PI3K inhib 
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  • ||||||||||  sapanisertib (CB-228) / Calithera
    Journal:  p53 haploinsufficiency and increased mTOR signaling define a subset of aggressive hepatocellular carcinoma. (Pubmed Central) -  Jan 15, 2022   
    Our data advance the current understanding of the activation of the Pten/PI3K/Akt/mTOR axis and its downstream target Abcc4 in hepatocarcinogenesis driven by p53 reduction and Tsc1 loss. Targeting mTOR, an unexpected vulnerability in p53 (haplo)deficiency HCC, can be exploited therapeutically to treat Abcc-4-positive HCC patients.
  • ||||||||||  PF-04691502 / Pfizer, Vanflyta (quizartinib) / Daiichi Sankyo
    Journal:  Synergistic cytotoxicity of dual PI3K/mTOR and FLT3 inhibition in FLT3-ITD AML cells. (Pubmed Central) -  Jan 14, 2022   
    Here, we report on the preclinical activity of the combination of the FLT3 inhibitor quizartinib with the dual PI3K/mTOR inhibitor PF-04691502 in FLT3-ITD cells. Briefly, we show that the association of these two molecules displays synergistic cytotoxicity in vitro in FLT3-ITD AML cells, triggering 90% cell death at nanomolar concentrations after 48 h.
  • ||||||||||  Preclinical, Journal:  Mechanism of astragaloside Ⅳ alleviating PC12 cell injury by activating PI3K/AKT signaling pathway: based on network pharmacology and in vitro experiments (Pubmed Central) -  Jan 14, 2022   
    In vitro experiments showed that AS-Ⅳ could effectively inhibit the decrease of the viability of PC12 induced by MPP~+ and up-regulate the mRNA expression levels of AKT1 and PI3 K as well as the phosphorylation levels of AKT and PI3 K. As an active component of Astragali Radix, AS-Ⅳ acts on PD through multiple targets and pathways. Furthermore, it inhibits neuronal apoptosis and protects neurons by activating the PI3 K/AKT signaling pathway, thereby providing reliable theoretical and experimental supports for the treatment of PD with AS-Ⅳ.
  • ||||||||||  temozolomide / Generic mfg.
    Journal:  Connexin 43 confers chemoresistance through activating PI3K. (Pubmed Central) -  Jan 14, 2022   
    These two different treatments synergistically inactivate PI3K and sensitize glioblastoma cells to temozolomide in vitro and in vivo. Our study has revealed novel mechanistic insights into Cx43/PI3K-mediated temozolomide resistance in glioblastoma and demonstrated that targeting Cx43 and PIK3CB/p110β together is an effective therapeutic approach for overcoming chemoresistance.
  • ||||||||||  Journal:  Substrate stiffening promotes VEGF-A functions via the PI3K/Akt/mTOR pathway. (Pubmed Central) -  Jan 13, 2022   
    This pathway is activated on stiffer substrates, is amplified by VEGF-A stimulation, and correlates with enhanced endothelial cell (EC) proliferation, contraction, pro-angiogenic secretion, and capillary-like tube formation. In the settings of advanced age-related macular degeneration, characterized by EC and retinal pigment epithelial (RPE)-mediated angiogenesis, these data implicate substrate stiffness as a novel causative mechanism and Akt/mTOR inhibition as a novel therapeutic pathway.
  • ||||||||||  Journal:  TRAM2 promotes the malignant progression of glioma through PI3K/AKT/mTOR pathway. (Pubmed Central) -  Jan 13, 2022   
    740Y-P, a PI3K activator, reversed the effects of TRAM2 silencing on glioma cell proliferation, invasion, migration and EMT process. Taken together, these findings establish that TRAM2/PI3K/AKT/mTOR signaling drives malignancy properties of glioma and indicate that TRAM2 may act as a potential therapeutic target for glioma.
  • ||||||||||  sirolimus / Generic mfg.
    Journal:  PI3-kinase inhibition as a strategy to suppress the leukemic stem cell niche in Ph+ chronic myeloid leukemia. (Pubmed Central) -  Jan 13, 2022   
    Furthermore, we show that BEZ235 and copanlisib cooperate with nilotinib and ponatinib in suppressing proliferation and survival of osteoblasts and endothelial cells...Together, targeting osteoblastic niche cells through PI3K inhibition may be a new effective approach to overcome niche-induced TKI resistance in CML. Whether this approach can be translated into clinical application and can counteract drug resistance of LSC in patients with CML remains to be determined in clinical trials.
  • ||||||||||  LY294002 / Eli Lilly
    Journal, IO biomarker:  DP from Euphorbia fischeriana S. mediated apoptosis in leukemia cells via the PI3k/Akt signaling pathways. (Pubmed Central) -  Jan 12, 2022   
    Whether this approach can be translated into clinical application and can counteract drug resistance of LSC in patients with CML remains to be determined in clinical trials. The in vivo and in vitro experimental results indicated that DP might inhibit the proliferation and induce the apoptosis of leukemia cells, which might be a result of suppressing the PI3k/Akt signaling pathways.
  • ||||||||||  Mekinist (trametinib) / Novartis, Estybon (rigosertib) / Onconova, SymBio Pharma, Knight Therap, Tafinlar (dabrafenib) / Novartis
    Journal, Checkpoint inhibition, PD(L)-1 Biomarker, IO biomarker:  Novel induction of CD40 expression by tumor cells with RAS/RAF/PI3K pathway inhibition augments response to checkpoint blockade. (Pubmed Central) -  Jan 12, 2022   
    P=N/A
    These results indicated that TEC might be an effective compound in the treatment for ischemic brain injury. Our data support the therapeutic use of RGS + αPD1 + αCTLA4 in RAS/RAF/PI3K pathway-activated melanomas and point to the need for clinical trials of RGS + ICB for melanoma patients who do not respond to ICB alone.
  • ||||||||||  LY294002 / Eli Lilly
    Journal, IO biomarker:  The mechanism analysis using PI3K/AKT pathway for the effects of levocarnitine in the treatment of spermatogenic dysfunction. (Pubmed Central) -  Jan 12, 2022   
    LEV and LY294002 (a PI3K pathway inhibitor) were then administered...Besides, the morphology of testicular tissue in the GTW + LEV and LY + LEV groups was superior to that in the GTW group. We can to the conclusion that LEV may operate via the PI3K/AKT signalling pathway, with increases in PI3K, p-AKT, and BCL-2 protein and mRNA expression, so that the percentages of GC-1 spg cells apoptosis decrease, and the sperm count and motility improve.