PI3K inhib 
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  • ||||||||||  quercetin (LY294002) / Eli Lilly, PD98059 / Wayne State University
    Preclinical, Journal:  Polyamine analogue QMA attenuated ischemic injury in MCAO rats via ERK and Akt activated Nrf2/HO-1 signaling pathway. (Pubmed Central) -  May 2, 2019   
    Further more, treatment with LY294002 (specific PI3K inhibitor), PD98059 (specific ERK inhibitor), brusatol (specific Nrf2 inhibitor) and SnPP (specific HO-1 inhibitor) deprived almost all the effects of QMA in MCAO rats and OGD-treated PC12 cells. These data suggested that the protective actions of QMA on the cerebral ischemia may be related to activation of endogenous cytoprotective mechanism via ERK and Akt activated Nrf2/HO-1 signaling pathway.
  • ||||||||||  Zydelig (idelalisib) / Gilead
    Review, Journal:  Targeting PI3K Signaling in Acute Lymphoblastic Leukemia. (Pubmed Central) -  May 2, 2019   
    ...A novel FDA-approved PI3Kδ inhibitor, CAL-101/idelalisib, leads to downregulation of p-AKT and increased apoptosis of CLL cells...Here, we review the role of PI3K in normal hematopoietic cells, and in ALL. We focus on summarizing targeting strategies of PI3K in ALL.
  • ||||||||||  Journal:  Enhanced β-adrenergic signalling underlies an age-dependent beneficial metabolic effect of PI3K p110α inactivation in adipose tissue. (Pubmed Central) -  May 2, 2019   
    This effect of p110α inactivation is due to a potentiating effect on β-adrenergic signalling, which leads to increased catecholamine-induced energy expenditure in the adipose tissue. Our findings provide a paradigm of how partial inactivation of an essential component of the insulin signalling pathway can have an overall beneficial metabolic effect and suggest that PI3K inhibition could potentiate the effect of β-adrenergic agonists in the treatment of obesity and its associated comorbidities.
  • ||||||||||  alpelisib (BYL719) / Novartis
    Journal:  The PI3Kα Inhibitor Alpelisib Has Activity in-altered Tumors. (Pubmed Central) -  May 1, 2019   
    These results suggest intelectin-1 promotes angiogenesis, inhibits oxidative stress and reduces apoptosis by stimulating the Akt-eNOS signaling pathway in response to ischemia in vitro. The PI3Kα inhibitor alpelisib achieved a 58.2% disease control rate in-altered solid tumors.
  • ||||||||||  umbralisib (TGR-1202) / TG Therapeutics
    Journal:  Umbralisib Inhibits PI3Kδ with Less Toxicity Than Previous Inhibitors. (Pubmed Central) -  May 1, 2019   
    The PI3Kα inhibitor alpelisib achieved a 58.2% disease control rate in-altered solid tumors. Umbralisib is well tolerated and has activity against relapsed or refractory hematologic cancers.
  • ||||||||||  Preclinical, Journal:  Cross-talk between insulin signalling and LPS responses in mouse macrophages. (Pubmed Central) -  Apr 30, 2019   
    Conversely, priming with PI3K inhibitor wortmannin prevents insulin attenuation of HG- and/or LPS-induced p38 MAPK and NF-κB activation, Tnf-α, Il-1β expression as well as NO production. Congruent with reduced Il-10 expression, MEK inhibition abrogates insulin action allowing significant increase in Tlr4 expression and LPS response indicating insulin-induced Il-10 might have pivotal influence in regulation of chronic as well as acute inflammatory response.
  • ||||||||||  Journal:  SCD1 is required for EGFR-targeting cancer therapy of lung cancer via re-activation of EGFR/PI3K/AKT signals. (Pubmed Central) -  Apr 27, 2019   
    ...This study aimed to investigate the role of SCD1 inhibition by EGFR inhibitor (Gefitinib)-based anti-tumor therapy of lung cancer both in vitro and in vivo...Furthermore, in spite of EGFR inhibition, overexpression of SCD1 in vivo significantly promoted tumor growth by activating EGFR/PI3K/AKT signaling in tumor tissues, but A939572 treatment restricted SCD1-induced tumor progression and inhibited EMT phenotype of cancer cells in vivo. These findings indicated that inhibition of oncogene SCD1 is required for targeting EGFR therapy in lung cancer.
  • ||||||||||  Reasanz (serelaxin) / Novartis
    Journal:  Relaxin induces up-regulation of ADAM10 metalloprotease in RXFP1-expressing cells by PI3K/AKT signaling. (Pubmed Central) -  Apr 26, 2019   
    ...H9c2 cardiomyocytes and NIH3T3 fibroblasts were incubated with human RLX-2 (17 nmol/l, 24 h) in presence or absence of the PI3K or Akt inhibitors wortmannin (WT, 100 nmol/l) and triciribine (TCN, 1 μmol/l)...RLX significantly increased Akt phosphorylation, ADAM10 and NICD expression, which were abolished by WT or TCN and did not occur with iRLX. These findings highlight a new receptor-specific signal transduction pathway of RLX.
  • ||||||||||  Journal:  CD47 promotes human glioblastoma invasion through activation of PI3K/Akt pathway. (Pubmed Central) -  Apr 26, 2019   
    AKT suppression with specific inhibitor impaired invasion of cells in which excessively expressed CD47, indicating that stimulation of PI3K/Akt pathway served as the downstream regulator of invasion triggered by CD47. These results suggest that CD47 might serve as a predictor of worse development as well as metastasis and brought about an innovative approach to treat glioblastoma.
  • ||||||||||  Journal:  EYA1 promotes tumor angiogenesis by activating the PI3K pathway in colorectal cancer. (Pubmed Central) -  Apr 26, 2019   
    Overexpression of Eya1 increased tumor angiogenesis in vivo and in vitro. Our study suggested that Eya1 is essential in regulating cancer cell-mediated angiogenesis and contributes to tumor growth, and that Eya1 provides a potential and specific target for new anti-angiogenesis drug development.
  • ||||||||||  Preclinical, Journal:  MFG-E8 induced differences in proteomic profiles in mouse CC cells and its effect on PI3K/Akt and ERK signal pathways. (Pubmed Central) -  Apr 26, 2019   
    Based on the analysis of KEGG and STRING database, further to verification the expression of PI3K and ERK phosphorylation levels by Western blot. This study found that the data of proteomic was complementary to recent MFG-E8 studies of protein expression patterns in developing myotubes and provided a holistic framework for understanding how diverse biochemical processes are coordinated at the cellular level during skeletal muscle development.
  • ||||||||||  Review, Journal:  The relation between PI3K/AKT signalling pathway and cancer. (Pubmed Central) -  Apr 26, 2019   
    Receptor tyrosine kinases upstream of PI3K, the p110a catalytic fractional unit of PI3K, the downstream kinase, AKT, and therefore the negative regulator, PTEN, are all often altered in cancer. In this review, we consider about the phosphoinositide 3-kinases family and mechanisms of PI3K-Akt stimulation in cancer.
  • ||||||||||  buparlisib (BKM120) / Novartis, Adlai Nortye
    Journal:  Oncolytic Herpes Simplex Virus and PI3K Inhibitor BKM120 Synergize to Promote Killing of Prostate Cancer Stem-like Cells. (Pubmed Central) -  Apr 25, 2019   
    In athymic mice bearing DU145 PCSC-derived tumors, the combination of intra-tumoral G47Δ and systemic BKM120 induced complete regression of tumors in 2 of 7 animals, and it exhibited superior anti-tumor activity compared to either monotherapy alone, with no detectable toxicity. oHSV synergizes with BKM120 in killing PCSCs in vitro, and the combination markedly inhibits tumor growth, even inducing regression in vivo.
  • ||||||||||  buparlisib (AN2025) / Adlai Nortye
    Trial completion date, Trial primary completion date, Metastases:  Buparlisib in Metastatic Transitional Cell Carcinoma of the Urothelium (clinicaltrials.gov) -  Apr 25, 2019   
    P2,  N=35, Active, not recruiting, 
    oHSV synergizes with BKM120 in killing PCSCs in vitro, and the combination markedly inhibits tumor growth, even inducing regression in vivo. Trial completion date: Mar 2019 --> Mar 2020 | Trial primary completion date: Mar 2019 --> Mar 2020
  • ||||||||||  Journal:  Oncogenic activation of PI3K induces progenitor cell differentiation to suppress epidermal growth. (Pubmed Central) -  Apr 24, 2019   
    An AKT substrate, SH3RF1, is identified as a specific promoter of epidermal differentiation that has no effect on proliferation. Our study provides evidence for a direct, cell autonomous mechanism that can suppresses progenitor cell renewal and block clonal expansion of epidermal cells bearing a common and activating mutation in Pik3ca.
  • ||||||||||  dexamethasone / generics
    Journal, IO Biomarker:  Dexamethasone induces osteoblast apoptosis through ROS-PI3K/AKT/GSK3β signaling pathway. (Pubmed Central) -  Apr 23, 2019   
    Our study provides evidence for a direct, cell autonomous mechanism that can suppresses progenitor cell renewal and block clonal expansion of epidermal cells bearing a common and activating mutation in Pik3ca. Our research verified that Dex induced osteoblasts apoptosis by ROS-PI3K/AKT/GSK3β signaling pathway.
  • ||||||||||  Review, Journal:  A patent update on PDK1 inhibitors (2015-present). (Pubmed Central) -  Apr 23, 2019   
    The majority of the new molecules synthetized interact with binding sites different from the ATP binding site (i.e. PIF pocket or DFG-out conformation). However, many researchers are still looking for innovative PDK1 modulation strategy such as combination of well-known inhibitory agents or multitarget ligands, aiming to block, together with PDK1, other different critical players in the wide panorama of proteins involved in tumor pathways.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal, IO Biomarker:  HS attenuates sepsis-induced cardiac dysfunction via a PI3K/Akt-dependent mechanism. (Pubmed Central) -  Apr 23, 2019   
    Furthermore, the PI3K inhibitor LY294002 eliminated the protective effects of HS. In conclusion, the results of the current study suggest that exogenous HS activates PI3K/Akt signaling to attenuate myocardial damage in sepsis.