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  • ||||||||||  Review, Journal:  Histone deacetylases as an epigenetic pillar for the development of hybrid inhibitors in cancer. (Pubmed Central) -  Dec 20, 2019   
    In this regard, because of their multiple anticancer effects, histone deacetylase inhibitors have become a privileged tool for the development of hybrid drugs. The clinical trials of two multi-acting chimeras, HDAC/EGFR/HER2 and HDAC/PI3K inhibitors, encouraged the design of novel hybrids, such as compounds 22a (LSD1/HDAC) and 16a (CDK4/JAK1/HDAC), which showed superior anticancer effects than single-targeting agents or their combination both in cellular and mouse models.
  • ||||||||||  Journal:  Liensinine induces gallbladder cancer apoptosis and G2/M arrest by inhibiting ZFX-induced PI3K/AKT pathway. (Pubmed Central) -  Dec 20, 2019   
    Liensinine also affected GBC cell cycle progression and induced apoptosis by down-regulating phosphorylated protein kinase B (AKT), phosphorylated protein kinase B (p-AKT), phosphatidylinositol 3-kinase (PI3K), and Zinc finger X-chromosomal protein (ZFX) proteins. Liensinine induced G2/M arrest and apoptosis in gallbladder cancer, suggesting that liensinine might represent a novel and effective agent against gallbladder cancer.
  • ||||||||||  Review, Journal:  PI3Kδ is a Treg target in cancer immunotherapy. (Pubmed Central) -  Dec 20, 2019   
    In this review we explore how PI3Kδ contributes to signalling through several major immune cell receptors, including the T cell receptor and costimulatory receptors such as CD28 and ICOS, but is antagonised by the immune checkpoint receptors CTLA-4 and PD-1. Understanding how PI3Kδ inhibition affects Treg signalling events will help inform how best to use PI3Kδ inhibitors in clinical cancer treatment.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, Faslodex (fulvestrant) / AstraZeneca, flutamide / Generic mfg.
    Journal:  Dehydroepiandrosterone Prevents HO-Induced BRL-3A Cell Oxidative Damage through Activation of PI3K/Akt Pathways rather than MAPK Pathways. (Pubmed Central) -  Dec 20, 2019   
    These effects of DHEA were not observed when the cells were pretreated with known antagonists of sex hormones (Trilostane, Flutamide, or Fulvestrant)...These effects of DHEA were abolished when the cells were pretreated with the PI3K inhibitor LY294002...In conclusion, our data demonstrate that DHEA protects BRL-3A cells against HO-induced oxidative stress and apoptosis through mechanisms that do not involve its biotransformation into steroid hormones or the activation of sex hormone receptors. Importantly, the protective effect of DHEA on BRL-3A cells was mainly associated with PI3K/Akt signaling pathways, rather than MAPK signaling pathways.
  • ||||||||||  etoposide IV / Generic mfg.
    Preclinical, Journal:  p53-Mediated PI3K/AKT/mTOR Pathway Played a Role in Ptox-Induced EMT Inhibition in Liver Cancer Cell Lines. (Pubmed Central) -  Dec 20, 2019   
    Moreover, recent study revealed that etoposide could also inhibit EMT...In addition, the Ptox exhibited significant inhibition in migration and invasion, which correlated with downregulation of matrix metalloproteinase (MMP). More importantly, Ptox could inhibit EMT in the absence or presence of TGF-β1, concomitant to the ROS production, and the additional evidence revealed that Ptox downregulated AKT/mTOR through upregulation of p53, indicating that Ptox induced EMT inhibition through the p53/PI3K/AKT/mTOR pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Preclinical, Journal, IO Biomarker:  Mytoxin B and Myrothecine A Induce Apoptosis in Human Hepatocarcinoma Cell Line SMMC-7721 via PI3K/Akt Signaling Pathway. (Pubmed Central) -  Dec 20, 2019   
    Moreover, the expression levels of caspases-3, -8, and -9, and cleaved caspases-3, -8, and -9 were all upregulated in both mytoxin B and myrothecine A-treated cells in Western blot analysis, which indicated that both compounds might induce SMMC-7721 cells apoptosis through not only the death receptor pathway but also the mitochondrial pathway. Finally, mytoxin B and myrothecine A were found to reduce the activity of PI3K/Akt signaling pathway that was similar to the effect of LY294002 (a potent and specific PI3K inhibitor), suggesting that both mytoxin B and myrothecine A might induce SMMC-7721 cells apoptosis via PI3K/Akt pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, PD98059 / Wayne State University
    Journal:  Serine Protease from Nereis virens Inhibits H1299 Lung Cancer Cell Proliferation via the PI3K/AKT/mTOR Pathway. (Pubmed Central) -  Dec 20, 2019   
    The effect of NAP on the downregulation of p-ERK and p-AKT was enhanced by the LY294002 (a PI3K inhibitor), while the inhibitor PD98059 had no obvious effect. Overall, the results suggested that NAP exhibits antiproliferative activity by inducing apoptosis, through the inhibition of the PI3K/AKT/mTOR pathway.
  • ||||||||||  Review, Journal:  Strategies to Overcome Resistance Mechanisms in T-Cell Acute Lymphoblastic Leukemia. (Pubmed Central) -  Dec 20, 2019   
    In this work, we describe pathways of resistance to common chemotherapeutic agents including glucocorticoids and review the resistance mechanisms to targeted therapy such as IL7R, PI3K-AKT-mTOR, NOTCH1, BRD4/MYC, Cyclin D3: CDK4/CDK6, BCL2 inhibitors, and selective inhibitors of nuclear export (SINE). Finally, to overcome the limitations of the current trial-and-error method, we summarize the experiences of anti-cancer drug sensitivity resistance profiling (DSRP) approaches as a rapid and relevant strategy to infer drug activity and provide functional information to assist clinical decision one patient at a time.
  • ||||||||||  Journal:  Galangin Suppresses Renal Inflammation via the Inhibition of NF-κB, PI3K/AKT and NLRP3 in Uric Acid Treated NRK-52E Tubular Epithelial Cells. (Pubmed Central) -  Dec 20, 2019   
    Moreover, western blotting showed that galangin treatment effectively inhibited nuclear factor-kappa B (NF-κB), phosphatidylinositol 3 kinase (PI3K)/protein kinase B (AKT) and nucleotide-binding domain- (NOD-) like receptor protein 3 (NLRP3) signaling pathway activation. Taken together, these findings suggested that galangin plays a pivotal role in renal inflammation by suppressing inflammatory responses, which might be closely associated with the inhibition of NLRP3 inflammasome, NF-κB and PI3K/AKT signaling pathway activation.
  • ||||||||||  sirolimus / Generic mfg.
    Journal:  Conjunctival Melanoma Targeted Therapy: MAPK and PI3K/mTOR Pathways Inhibition. (Pubmed Central) -  Dec 20, 2019   
    To analyze the activity of mitogen-activated protein kinase (MAPK) and phosphoinositide 3-kinases/mechanistic target of rapamycin (PI3K/mTOR) pathways in benign and malignant conjunctival melanocytic proliferations and explore whether specific inhibitors can suppress growth of conjunctival melanoma (CJM) cells...WST-1 assays were performed with a BRAF inhibitor (vemurafenib), two MEK inhibitors (trametinib, selumetinib), a PI3K inhibitor (pictilisib), and a dual PI3K/mTOR inhibitor (dactolisib)...The MAPK pathway activity in CJM is increased, not only as a consequence of the BRAF V600E mutation. Targeted therapy may be useful for patients with CJM, especially those with activating BRAF mutations, whereas NRAS-mutated melanomas are relatively resistant.
  • ||||||||||  Preclinical, Journal:  Carnosine Protects Mouse Podocytes from High Glucose Induced Apoptosis through PI3K/AKT and Nrf2 Pathways. (Pubmed Central) -  Dec 19, 2019   
    Quantitative real-time PCR, Western blotting, and immunofluorescence staining revealed that high glucose induced ROS levels and podocytes apoptosis were downregulated by PI3K/AKT and Nrf2 signaling pathways. The current findings suggest that carnosine may reduce ROS levels and MPC5 cells apoptosis by PI3K/AKT and Nrf2 signaling pathways activation.
  • ||||||||||  Preclinical, Journal:  Gymnemic Acid Ameliorate Hyperglycemia Through PI3K/AKT and AMPK Mediated Signaling Pathway in T2DM Rats. (Pubmed Central) -  Dec 19, 2019   
    In addition, key proteins involved in AMPK-mediated gluconeogenesis (such as phosphoenolpyruvate carboxy kinase (PEPCK) and glucose-6-phosphatase (G6Pase)) were down-regulated in GA-treated T2DM rats. In summary, the hypoglycemic mechanisms of GA may be related to promoting insulin signal transduction and activating PI3K/Akt and AMPK-mediated signaling pathway in T2DM rats.
  • ||||||||||  Aliqopa (copanlisib) / Bayer
    Trial completion date, Trial primary completion date:  Safety, Tolerability, Efficacy and Pharmacokinetics of Copanlisib in Pediatric Patients (clinicaltrials.gov) -  Dec 19, 2019   
    P1/2,  N=130, Recruiting, 
    In summary, the hypoglycemic mechanisms of GA may be related to promoting insulin signal transduction and activating PI3K/Akt and AMPK-mediated signaling pathway in T2DM rats. Trial completion date: May 2023 --> May 2024 | Trial primary completion date: Jan 2023 --> Jan 2024
  • ||||||||||  Rituxan (rituximab) / Biogen, Zenyaku Kogyo, Roche
    Review, Journal, IO biomarker:  Drug therapy for double-hit lymphoma. (Pubmed Central) -  Dec 19, 2019   
    Typically, patients become refractory to standard R-CHOP, and more aggressive regimens such as DA-EPOCH-R, R-hyperCVAD or CODOX-R regimens are typically needed...In this review, we also discuss the role of hematopoietic stem cell transplantation (HCT) and chimeric antigen receptor (CAR) T-cell therapy in DHL. We also discuss the role of potential novel agents such as BCL2 inhibitors, checkpoint inhibitors, bromodomain and extraterminal (BET) family inhibitors, Pi3K inhibitors, and others.
  • ||||||||||  parsaclisib (INCB50465) / Incyte
    Trial completion date, Trial primary completion date:  A Study of INCB050465 in Subjects With Relapsed or Refractory Marginal Zone Lymphoma (CITADEL-204) (clinicaltrials.gov) -  Dec 12, 2019   
    P2,  N=90, Recruiting, 
    This finding suggests VGLL1 as a novel prognostic biomarker and a potential therapeutic target. Trial completion date: Mar 2022 --> Jan 2021 | Trial primary completion date: Mar 2020 --> Jan 2021
  • ||||||||||  Journal:  CSNK2A1 Promotes Gastric Cancer Invasion Through the PI3K-Akt-mTOR Signaling Pathway. (Pubmed Central) -  Dec 12, 2019   
    We further verified that epithelial-mesenchymal transition (EMT) was affected by CSNK2A1 and that CSNK2A1 promotes GC cell invasion through the PI3K-Akt-mTOR signaling pathway. Our findings suggested that CSNK2A1 plays important oncogenic roles in GC invasion via EMT and the PI3K-Akt-mTOR signaling pathway and that CSNK2A1 may serve as a novel prognostic and/or therapeutic target in GC.
  • ||||||||||  Journal, IO Biomarker:  B7-H3 Induces Ovarian Cancer Drugs Resistance Through An PI3K/AKT/BCL-2 Signaling Pathway. (Pubmed Central) -  Dec 12, 2019   
    B7-H3 expression induces the activation the PI3K/AKT signaling pathway and up-regulates BCL-2 in protein level, resulting in the sustained growth and chemo-resistance in ovarian cancer. Blockade of B7-H3 signals efficiently reverses the chemo-resistance, which provides an innovative target in ovarian cancer treatment.