PI3K inhib 
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  • ||||||||||  Tamoxis (tamoxifen) / Bioprofarma
    Journal, Tumor-Infiltrating Lymphocyte:  Cancer-immune interactions in ER-positive breast cancers: PI3K pathway alterations and tumor-infiltrating lymphocytes. (Pubmed Central) -  Jan 27, 2020   
    Thus, we concluded that PI3K may, at least in part, act upstream of PPARα to regulate Plin5 expression and lipid droplets formation in HepG2 cells. These exploratory analyses of a prospective trial in luminal breast cancer suggest high CD8 infiltration is associated with unfavorable outcome and that PI3K pathway alterations might be associated with the composition of the tumor microenvironment.
  • ||||||||||  Journal:  (Sterol)ized Immunity: Could PI3K/AKT3 Be the Answer? (Pubmed Central) -  Jan 26, 2020   
    In this issue of Immunity, Xiao et al. (2020) reveal that type I IFN signaling and 7-dehydrocholesterol (7-DHC) accumulation form a positive feedback loop to amplify innate immune responses to control viral infections by activating AKT3.
  • ||||||||||  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.
  • ||||||||||  Characterizing roles of the PTEN-PI3K axis in breast tumorigenesis (Trade Area Level 2&3) -  Jan 24, 2020 - Abstract #LCC2020LCC_161;    
    Proteomic and transcriptomic analyses identified key molecular signatures activated upon loss of PTEN protein-phosphatase function able to restrain tumor cell survival. Altogether, our studies provide new insights into mechanisms of PTEN-dependent tumour suppression and have important therapeutic implications for a range of clinical conditions.
  • ||||||||||  Cep55 overexpression causes tumorigenesis in mice though multiple mechanisms (Trade Area Level 2&3) -  Jan 24, 2020 - Abstract #LCC2020LCC_102;    
    Importantly, this phenotype was rescued by pharmacological inhibition of Pi3k/Akt or expression of mutant Chk1 (S280A), that is insensitive to regulation by active AKT, in Cep55 overexpressing cell. Collectively, our data demonstrates causative effects of deregulated Cep55 on genome stability and tumorigenesis which have potential implications for therapy.
  • ||||||||||  Piqray (alpelisib) / Novartis
    Overcoming resistance to PI3K inhibitors in colorectal cancer (Trade Area Level 2&3) -  Jan 24, 2020 - Abstract #LCC2020LCC_65;    
    Interestingly, the gene knock out results so far show a change in drug sensitivity in several cellular pathways and processes including: the mTOR pathway (PTEN, TSC2, NPRL2 and DEPDC5), the glycolysis pathway (PGP and ENO1), the pentose phosphate pathway (PGD), mitochondrial function (PET117, NDUFA1, NDUFA9, NDUFS1, COA6 and COX17), protein translation (DPH1, DNAJC24, EIF4A1, DPH6 and DPH5), and the cytoskeleton and cell migration (MYH9, LIMK2 and ROCK2).Finally, other top candidate hits present ambiguous connections such as RALGAPB, KCTD5 and LCMT1. Upon functional validation, the most promising targets will be used to test combinational therapy together with Alpelisib to find new treatments to overcome resistance to PI3K inhibitors in CRC.
  • ||||||||||  Journal:  Ethanol Extracts of Dietary Herb, Alpinia nantoensis, Exhibit Anticancer Potential in Human Breast Cancer Cells. (Pubmed Central) -  Jan 24, 2020   
    These results indicate that extracts of A nantoensis could inhibit signal transduction at least involved in EGFR as well as the PI3K/AKT and Ras-ERK pathways, which are crucial players of tumor cell migration and invasion. Our study strongly supports that the extracts of A nantoensis could be a novel botanical drug lead for the development of an antimetastatic agent for the treatment of human malignant breast cancer.
  • ||||||||||  GDC-0084 / Kazia
    Clinical, Journal:  An LC/ESI-MS/MS method to quantify the PI3K inhibitor GDC-0084 in human plasma and cerebrospinal fluid: validation and clinical application. (Pubmed Central) -  Jan 24, 2020   
    The lower limit of quantitation and limit of detection for GDC-0084 in human plasma were 0.2 ng/mL (signal/noise ≥ 47) and 0.005 ng/mL (signal/noise ≥ 3.5), respectively, and for GDC-0084 in human CSF were 0.2 ng/mL (signal/noise ≥ 19.7) and 0.04 ng/mL (signal/noise ≥ 7.2). This method was successfully applied to analyze serial plasma samples obtained from children with diffuse intrinsic pontine gliomas and other midline gliomas who participated in pharmacokinetic studies as part of a phase I clinical trial of GDC-0084.
  • ||||||||||  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.
  • ||||||||||  Journal:  Osteogenesis activity of isocoumarin a through the activation of the PI3K-Akt/Erk cascade-activated BMP/RUNX2 signaling pathway. (Pubmed Central) -  Jan 23, 2020   
    Subsequently, the in vivo investigation on the zebrafish embryos model demonstrated that isocoumarin A (0.30 mM) increased the number of vertebrae (5.38 ± 2.07 pcs) and the vertebral area (433.25 ± 111.77 μm) in the development process of zebrafish embryos after a 7-day postfertilization (dpf) culture compared with the control group (2.50 ± 1.16 pcs and 209.75 ± 86.40 μm). Together, these results indicated that isocoumarin A could be viewed as a promising candidate in early drug discovery and development to promote the healing of fractures and postmenopausal osteoporosis.
  • ||||||||||  Journal:  Muscarinic m2 receptor-mediated actin polymerization via PI3 kinase γ and integrin-linked kinase in gastric smooth muscle. (Pubmed Central) -  Jan 21, 2020   
    Osteoblast-derived ECM could be further investigated as titanium scaffold-coating to improve BTE. In gastric smooth muscle cells, activation of PI3Kγ by muscarinic m2 receptors causes ILK-dependent phosphorylation of paxillin, an association of paxillin with Cdc42 GEF proteins and activation of Cdc42, which, in turn, causes phosphorylation of N-WASp and its association with Arp2/3 complex leading to actin polymerization.
  • ||||||||||  cisplatin / Generic mfg.
    Preclinical, Journal:  SPP1 inhibition improves the cisplatin chemo-sensitivity of cervical cancer cell lines. (Pubmed Central) -  Jan 21, 2020   
    In gastric smooth muscle cells, activation of PI3Kγ by muscarinic m2 receptors causes ILK-dependent phosphorylation of paxillin, an association of paxillin with Cdc42 GEF proteins and activation of Cdc42, which, in turn, causes phosphorylation of N-WASp and its association with Arp2/3 complex leading to actin polymerization. SPP1 inhibition could suppress proliferation, induce apoptosis and increase the DDP chemo-sensitivity of HeLa cells.
  • ||||||||||  Review, Journal:  PI3k/AKT signaling pathway: Erythropoiesis and beyond. (Pubmed Central) -  Jan 19, 2020   
    In this review, we focus on the role of PI3K/AKT pathway in erythropoiesis and discuss the function of some of the most important genes, transcription factors, and miRNAs that regulate different stages of erythropoiesis which play roles in differentiation and maturation of RBCs, prevention of apoptosis, and autophagy induction. Understanding the role of the PI3K pathway in erythropoiesis may provide new insights into diagnosing erythrocyte disorders.
  • ||||||||||  Journal:  Interaction between IGF2-PI3K axis and Cancer-Associated-Fibroblasts promotes anal squamous carcinogenesis. (Pubmed Central) -  Jan 19, 2020   
    We also demonstrated that IGF2 expression is mainly due to cancer-associated fibroblasts and that IGF2 secreted by cancer-associated fibroblasts from ASCC samples promotes proliferation of a human ASCC cell line via IGF2 paracrine signalling. Altogether, these results highlight the key role of the IGF2/PI3K axis, and the major role of cancer-associated fibroblasts in tumour growth via IGF2 secretion, suggesting a major role of IGF2/IGF1R inhibitors in ASCC therapies.
  • ||||||||||  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.