PI3K inhib 
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  • ||||||||||  Review, Journal:  Reaserch Advances on the Role of PI3K/AKT Signaling Pathway and MiRNA in Acute T-Cell Lymphocytic Leukemia--Review (Pubmed Central) -  Aug 29, 2019   
    Apart from the inhibitors and traditional Chinese medicines that target the PI3K/AKT signaling pathway, regulation of the expression of the corresponding miRNA may also be a potential treatment protocol for T-ALL. The mechanisms of PI3K/AKT signaling pathway involved in the development of T-ALL, the role of miRNAs in the PI3K/AKT signaling pathway and the targeted therapy based on this signaling pathway are summarized briefly in this review.
  • ||||||||||  IPI-549 / Infinity Pharma
    Journal, PD(L)-1 Biomarker, IO Biomarker:  Multifunctional Nanoregulator Reshapes Immune Microenvironment and Enhances Immune Memory for Tumor Immunotherapy. (Pubmed Central) -  Aug 29, 2019   
    ...Here, a multifunctional nanoregulator incorporating MnO particles and small molecular IPI549 is developed, which can reshape the tumor immune microenvironment (TIME) to unleash the immune system...Furthermore, the local generation of Mn in TME allows tumor-specific magnetic resonance imaging (MRI). More excitingly, the nanoregulator-reshaped TIME is effectively reserved due to the synergistic effect of hypoxia alleviation and MDSC PI3Kγ inhibition, leading to remarkable post-medication inhibition of tumor re-growth and metastasis in an animal study.
  • ||||||||||  Somavert (pegvisomant) / Pfizer, quercetin (LY294002) / Eli Lilly
    Preclinical, Journal:  IGF1 suppresses cholesterol accumulation in the liver of growth hormone deficient mice via the activation of ABCA1. (Pubmed Central) -  Aug 28, 2019   
    ...The activity of a reporter construct containing the ABCA1 promoter was induced by IGF1, and this effect was blocked by LY294002, a specific inhibitor of phosphatidylinositol 3-kinase (PI3K)...For in vivo experiments, we used an inhibitor for the GH receptor (Pegvisomant) to reduce the IGF1 level...IGF1-treatment stimulated ABCA1 expression to improve cholesterol accumulation in these mice. These results show that the PI3K/Akt/FoxO1 pathway contributes to the regulation of ABCA1 expression in response to IGF1-stimulation that suppressed FL in GH-deficient mice.
  • ||||||||||  Journal:  Research progress on the PI3K/AKT signaling pathway in gynecological cancer (Review). (Pubmed Central) -  Aug 28, 2019   
    This is a common phenomenon; overactivation of the pathway is present in human malignancies and has been implicated in cancer progression, hence one of the important approaches to the treatment of tumors is rational drug design using molecular targets in the PI3K/AKT signaling pathway. In brief, the present review analyzed the effects of the PI3K/AKT signaling pathway on certain gynecological cancer types.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  FABP5 regulates the proliferation of clear cell renal cell carcinoma cells via the PI3K/AKT signaling pathway. (Pubmed Central) -  Aug 28, 2019   
    ...In addition, treatment with the phosphatidylinositol‑4,5‑bisphosphate 3‑kinase (PI3K)/AKT inhibitor, LY294002, attenuated the pro‑proliferative effects of exogenous FABP5 expression in Caki‑1 and 786O cells...Furthermore, FABP5 was observed to regulate tumor growth in nude mice in vivo. In conclusion, the results of the present study suggest that FABP5 may exert a pro‑proliferative role in ccRCC and may be associated with malignant progression and tumorigenesis.
  • ||||||||||  Mekinist (trametinib) / Novartis, uprosertib (UPB795) / Laekna Therap, Avastin (bevacizumab) / Roche
    P2 data, Journal, PD(L)-1 Biomarker, IO biomarker:  Results from a single arm, single stage phase II trial of trametinib and GSK2141795 in persistent or recurrent cervical cancer. (Pubmed Central) -  Aug 27, 2019   
    The combination of trametinib and GSK2141795 was feasible but required dose holds and modifications for adverse events; however, anti-cancer activity was minimal, even in patients with PI3K or RAS pathway alterations. Although the study was terminated early after GSK2141795 development was halted, the findings in these 14 patients do not support further development of this combination in cervical cancer.
  • ||||||||||  Journal:  Calcium Dobesilate Restores Autophagy by Inhibiting the VEGF/PI3K/AKT/mTOR Signaling Pathway. (Pubmed Central) -  Aug 27, 2019   
    Moreover, CaD reduced the activation of the autophagy-related PI3K/AKT/mTOR pathway possibly via decreasing VEGF and downregulating VEGF receptor 2. Overall, CaD, as a novel potential therapeutic drug for DKD, plays a key role in protecting renal function and restoring autophagy by blocking VEGF/VEGFR2 and inhibiting the PI3K/AKT/mTOR signaling pathway.
  • ||||||||||  Insulin resistance exacerbates lung inflammation in obese patients via PI3K/Akt signaling pathway (6B) -  Aug 26, 2019 - Abstract #ERS2019ERS_3544;    
    The expression levels of the phosphorylated IRS-1 and phosphorylated Akt in lung tissue of obese group was significantly increased. Conclusion These findings indicate that obesity results in a systemic state of low-grade inflammation and insulin resistance, and IR may increase lung inflammation by inducing activation of PI3K/Akt signaling pathway.
  • ||||||||||  metformin / generics
    Review, Journal:  Targeting acidity in cancer and diabetes. (Pubmed Central) -  Aug 25, 2019   
    ...For example, metformin is commonly used to reduce hyperglycemia in diabetic patients, and has been demonstrated to reduce cancer incidence...In diabetes, acidosis impacts the ability of insulin to bind to its receptor, leading to peripheral resistance and an exacerbation of symptoms. Thus, acidosis may be a relevant therapeutic target, and we describe three approaches for targeting: buffers, nanomedicine, and proton pump inhibitors.
  • ||||||||||  Review, Journal:  Targeting PI3K signaling in cancer: Challenges and advances. (Pubmed Central) -  Aug 25, 2019   
    The effort to develop isoform-specific inhibitors, together with novel therapeutic strategies aimed at reducing the toxicity and adverse effects, opened a new promising era for PI3K inhibitors. In addition, we will focus on the recent emergence of class II and III PI3K inhibitors, which helped to define their class I non-redundant role.
  • ||||||||||  Review, Journal:  Structural Determinants of Isoform Selectivity in PI3K Inhibitors. (Pubmed Central) -  Aug 23, 2019   
    We present an analysis of the available structure-selectivity-activity relationship data to highlight key insights into how the various regions of the PI3K binding site influence isoform selectivity. The picture that emerges is one that is far from simple and emphasizes the complex nature of protein-inhibitor binding, involving protein flexibility, energetics, water networks and interactions with non-conserved residues.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Preclinical, Journal:  Effects of scalp electroacupuncture on the PI3K/Akt signalling pathway and apoptosis of hippocampal neurons in a rat model of cerebral palsy. (Pubmed Central) -  Aug 23, 2019   
    Basso, Beattie and Bresnahan (BBB) locomotor scores, hippocampal protein expression of Akt and p-Akt (by Western blot analysis) and neuronal apoptosis in hippocampal tissue (by histopathology) were assessed at 7, 14 and 21 days post-CP induction.Results CP rats receiving scalp EA treatment demonstrated improved behavioural scores, less hippocampal neuronal apoptosis and higher expression levels of Akt and p-Akt (p<0.05) at all time points studied compared with untreated CP rats. There were no significant differences observed between CP+EA+LY294002 and untreated CP model groups.Conclusions The effects of scalp EA on the PI3K/ Akt signalling pathway may represent one of the mechanisms involved in the inhibition of hippocampal neuronal apoptosis and improvement of deficits associated with CP in a rat model.
  • ||||||||||  Review, Journal:  Pitfalls of Combining Novel Agents in Lymphoma. (Pubmed Central) -  Aug 23, 2019   
    Thus far, research has shown that combination therapies are successful when not only avoiding overlapping toxicity but also capitalizing on synergy. We believe that more specific targets and an improved understanding of their off-/on-target effects will further successful novel combinations.
  • ||||||||||  Venclexta (venetoclax) / Roche, AbbVie, Aliqopa (copanlisib) / Bayer
    Journal, IO Biomarker:  Targeted inhibition of PI3Kα/δ is synergistic with BCL-2 blockade in genetically defined subtypes of DLBCL. (Pubmed Central) -  Aug 23, 2019   
    Indeed, we observed synergistic activity of copanlisib/venetoclax in BCR-dependent DLBCLs with genetic bases for BCL-2 dysregulation in vitro and confirmed these findings in a xenograft model. These results provide pre-clinical evidence for the rational combination of PI3Kα/δ and BCL-2 blockade in genetically defined DLBCLs.
  • ||||||||||  Journal:  LSD1 Activates PI3K/AKT Signaling Through Regulating p85 Expression in Prostate Cancer Cells. (Pubmed Central) -  Aug 22, 2019   
    In this study, we show that LSD1 can activate PI3K/AKT pathways in absence of androgen stimulation, and we further demonstrate that LSD1 transcriptionally regulates the expression of PI3K regulatory subunit, p85, possibly through epigenetic reprogramming of enhancer landscape in PCa cells. Our study suggests that LSD1 has dual functions in promoting PCa development, that it enhances AR signaling through its coactivator function, and that it activates PI3K/AKT signaling through increasing p85 gene expression.