PI3K inhib 
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  • ||||||||||  Journal:  First PI3K Inhibitor for Breast Cancer. (Pubmed Central) -  Jul 3, 2019   
    Overall, our results demonstrate that miR-146b-3p, directly suppressing PI3K/AKT pathway and MDFIC, acts in the proliferation, differentiation, and apoptosis of myoblast in chicken. No abstract available
  • ||||||||||  Preclinical, Journal:  Signalling Pathways Involved in p47 -dependent Reactive-oxygen species in Platelets of Endotoxemic Rats. (Pubmed Central) -  Jun 30, 2019   
    Moreover, in the LPS group, the sGC inhibitor ODQ, the PKG inhibitor Rp-8-Br and the PKC inhibitor GF109203X abrogated the increased p47 phosphorylation and reduced the ROS levels. In conclusion, selective inhibitors of cGMP-PKG and PKC-p47 pathways that regulate ROS generation by LPS in platelets may help control the redox balance in sepsis improving the survival of patients.
  • ||||||||||  Clinical, Review, Journal:  Safety and Tolerability of Phosphatidylinositol-3-Kinase (PI3K) Inhibitors in Oncology. (Pubmed Central) -  Jun 30, 2019   
    For example, combination of alpelisib with fulvestrant has recently demonstrated unexpectedly superior efficacy compared to fulvestrant alone. Furthermore, the immunomodulatory activity of PI3Kδ and PI3Kγ inhibitors also provides unexpected opportunities for their use in cancer immunotherapy, as is currently being tested in several clinical trials.
  • ||||||||||  Journal, IO Biomarker:  Effects of BENC-511, a novel PI3K inhibitor, on the proliferation and apoptosis of A549 human lung adenocarcinoma cells. (Pubmed Central) -  Jun 30, 2019   
    BENC-511 decreased the expression of cyclin A, proliferating cell nuclear antigen (PCNA), B-cell lymphoma-2 (Bcl-2), phospho-mammalian target of rapamycin (p-mTOR), and phospho-Akt (p-Akt) and it increased the expression of p21WAF1CIP1(p21), Caspase-3 and Caspase-9. In conclusion, BENC-511 inhibited the proliferation of A549 human lung adenocarcinoma cells via S phase arrest as a result of up-regulation of p21 and reduction of Cyclin A/cyclin-dependent kinase 2 (CDK2)/PCNA complex and it induced apoptosis by reducing the mitochondrial membrane potential via the Akt/Bcl-2/Caspase-9 mitochondrial pathway of apoptosis.
  • ||||||||||  buparlisib (BKM120) / Novartis, Adlai Nortye
    Journal:  Benefits versus risk profile of buparlisib for the treatment of breast cancer. (Pubmed Central) -  Jun 30, 2019   
    Expert opinion: Targeting PI3K showed efficacy in BC. Buparlisib, a pan PI3K inhibitor, presents manageable but not negligible toxicity with an activity/toxicity ratio in favor of the use of emerging second generation, α-selective PI3K inhibitors for ongoing and future trials.
  • ||||||||||  Review, Journal:  The role of PI3K/AKT/FOXO signaling in psoriasis. (Pubmed Central) -  Jun 28, 2019   
    Finally, we summarized that PI3K/AKT/FOXO signaling and its upstream and downstream molecule which could be underlying therapeutic target for psoriasis. This article is part of a special issue entitled: PI3K-AKT-FOXO axis in psoriasis.
  • ||||||||||  Preclinical, Journal:  Up-Regulation of Trem2 Inhibits Hippocampal Neuronal Apoptosis and Alleviates Oxidative Stress in Epilepsy via the PI3K/Akt Pathway in Mice. (Pubmed Central) -  Jun 28, 2019   
    Moreover, activation of the PI3K/Akt pathway through over-expression of Trem2 alleviated oxidative stress, as shown by the increased expression of SOD and GSH-Px and the decreased expression of MDA and 8-OHdG. The current study defines the potential role of Trem2 in inhibiting the development of epilepsy, indicating that Trem2 up-regulation alleviates hippocampal neuronal injury and oxidative stress, and inhibits neuronal apoptosis in epilepsy by activating the PI3K/Akt pathway.
  • ||||||||||  Journal:  Tetracycline antibiotics as PI3K inhibitors in the Nrf2-mediated regulation of antioxidative stress in zebrafish larvae. (Pubmed Central) -  Jun 28, 2019   
    Further molecular docking and molecular dynamics simulations revealed that CTC and OTC are capable of docking into the binding pocket of zebrafish PI3K, an important molecule in the activation of Nrf2, and can form stable interactions through hydrogen bonds. The overall results indicated that CTC and OTC significantly induced oxidative stress responses in zebrafish larvae, and both CTC and OTC act as inhibitors of PI3K to inhibit the activation of the Nrf2/ARE signaling pathway, thus reducing the antioxidant capacity of fish.
  • ||||||||||  Preclinical, Journal, IO Biomarker:  HO-1 protects the nerves of rats with cerebral hemorrhage by regulating the PI3K/AKT signaling pathway. (Pubmed Central) -  Jun 27, 2019   
    In addition, the content of Evans blue, MDA, the number of apoptotic cells, the water content of brain tissue and the expression of BAX were significantly increased, while the SOD activity and the expressions of Bcl-2, p-PI3K and p-AKT protein were decreased. HO-1 could protect the nerves of rats with cerebral hemorrhage by regulating the PI3K/AKT signaling pathway.
  • ||||||||||  Journal, IO Biomarker:  Antitumor effects of conditioned media of human fetal dermal mesenchymal stem cells on melanoma cells. (Pubmed Central) -  Jun 27, 2019   
    CM-FDMSC can inhibit the tumor-forming behaviors of A375 melanoma cells and inhibit PI3K/AKT and mitogen-activated protein kinase signaling to shift their BCL-2/BAX ratio toward a proapoptotic state. Identification of the bioactive components in CM-FDMSC will be important for translating these findings into novel therapies for malignant melanoma.
  • ||||||||||  sirolimus / generics
    Journal:  Effects of insulin and pathway inhibitors on the PI3K-Akt-mTOR phosphorylation profile in acute myeloid leukemia cells. (Pubmed Central) -  Jun 27, 2019   
    The phosphatidylinositol 3-kinase (PI3K)-Akt-mechanistic target of rapamycin (mTOR) pathway is constitutively activated in human acute myeloid leukemia (AML) cells and is regarded as a possible therapeutic target...In contrast, mTOR inhibition reduced mTOR pS2448 and S6 pS244 phosphorylation but increased Akt pT308 phosphorylation. In conclusion, the effects of both insulin and PI3K-Akt-mTOR inhibitors differ between AML patient subsets, and differences in insulin responsiveness are associated with differential susceptibility to metabolic targeting.
  • ||||||||||  Clinical, Journal:  A Deregulated PI3K-AKT Signaling Pathway in Patients with Colorectal Cancer. (Pubmed Central) -  Jun 26, 2019   
    In conclusion, the effects of both insulin and PI3K-Akt-mTOR inhibitors differ between AML patient subsets, and differences in insulin responsiveness are associated with differential susceptibility to metabolic targeting. Taken together, the present study identified a deregulated PI3K-AKT signaling pathway in CRC patients, which might serve as therapeutic target(s).
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  miR-188-5p regulates proliferation and invasion via PI3K/Akt/MMP-2/9 signaling in keloids. (Pubmed Central) -  Jun 26, 2019   
    The upregulation of MMP-2 and MMP-9 by miR-188-5p inhibitor could be abolished by LY294002. These findings together demonstrate a tumor-suppressive role of miR-188-5p in KD proliferation and invasion via PI3K/Akt/MMP-2/9 signaling, indicating that miR-188-5p may be a potential prognostic marker and therapeutic target for KDs.
  • ||||||||||  Aliqopa (copanlisib) / Bayer
    Trial completion date, Trial primary completion date:  Safety, Tolerability, Efficacy and Pharmacokinetics of Copanlisib in Pediatric Patients (clinicaltrials.gov) -  Jun 25, 2019   
    P1/2,  N=130, Recruiting, 
    Taken together, Lir inhibits AngII and pressure overload induced cardiac remodeling via regulating PI3K/Akt1 and AMPKα signaling. Trial completion date: Aug 2021 --> Dec 2022 | Trial primary completion date: Aug 2021 --> Apr 2022
  • ||||||||||  Erbitux (cetuximab) / Eli Lilly, EMD Serono, buparlisib (AN2025) / Novartis, Adlai Nortye
    Trial completion, Trial completion date, Trial primary completion date, Monotherapy, Metastases:  PIK-ORL: Activity and Safety Study of BKM120 in Monotherapy in Patient With Metastatic Head and Neck Cancer Recurrent or Progressive (clinicaltrials.gov) -  Jun 24, 2019   
    P2,  N=58, Completed, 
    Trial completion date: Aug 2021 --> Dec 2022 | Trial primary completion date: Aug 2021 --> Apr 2022 Recruiting --> Completed | Trial completion date: Apr 2020 --> Mar 2019 | Trial primary completion date: Apr 2019 --> Sep 2018
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  An essential role of PI3K in the control of West Nile virus infection. (Pubmed Central) -  Jun 24, 2019   
    ...Inhibition of PI3K activity by 3-methyl adenine (3-MA), Wortmannin (WM) and LY294002 (LY) increased viral titers by 3-16 folds in primary mouse macrophages, embryonic fibroblasts and human cell lines...Lastly translocation of interferon regulatory factor 7(IRF7) from the cytosol to the nuclei was effectively blocked in the presence of PI3K inhibitors. Our results clearly define an antiviral role of PI3K by modulating immune responses and demonstrate differential mode of action of three PI3K inhibitors on IFN-I.
  • ||||||||||  Journal:  The PI3K pathway at the crossroads of cancer and the immune system: strategies for next generation immunotherapy combinations. (Pubmed Central) -  Jun 24, 2019   
    In this review, we first summarize two key learnings from the initial studies of inhibitors of this pathway, including the profile of immune-related adverse events such as colitis, transaminitis and pneumonitis and the increased incidence of infections with the majority of agents that target the PI3K-AKT-mTOR pathway. We then discuss recent advances in our understanding of the role of this pathway in the tumour micro-environment, and in the regulation of innate and adaptive immune responses, and propose synergistic combination strategies with PI3K-network inhibitors and cancer immunotherapy.