PI3K inhib 
Welcome,         Profile    Billing    Logout  
 67 Companies  59 Products   59 Products   344 Diseases   343 Trials   12261 News 


«12...177178179180181182183184185186187...229230»
  • ||||||||||  Journal:  Pharmacological actions of neferine in the modulation of human platelet function. (Pubmed Central) -  Mar 8, 2020   
    Western blot analysis showed that neferine inhibited PI3K activation, and decreased the levels of phosphorylation of Akt, GSK3β and p38 MAPK in platelets. In summary, neferine has the potential to be an antiplatelet and antithrombotic agent by inhibiting the PI3K-Akt-GSK3β/p38 MAPK signaling pathway.
  • ||||||||||  Review, Journal:  Mechanisms of resistance to estrogen receptor modulators in ER+/HER2- advanced breast cancer. (Pubmed Central) -  Mar 8, 2020   
    Additionally, genomic evolution is complex in tumors exposed to hormonal therapy. We highlight the genomic alterations present in ESR1 and PIK3CA genes to elucidate adaptive mechanisms of endocrine resistance, and discuss how these mutations may inform novel combinations to improve clinical outcomes in the future.
  • ||||||||||  [VIRTUAL] Developing Rational Combinations of Targeted Drugs (Ballroom 20 A-C - Upper Lvl - SDCC) -  Mar 6, 2020 - Abstract #AACR2020AACR_1514;    
    Wong will talk about the synergistic interaction of checkpoint blockade and Cdk7 inhibitors. P. Workman will discuss synergistic interaction between Bcl2 inhibitor with Pi3K/Mek combinations, augmenting Cdk4/6 inhibition by coinhibition of FAK and Mek, and the advantage to developing high-quality chemical probes to interrogate the pharmacologic consequences of targeting new targets such as Cdk8 and Cdk19.
  • ||||||||||  [VIRTUAL] PI 3-Kinase and Cancer Metabolism (Room 6 A - Upper Lvl - SDCC) -  Mar 6, 2020 - Abstract #AACR2020AACR_777;    
    This same enzyme mediates insulin responses in liver, muscle, fat and other tissues and drugs that inhibit this enzyme have the expected effect of raising serum glucose and insulin levels. Data will be presented showing that dietary and pharmaceutical interventions that limit elevation of serum insulin improve responses to PI3K inhibitors in mouse models of cancer by preventing insulin-dependent activation of PI3K in tumors.
  • ||||||||||  etoposide IV / Generic mfg.
    Journal:  Antitumor activity of a novel dual functional podophyllotoxin derivative involved PI3K/AKT/mTOR pathway. (Pubmed Central) -  Mar 5, 2020   
    In a xenograft animal local expansion model, PtoxPdp was superior to etoposide in tumor repression...Furthermore, PtoxPdp could also inhibit epithelial-mesenchymal transition, which was achieved by downregulating both PI3K/AKT/mTOR and NF-κB/Snail pathways. Taken together, our results reveal that PtoxPdp is a promising antitumor drug candidate.
  • ||||||||||  Journal:  Knockdown of TRIM47 inhibits breast cancer tumorigenesis and progression through the inactivation of PI3K/Akt pathway. (Pubmed Central) -  Mar 5, 2020   
    Furthermore, TRIM47 knockdown markedly inhibited the activation of PI3K/Akt signaling pathway, while the effects of TRIM47 knockdown were reversed by the treatment of insulin-like growth factor-1 (IGF-1), which is an activator of PI3K/Akt. Taken together, the findings indicated that knockdown of TRIM47 suppressed tumorigenesis and progression of breast cancer through the inhibition of PI3K/Akt pathway, and suggested that TRIM47 might be a potential therapy target for breast cancer treatment.
  • ||||||||||  Journal:  MRPS16 facilitates tumor progression via the PI3K/AKT/Snail signaling axis. (Pubmed Central) -  Mar 5, 2020   
    Furthermore, we observed that the decrease in tumor cell growth, migration, invasion and Snail expression mediated by MRPS16 knockdown could be rescued by Snail over-expression. In short, our data demonstrate that MRPS16 over-expression remarkably promotes tumor cell growth, migration and invasion via the PI3K/AKT/Snail axis, which may be a promising prognostic marker for glioma.
  • ||||||||||  Review, Journal:  PI3K isoforms in cell signalling and vesicle trafficking. (Pubmed Central) -  Mar 4, 2020   
    Here, we summarize current knowledge of the different PI3K classes and isoforms, focusing on recently uncovered biological functions and the mechanisms by which these kinases are activated. Deeper insight into the PI3K isoforms will undoubtedly continue to contribute to a better understanding of fundamental cell biological processes and, ultimately, of human disease.
  • ||||||||||  Biomarker, Journal:  lncRNA H19 binds VGF and promotes pNEN progression via PI3K/AKT/CREB signaling. (Pubmed Central) -  Mar 4, 2020   
    These findings indicate that H19 is a promising prognostic factor in pNENs with malignant behaviors and functions as an oncogene via the VGF-mediated PI3K/AKT/CREB pathway. In addition, our study implies that VGF may also serve as a candidate prognostic biomarker and therapeutic target in pNENs.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, dalfampridine / Generic mfg.
    Preclinical, Journal:  Blockade of voltage-gated potassium channels ameliorates diabetes-associated cognitive dysfunction in vivo and in vitro. (Pubmed Central) -  Mar 4, 2020   
    Additionally, the PI3K inhibitor LY294002 partially abolished the effects of TEA and 4-AP. These findings indicate that the blockade of Kv channels by TEA and 4-AP ameliorates the diabetes-associated cognitive dysfunction via PI3K/Akt pathway, suggesting that targeting Kv channels could be a promising strategy for the treatments of cognitive impairments in diabetes.
  • ||||||||||  Journal:  Effects of PI3K Inhibition on Afucosylated Antibody-Driven FcγRIIIa Events and Phospho-S6 Activity in NK Cells. (Pubmed Central) -  Mar 3, 2020   
    In this study, a kinetic delay in PI3K-driven phosphorylation of S6 was observed to control transcription of the temporally regulated production of IFN-γ and TNF-α but not MIP-1α, MIP-1β, and RANTES. Together, these studies demonstrate the importance of the PI3K pathway for S6 phosphorylation in human NK cells and the need to combine PI3K inhibitors with therapeutic molecules that enhance immunomodulatory function for anticancer therapies.
  • ||||||||||  Zyclara (imiquimod) / Mochida, Mylan, Bausch Health, Vesimune (imiquimod) / UroGen
    Preclinical, Journal:  PSORI-CM02 ameliorates psoriasis in vivo and in vitro by inducing autophagy via inhibition of the PI3K/Akt/mTOR pathway. (Pubmed Central) -  Mar 3, 2020   
    Together, these studies demonstrate the importance of the PI3K pathway for S6 phosphorylation in human NK cells and the need to combine PI3K inhibitors with therapeutic molecules that enhance immunomodulatory function for anticancer therapies. These results suggest that PSORI-CM02 treats psoriasis by inducing autophagy via inhibition of the PI3K/Akt/mTOR pathway.
  • ||||||||||  tivantinib (ARQ 197) / Daiichi Sankyo, Kyowa Hakko Kirin, Merck (MSD)
    Journal:  Tivantinib Hampers the Proliferation of Glioblastoma Cells via PI3K/Akt/Mammalian Target of Rapamycin (mTOR) Signaling. (Pubmed Central) -  Mar 3, 2020   
    Tivantinib (1 μmol/L) in combination with PI3K inhibitor LY294002 (0.5 μmol/L) and mTOR inhibitor rapamycin (0.1 nmol/L) largely inhibited the proliferation of glioblastoma cells. CONCLUSIONS c-MET inhibitor tivantinib blocks PIKE/Akt/mTOR signaling and hampers the proliferation of glioblastoma cells, which endows the drug a therapeutic effect.
  • ||||||||||  dizocilpine (MK801) / Merck (MSD)
    Preclinical, Journal:  Modulation of Hippocampal Gamma Oscillations by Dopamine in Heterozygous Reeler Mice in vitro. (Pubmed Central) -  Mar 3, 2020   
    Third, inhibition of phosphatidylinositol 3-kinase (PI3K), a downstream molecule of NMDAR, increased γ power and blocked the effects of DA on γ oscillation in WTM and had no significant effect on γ power but largely restored DA modulation of γ oscillations in HRM. Our results reveal that impaired DA function in HRM is associated with dysregulated NMDAR-PI3K signaling, a mechanism that may be relevant in the pathology of schizophrenia.
  • ||||||||||  Journal:  Phosphoinositide 3-Kinase Promotes Oxidative Burst, Stomatal Closure and Plant Immunity in Bacterial Invasion. (Pubmed Central) -  Mar 3, 2020   
    The production of hydrogen peroxide and the expression of gene encoding antioxidant enzyme were both enhanced in AtVPS34 overexpressing lines after spray inoculation or syringe infiltration with Pst DC3000 (avrRpt2). Collectively, these results unraveled a novel and broad role of PI3K in plant immunity which promoted stomatal closure and PR gene expression possibly via regulating ROS production.
  • ||||||||||  chlorpromazine / Generic mfg.
    Journal:  PELP1 Suppression Inhibits Gastric Cancer Through Downregulation of c-Src-PI3K-ERK Pathway. (Pubmed Central) -  Mar 3, 2020   
    It was also implied that chlorpromazine (CPZ) can inhibit the malignant traits of GC and downregulate the expression of PELP1. In a word, PELP1 is an oncogene in gastric cancer and c-Src-PI3K-ERK pathway activation may be responsible for its tumorigenesis, PELP1 may be a potential therapeutic target of chlorpromazine in GC.
  • ||||||||||  ARS-1620 / Kura Oncology, J&J
    Journal, Combination therapy:  KRAS G12C NSCLC models are sensitive to direct targeting of KRAS in combination with PI3K inhibition. (Pubmed Central) -  Mar 2, 2020   
    In a word, PELP1 is an oncogene in gastric cancer and c-Src-PI3K-ERK pathway activation may be responsible for its tumorigenesis, PELP1 may be a potential therapeutic target of chlorpromazine in GC. Our findings suggest that signaling adaptation can in some instances limit the efficacy of ARS1620 but combination with PI3K inhibitors can overcome this resistance.
  • ||||||||||  metformin / Generic mfg., quercetin (LY294002) / Eli Lilly
    Journal:  Evaluation of Angiogenesis Process After Metformin and LY294002 Treatment in Mammary Tumor. (Pubmed Central) -  Mar 2, 2020   
    Our findings suggest that signaling adaptation can in some instances limit the efficacy of ARS1620 but combination with PI3K inhibitors can overcome this resistance. Our results demonstrate the effectiveness of metformin and LY294002 in controlling the angiogenesis process in mammary tumors by VEGF and HIF-1, the most important angiogenic markers.
  • ||||||||||  Review, Journal:  The cell biology behind the oncogenic PIP3 lipids. (Pubmed Central) -  Mar 2, 2020   
    The different mechanisms of phosphoinositide 3-kinase (PI3K) activation in cancer as well as the events that result in PI3K pathway reactivation after patient treatment with PI3K inhibitors was discussed on October 15-17th, 2018, in the medieval town of Baeza (Universidad Internacional de Andalucía, Spain) at the workshop entitled 'The cell biology behind the oncogenic PIP3 lipids'. These topics and the data presented regarding cellular functions altered by PI3K deregulation, the cooperation of PI3K/PTEN mutations with other tumor drivers, and the lessons learned for PI3K-targeted therapy, are discussed below.
  • ||||||||||  Biomarker, Journal:  Knockdown of LINC02465 suppresses gastric cancer cell growth and metastasis via PI3K/AKT pathway. (Pubmed Central) -  Mar 2, 2020   
    Mechanistically, LINC02465 inhibition inactivates PI3K/AKT signaling pathway and the activation of this pathway by 740Y-P reverses the inhibition effect of LINC02465 suppression on biological behaviors of GC cells. Taken together, LINC02465 is an oncogenic lncRNA which facilitates the tumorigenesis and progression of GC via PI3K/AKT pathway, demonstrating a novel effective therapeutic target and prognostic biomarker for GC patients.
  • ||||||||||  sirolimus / Generic mfg.
    Journal:  Aberrant IGF1-PI3K/AKT/MTOR signaling pathway regulates the local immunity of oral lichen planus. (Pubmed Central) -  Mar 2, 2020   
    Taken together, LINC02465 is an oncogenic lncRNA which facilitates the tumorigenesis and progression of GC via PI3K/AKT pathway, demonstrating a novel effective therapeutic target and prognostic biomarker for GC patients. The aberrant IGF1-PI3K/AKT/MTOR signaling may participate in the immunoregulatory mechanism of OLP, via regulation on the crosstalk between T cells and keratinocytes, as well as imbalanced cytokine networks.
  • ||||||||||  Jakafi oral (ruxolitinib) / Novartis, Incyte, Xeljanz (tofacitinib) / Pfizer
    Biomarker, Journal, PD(L)-1 Biomarker, IO Biomarker:  Interferon-γ upregulates Δ42PD1 expression on human monocytes via the PI3K/AKT pathway. (Pubmed Central) -  Mar 2, 2020   
    We demonstrated that IFN-γ increases Δ42PD1 expression on human monocytes via activating the PI3K/AKT signaling pathway downstream of JAKs, and that the PD-1 Δ/F ratio is a potential biomarker to predict the functional state of monocytes. Notably, we revealed the Δ42PD1 play a role in T-cell regulation, providing a novel potential approach to manipulate adaptive immune response.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Preclinical, Journal:  The protective effects of Ghrelin/GHSR on hippocampal neurogenesis in CUMS mice. (Pubmed Central) -  Mar 2, 2020   
    Furthermore, the in vivo data displayed that LY294002 (50 nmol, i.c.v.) can significantly block the antidepressant-like action of exogenous ghrelin treatment. All these results suggest that ghrelin/GHSR signaling maintains the integrity of hippocampus and has an inherent neuroprotective effect whether facing stress or not.