PI3K inhib 
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  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Role of PI3K/AKT Signaling Pathway in Nucleus Pulposus Cells. (Pubmed Central) -  Sep 24, 2021   
    Nucleus pulposus (NP) cells were isolated from SD rat, and thereafter, passage three (P3) NP cells were divided into the following experimental groups: control, PI3K/AKT agonist IGF-1 (25 ng/ml, 50 ng/ml, and 100 ng/ml), and PI3K/AKT inhibitor LY294002 (5 μM, 10 μM, and 20 μM)...However, the activation of PI3K/AKT pathway partly prevented the NP cell from apoptosis and promoted their proliferation. Meanwhile, its activation also delayed the loss of extracellular matrix.
  • ||||||||||  perifosine (D21266) / AEterna Zentaris
    Journal:  HTR2A promotes the development of cardiac hypertrophy by activating PI3K-PDK1-AKT-mTOR signaling. (Pubmed Central) -  Sep 23, 2021   
    Finally, we showed that HTR2A regulated AKT-mTOR signaling through activating the PI3K-PDK1 pathway, and inhibition of either PI3K or PDK1 blocked the roles of HTR2A in regulating AKT-mTOR signaling and cardiomyocyte hypertrophy. Altogether, these findings demonstrated that HTR2A activated PI3K-PDK1-AKT-mTOR signaling and promoted cardiac hypertrophy.
  • ||||||||||  Journal, PARP Biomarker:  GHR is involved in gastric cell growth and apoptosis via PI3K/AKT signalling. (Pubmed Central) -  Sep 23, 2021   
    On the basis of the results, that GHR regulates gastric cancer cell growth and apoptosis through controlling G1 cell cycle progression via mediating PI3K/AKT signalling pathway. These findings provide a novel understanding for the role of GHR in gastric cancer.
  • ||||||||||  Journal:  Nutrition and PI3K/Akt signaling are required for p38-dependent regeneration. (Pubmed Central) -  Sep 23, 2021   
    Our results demonstrate that Ask1 controls the activation of p38 through Ser83, and that the phosphorylation of p38 during regeneration is nutrient sensitive. This mechanism is important for discriminating between p38 and JNK in the cells involved in tissue repair and regenerative growth.
  • ||||||||||  Piqray (alpelisib) / Novartis
    Journal:  Alpelisib in the treatment of metastatic HR+ breast cancer with PIK3CA mutations. (Pubmed Central) -  Sep 22, 2021   
    Herein, we review its pharmacodynamic and pharmacokinetic properties, safety and efficacy data, as well as Phase III SOLAR-1 trial, prompting FDA approval of alpelisib in hormone receptor-positive metastatic breast cancer harboring PIK3CA mutations. Furthermore, implications for clinical use and current research will also be discussed.
  • ||||||||||  Journal:  miRNA-26b suppresses the TGF-β2-induced progression of HLE-B3 cells via the PI3K/Akt pathway. (Pubmed Central) -  Sep 21, 2021   
    Together, the depression-like behaviors in LPS-treated mice were alleviated by a single dose of Qc likely via inhibition of the activations PI3K/AKT/NF-κB inflammation signaling and subsequent improvement of neuroplasticity. The miR-26b suppresses TGF-β2-induced growth, migration, and EMT in HLE-B3 cells by regulating the PI3K/Akt signaling pathway.
  • ||||||||||  [VIRTUAL] Pathway-Driven Drug Repositioning in Systemic Sclerosis from Omics Data () -  Sep 21, 2021 - Abstract #ACRCONVERGENCE2021ACR_CONVERGENCE_1247;    
    Multiple small molecule inhibitors have been identified that regulate gene set pathways that are specific to two molecular subsets of SSc patients determined by gene expression profiling. Testing these perturbagens within cell culture and 3D skin like tissues showed that PI3K inhibitors may inhibit multiple aspects of SSc disease progression in dermal fibroblasts.
  • ||||||||||  cisplatin / Generic mfg.
    Journal:  Investigation of EGFR/pi3k/Akt signaling pathway in seminomas. (Pubmed Central) -  Sep 19, 2021   
    The EGFR/pI3 k/Akt signaling pathway is linked to TDRG1, which regulates chemosensitivity to cisplatin; this is a mechanism of resistance to treatment. TDRG1 and the EGFR/pI3 k/pAkt pathway could be therapeutic targets for seminomas resistant to cisplatin.
  • ||||||||||  buparlisib (BKM120) / Novartis, Adlai Nortye
    Journal:  Cutaneous T cell lymphoma PDX drug screening platform identifies cooperation between inhibitions of PI3Kα/δ and HDAC. (Pubmed Central) -  Sep 19, 2021   
    A PI3K inhibitor, BKM120, was tested in our patient-derived xenograft model leading to disease attenuation and prolonged survival...Additional studies showed synergistic combination of PI3K-α/δ inhibitors with histone deacetylase (HDAC) inhibitors. The strong preclinical efficacy of this potent combination against multiple PDX models makes it an excellent candidate for further clinical development.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, SP600125 / BMS
    Journal:  Cadmium induces CCL2 production in glioblastoma cells via activation of MAPK, PI3K, and PKC pathways. (Pubmed Central) -  Sep 19, 2021   
    Moreover, when cells were pretreated with Ro 32-0432 (an inhibitor of calcium-dependent PKC) and LY294002 (a PI3K inhibitor), this also resulted in a down-regulation of any Cd-induced CCL2 expression. Taken together, the results of this study allow for the conclusion to be made that CCL2 up-regulation in U-87 MG cells induced by Cd is mediated, in part, by an activation of MAPK, PI3K/Akt, and PKC pathways.
  • ||||||||||  imatinib / Generic mfg., sirolimus / Generic mfg.
    Review, Journal, Combination therapy:  Combating TKI resistance in CML by inhibiting the PI3K/Akt/mTOR pathway in combination with TKIs: a review. (Pubmed Central) -  Sep 19, 2021   
    Even in Imatinib, Nilotinib, and Ponatinib-resistant CML cells, a dual PI3K/mTOR inhibitor, BEZ235, showed antiproliferative activity. Therefore, by considering the literature data of these reviews and further examining some of the reported inhibitors, which proved effective against the PI3K/Akt/mTOR signaling pathway in multiple cancers, may improve the therapeutic approaches towards TKI-resistant CML cells where the respective signaling pathway gets upregulated.
  • ||||||||||  hydroxychloroquine / Generic mfg.
    Clinical, Review, Journal:  Aminoquinolines as Translational Models for Drug Repurposing: Anticancer Adjuvant Properties and Toxicokinetic-Related Features. (Pubmed Central) -  Sep 18, 2021   
    The low cost and availability on the world market have converted aminoquinolines into "star drugs" for pharmaceutical repurposing, but a continuous pharmacovigilance is necessary because these antimalarials have multiple modes of action/unwanted targets, relatively narrow therapeutic windows, recurrent adverse effects, and related poisoning self-treatment. Therefore, their use must obey strict rules, ethical and medical prescriptions, and clinical and laboratory monitoring.
  • ||||||||||  Journal:  Hyperoside suppresses BMP-7-dependent PI3K/AKT pathway in human hepatocellular carcinoma cells. (Pubmed Central) -  Sep 18, 2021   
    In addition, silencing of BMP-7 abrogated the difference of AKT phosphorylation between cells with and without HP treatment. Our results indicated that HP suppressed cell proliferation by inhibiting the BMP-7-dependent PI3K/AKT signaling pathway in HepG2 HCC cells, and either HP supplement or targeting BMP-7 might be a promising treatment against HCC.
  • ||||||||||  Piqray (alpelisib) / Novartis
    [VIRTUAL] Recurrent PIK3CA H1047R-Mutated Infiltrative Facial Lipomatosis () -  Sep 18, 2021 - Abstract #CAP2021CAP_602;    
    Although there are no sufficient data about an increased risk of PIK3CA-associated adult cancers among PROS patients, cooperating mutations might still contribute to cancer development in this population of patients. Besides surgical debulking, novel therapeutic agents such as Alpelisib (PI3K inhibitor) continue to be trialed in patients with PROS to prevent future recurrence.
  • ||||||||||  Journal:  RNF8 promotes epithelial-mesenchymal transition in lung cancer cells via stabilization of Slug. (Pubmed Central) -  Sep 17, 2021   
    Taken together, these results indicate that RNF8 is a key regulator of EMT process in lung cancer and suggest that inhibition of RNF8 could be a useful strategy for lung cancer treatment. Implications: This study provides a new mechanistic insight into the noval role of RNF8 and identifies RNF8 as a potential new therapeutic target for the treatment of lung cancer.
  • ||||||||||  Piqray (alpelisib) / Novartis, buparlisib (BKM120) / Novartis, Adlai Nortye
    Journal:  Divergent Roles of PI3K Isoforms in PTEN-Deficient Glioblastomas. (Pubmed Central) -  Sep 17, 2021   
    BKM120 extends the survival of mice bearing intracranial tumors in which p110β, but not p110α, has been genetically ablated in the Pten/p53 null glioma, indicating that BKM120 fails to inhibit p110β effectively. Our study suggests that the failure of PI3K inhibitors in GBM may be due to insufficient inhibition of p110β and indicates a need to develop brain-penetrant p110α/β inhibitors.