021   
    Furthermore, inhibition of PI3K-Akt pathway by pharmacological inhibitor, LY294002 enhanced the apoptotic cell death induced by alpha-santalol as determined by cell viability, cellular morphology, active caspase-3 activity and expression of cleaved PARP, cleaved caspase-3 levels. In conclusion, the present study provides novel insight into the molecular circuitry of alpha-santalol-induced cell death and reveals that alpha-santalol targets Akt/Survivin pathway to induce cell death and that the cell death is increased in the presence of a known inhibitor of the pathway.
  • ||||||||||  Review, Journal:  Nexus between PI3K/AKT and Estrogen Receptor Signaling in Breast Cancer. (Pubmed Central) -  Jan 28, 2021   
    As a result of these studies, several therapies that combine anti-estrogens that degrade ERα with PI3K/AKT/mTOR inhibitors targeting growth factor signaling or CDK4/6 inhibitors targeting cell cycle machinery are used clinically to treat recurrent ERα+ breast cancers. In this review, we discuss the nexus between ERα-PI3K/AKT/mTOR pathways and how understanding of this nexus has helped to develop combination therapies.
  • ||||||||||  Clinical, Journal:  Combination of PI3K and MEK inhibitors yields durable remission in PDX models of PIK3CA-mutated metaplastic breast cancers. (Pubmed Central) -  Jan 27, 2021   
    AGK promotes the progression of RCC via activating the PI3K/AKT/GSK3β signalling pathway and might be a potential target for the further research of RCC. The treatment of metaplastic breast cancer PDXs by activation of the PI3K-AKT-mTOR and RTK-MAPK pathways at the genomic and protein levels with a combination of PI3K and MEK inhibitors resulted in tumor regression in mutated models and may therefore be of interest for therapeutic purposes.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, PRI-724 / PRISM Pharma, Ohara Pharma
    Journal:  The PI3K/AKT pathway promotes fracture healing through its crosstalk with Wnt/β-catenin. (Pubmed Central) -  Jan 27, 2021   
    Notably, the PI3K/AKT pathway is also activated by Wnt3a and is involved in Wnt3a-induced osteoblast proliferation and differentiation. Hence, our results reveal the existence of a Wnt/PI3K/AKT/β-catenin signaling nexus in osteoblasts, highlighting complex crosstalk between PI3K/AKT and Wnt/β-catenin pathways that are critically implicated in fracture healing.
  • ||||||||||  Journal:  Isoform-Selective PI3K Inhibitors for Various Diseases. (Pubmed Central) -  Jan 26, 2021   
    Because of the important role of type I PI3K family members in various pathophysiological processes, isoform-selective PI3K inhibitors may ultimately have considerable efficacy in a wide range of human diseases. This review summarizes the progress of isoform-selective PI3K inhibitors in preclinical and early clinical studies for anticancer and other various diseases.
  • ||||||||||  Review, Journal:  The PI3K-Akt-mTOR Signaling Pathway in Human Acute Myeloid Leukemia (AML) Cells. (Pubmed Central) -  Jan 26, 2021   
    However, AML patients seem to differ regarding their susceptibility to various small-molecule inhibitors, reflecting biological heterogeneity in the intracellular signaling status. These findings should be further investigated in both preclinical and clinical settings, along with the potential use of this pathway as a prognostic biomarker, both in patients receiving intensive curative AML treatment and in elderly/unfit receiving AML-stabilizing treatment.
  • ||||||||||  docetaxel / Generic mfg.
    Journal:  CNTN-1 promotes docetaxel resistance and epithelial-to-mesenchymal transition via the PI3K/Akt signaling pathway in prostate cancer. (Pubmed Central) -  Jan 26, 2021   
    Knockdown of CNTN-1 resulted in an anti-tumor effect in the xenograft tumor model, and decreased activity of the phosphoinositide 3-kinase (PI3K)/Akt signaling pathway both in vitro and in vivo. The results of the present study suggest that downregulation of CNTN-1 may be an important mechanism to reverse chemoresistance in Dox-resistant PCa progression, thus shedding light on the development of novel anti-tumor therapeutics for the treatment of PCa.
  • ||||||||||  Journal, IO biomarker:  TSPAN7 Exerts Anti-Tumor Effects in Bladder Cancer Through the PTEN/PI3K/AKT Pathway. (Pubmed Central) -  Jan 26, 2021   
    Western blotting showed that overexpression of TSPAN7 activated Bax, cleaved caspase-3 and PTEN but inactivated Bcl-2, p-PI3K, and p-AKT to inhibit BCa cell growth via the PTEN/PI3K/AKT pathway. Taken together, our study will help identify a potential marker for BCa diagnosis and supply a target molecule for BCa treatment.
  • ||||||||||  Journal, PARP Biomarker:  HS‑146, a novel phosphoinositide 3‑kinase α inhibitor, induces the apoptosis and inhibits the metastatic ability of human breast cancer cells. (Pubmed Central) -  Jan 23, 2021   
    Hypoxia‑inducible factor (HIF)‑1α and vascular endothelial growth factor (VEGF) expression were also suppressed by HS‑146 under hypoxic conditions, and HS‑146 inhibited the migration and invasion of MCF‑7 cells in a concentration‑dependent manner. On the whole, the findings of the present study suggest that HS‑146, a novel PI3Kα inhibitor, may be an effective novel therapeutic candidate that suppresses breast cancer proliferation and metastasis by inhibiting the PI3K/Akt/mTOR pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Down-regulation of miRNA-196b expression inhibits the proliferation, migration and invasiveness of HepG2 cells while promoting their apoptosis via the PI3K/Akt signaling pathway. (Pubmed Central) -  Jan 23, 2021   
    The HepG2 cells were also treated with PI3K/Akt signaling pathway inhibitor LY294002, and its effect on cell proliferation, migration, invasion, and apoptosis, and expressions of PIK3, Akt, and p-Akt proteins were determined...Similarly, the protein expressions of PIK3 and p-Akt in the non-treatment group was significantly upregulated, relative to the treatment group (p < 0.05), but there was no significant difference in the expression of Akt protein between the two groups (p > 0.05). Downregulation of miRNA-196b expression inhibits the proliferation, migration and invasiveness of HepG2 cells, while promoting their apoptosis via a mechanism involving the PI3K/Akt signaling pathway.
  • ||||||||||  Miostat (carbachol) / Novartis
    Journal:  Muscarinic-dependent phosphorylation of the cardiac ryanodine receptor by protein kinase G is mediated by PI3K-AKT-nNOS signaling. (Pubmed Central) -  Jan 23, 2021   
    We found that this signaling pathway is compartmentalized in myocytes, as it was distinct from atrial natriuretic peptide receptor (ANPR)-cGMP-PKG-RyR2 Ser-2808 signaling and independent of muscarinic-induced phosphorylation of Ser-239 in vasodilator-stimulated phosphoprotein (VASP). These results provide detailed insights into muscarinic-induced PKG signaling and the mediators that regulate cardiac RyR2 phosphorylation critical for cardiovascular function.
  • ||||||||||  Journal:  Leptin Regulated ILC2 Cell through the PI3K/AKT Pathway in Allergic Rhinitis. (Pubmed Central) -  Jan 23, 2021   
    The AR mice treated with leptin showed as stronger ILC2 inflammation and symptoms compared with control mice. Our data provide evidence that upregulation of leptin promotes ILC2 responses in AR and this process was achieved through the PI3K/AKT pathway.
  • ||||||||||  Journal, Microsatellite instability:  Downregulation of GLYR1 contributes to microsatellite instability colorectal cancer by targeting p21 via the p38MAPK and PI3K/AKT pathways. (Pubmed Central) -  Jan 23, 2021   
    Flavokawain-B targets gemcitabine-resistant NSCLC cells selectively without inducing any significant toxicity in normal cells and these effects are mediated via apoptosis induction, ROS production, loss of MMP, suppression of cell migration and invasion and blocking PI3K/AKT signalling pathway. Ours is the first study to elucidate the role of GLYR1 in tumors and provide evidence for GLYR1 as a biological marker that reflects the degree of malignancy and sensitivity to 5-FU in MSI CRC.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Preclinical, Journal:  Hypoglycemic Activity and the Mechanisms of Lycium Bark Extract in db/db Mice. (Pubmed Central) -  Jan 23, 2021   
    Furthermore, LBE increased the glucose uptake, which was measured using C2C12 myotubes, in a concentration-dependent manner, independent of the addition of a phosphatidylinositol 3-kinase inhibitor (i.e., LY294002) and an AMP-activated kinase inhibitor (i.e., dorsomorphin)...These results suggested that LBE decreased the blood glucose level by additive effect such as improvement of the insulin secretion, promoting activity of glucose uptake. These findings suggested that LBE administration can be a novel therapeutic approach for type 2 diabetes.