PI3K inhib 
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  • ||||||||||  paclitaxel / Generic mfg.
    Journal:  H1.0 induces paclitaxel-resistance genes expression in ovarian cancer cells by recruiting GCN5 and androgen receptor. (Pubmed Central) -  Aug 11, 2022   
    These findings suggest that Txr in ovarian cancer involves the PI3K/AKT pathway and leads to upregulation of histone H1.0, recruitment of GCN5 and AR, followed by upregulation of a sub-group of Txr genes that include ABCB1 and ABCG2. This study is the first report describing the relationship between histone H1.0 and GCN5 which cooperate to induce AR-dependent Txr in ovarian cancer cells.
  • ||||||||||  Piqray (alpelisib) / Novartis, inavolisib (GDC-0077) / Roche, serabelisib (MLN1117) / Takeda, Petra Pharma, Faeth Therap
    Journal:  Comparative molecular dynamics analyses on PIK3CA hotspot mutations with PI3Kα specific inhibitors and ATP. (Pubmed Central) -  Aug 11, 2022   
    Moreover, correlated motions of all residues were generally higher for ATP except the H1047R mutation which exhibited a distinguishable reduction. The results presented here could be guiding for pre-clinical and clinical studies of personalized medicine where individual mutations are a strong consideration point.
  • ||||||||||  buparlisib (AN2025) / Novartis, Adlai Nortye
    Preclinical, Journal:  Apoptin Overexpression Efficiently Amplified Cytotoxic Effects of PI3K Inhibition Using BKM120 in Lymphoblastic Leukemia Cell Lines. (Pubmed Central) -  Aug 10, 2022   
    The efficacy of apoptin transduction was not limited to these findings, as we reported for the first time that the overexpression of this gene could potentiate the anti-leukemic property of pan PI3K inhibitor BKM120. The results of this study showed that the transduction of apoptin into lymphoblastic leukemia cell lines induced cytotoxic effects and enhanced therapeutic value of PI3K inhibition; however, further investigations are demanded to ascertain the safety and the efficacy of apoptin transduction in patients with ALL.
  • ||||||||||  Review, Journal:  Research Progress on the Regulation Mechanism of Key Signal Pathways Affecting the Prognosis of Glioma. (Pubmed Central) -  Aug 10, 2022   
    In this way, notch cannot only be treated for glioma stem cells in clinic, but also be used as an evaluation index to evaluate the prognosis, and provide an exploratory attempt for the direction of glioma treatment. MiRNA plays an important role in diagnosis, and in the treatment of glioma, VPS25, KCNQ1OT1, KB-1460A1.5, and CKAP4 are promising prognostic indicators and a potential therapeutic targets for glioma, meanwhile, Rheb is also a potent activator of Signaling cross-talk etc. It is believed that these studies will help us to have a deeper understanding of glioma, so that we will find new and better treatment schemes to gradually conquer the problem of glioma.
  • ||||||||||  Molecular modelling and synthesis of benzimidazole derivatives as PI3K inhibitors (Virtual-only (Zoom)) -  Aug 9, 2022 - Abstract #ACSFall2022ACS_Fall_13112;    
    PI3K inhibitors were synthesized and characterized using FT- IR, MASS, 1H and 13C NMR analytical methods. In vitro, pharmacological studies of synthesized derivatives will be done on breast cancer cell line (MDA-MB-231) using MTT assay.
  • ||||||||||  Journal:  YBX1 promotes MSC osteogenic differentiation by activating the PI3K/AKT pathway. (Pubmed Central) -  Aug 6, 2022   
    Our results indicate that calycosin shows inhibitory effects on CRC cells, which might be obtained by targeting ERβ, upregulating PTEN, and inhibiting the PI3K/Akt signal pathway. Our study provides a new target and theoretical basis for the treatment of bone diseases.
  • ||||||||||  Journal:  Lupeol protects against cardiac hypertrophy via TLR4-PI3K-Akt-NF-κB pathways. (Pubmed Central) -  Aug 5, 2022   
    Moreover, pre-treatment with a TLR4 agonist RS 09 abolished the protective effects of lupeol and restored the inhibition of PI3K-Akt-NF-κB signaling by lupeol in PE-stimulated NRCMs. Collectively, our results demonstrate that the lupeol protects against cardiac hypertrophy via anti-inflammatory mechanisms, which results from inhibiting the TLR4-PI3K-Akt-NF-κB signaling.
  • ||||||||||  Journal:  PI3K inhibitors in haematological malignancies. (Pubmed Central) -  Aug 5, 2022   
    SGKL targets the PI3K/Akt/mTOR pathway by altering gut microbiota and metabolites, which ameliorates altered behavior and inflammation in the hippocampus. No abstract available
  • ||||||||||  Journal:  Effects of circFOXO3 on the Proliferation and Invasion of Liver Cancer Cells by Regulating PI3K/Akt Pathway. (Pubmed Central) -  Aug 3, 2022   
    Compared with the circFOXO3 mimic group, the apoptosis rate of HuH-7 liver cancer cells in the circFOXO3 mimic + PI3K activator group was significantly reduced (P < 0.05) and the PI3K/Akt pathway-related protein expression, cell viability, invasion and migration abilities were significantly increased (P < 0.05). Highly expressed circFOXO3 can inhibit the proliferation and invasion of HuH-7 liver cancer cells, which may be achieved by inhibiting the PI3K/Akt pathway.
  • ||||||||||  Biomarker, Journal, Real-world evidence, Next-generation sequencing, BRCA Biomarker, PARP Biomarker:  Clinical Application of Next-Generation Sequencing in Patients With Breast Cancer: Real-World Data. (Pubmed Central) -  Aug 2, 2022   
    NGS panel testing allowed MP-guided treatment in only 4.7% (6/127) of patients with advanced breast cancer in a real-world setting. The availability of matched drugs is critical for the realistic implementation of personalized treatment.
  • ||||||||||  Piqray (alpelisib) / Novartis
    PI3K Inhibition Sensitized Cancerous Cells to Tumor Treating Fields (TTFields) (Henry B. Gonzalez Convention Center, Exhibit Hall 1) -  Aug 1, 2022 - Abstract #ASTRO2022ASTRO_1949;    
    The current study demonstrated that the PI3K/AKT/mTOR signaling pathway is involved in reduced cancer cell sensitivity to long-term application of TTFields. Furthermore, re-sensitization to TTFields could be achieved with PI3K inhibitors, providing a rationale for further examining the potential benefit of TTFields concomitant with PI3K inhibitors.
  • ||||||||||  doxycycline / Generic mfg.
    TRIBBLES1 (TRIB1) Pseudokinase Induces Treatment Resistance in GBM by Promoting Survival of Tumor Cells through the Akt Pathway (Henry B. Gonzalez Convention Center, Exhibit Hall 1) -  Aug 1, 2022 - Abstract #ASTRO2022ASTRO_666;    
    Our data suggest that heightened expression of TRIB1 in GBM cells contributes to RT/TMZ resistance by activating the prosurvival Akt signaling cascades. Therefore, targeting TRIB1 mediated Akt activation could provide a therapeutic benefit over targeting Akt directly, which may reduce Akt’s oncogenic signal without risking the toxicity associated with available Akt- specific inhibitors.
  • ||||||||||  methotrexate / Generic mfg., floxuridine / Generic mfg.
    Journal:  DNA Base Pairing-Inspired Supramolecular Nanodrug Camouflaged by Cancer-Cell Membrane for Osteosarcoma Treatment. (Pubmed Central) -  Jul 30, 2022   
    More importantly, cell membrane camouflage significantly prolongs the circulation half-life of CCNPs, elevates the drug accumulation at tumor sites, and promotes anti-tumor efficacy in vivo. As a convenient and effective strategy to construct a biomimetic NP with high drug loading ratio, the CCNPs provide new potentials for precise and synergistic antitumor treatment.
  • ||||||||||  Journal:  PI3K inhibitors in chronic lymphocytic leukemia: where do we go from here? (Pubmed Central) -  Jul 29, 2022   
    However, the severe toxicity profile associated with the first-generation inhibitors idelalisib and duvelisib, combined with the availability of other more tolerable agents, have limited their use...Current strategies to overcome treatment limitations include intermittent dosing, which is established for copanlisib and zandelisib and under investigation for duvelisib and parsaclisib...In addition to these approaches, it is of interest to identify higher-resolution actionable biomarkers that can predict treatment responses and toxicity, and inform personalized treatment decisions. Here, we discuss the current status of PI3K inhibitors in CLL, factors limiting the use of currently approved PI3K inhibitors in CLL, current strategies to overcome these limitations, and where to go next.
  • ||||||||||  LY294002 / Eli Lilly, eganelisib (IPI-549) / Infinity Pharma
    Journal, IO biomarker:  Anti-Ischemic Effects of PIK3IP1 Are Mediated through Its Interactions with the ET-PI3Kγ-AKT Axis. (Pubmed Central) -  Jul 29, 2022   
    Our results demonstrated that ROS-induced cardiac cell death may occur through the ETA-PI3Kγ-AKT axis, and that PIK3IP1 inhibits binding with both ETA and PI3Kγ. Taken together, these findings reveal that PIK3IP1 plays an anti-ischemic role by reducing the likelihood of programmed cell death via interaction with the ETA-PI3Kr-AKT axis.
  • ||||||||||  Review, Journal:  Crucial Role of Oncogenic KRAS Mutations in Apoptosis and Autophagy Regulation: Therapeutic Implications. (Pubmed Central) -  Jul 29, 2022   
    Several therapies have been developed in order to overcome KRAS-induced cell death resistance and the downstream signaling pathways blockade, especially by combining MAPK and PI3K inhibitors, which demonstrated promising results. Understanding the involvement of KRAS mutations in apoptosis and autophagy regulation, might bring new avenues to the discovery of therapeutic approaches for CRCs harboring KRAS mutations.
  • ||||||||||  Journal:  Effect of Autophagy Inhibitors on Radiosensitivity in DNA Repair-Proficient and -Deficient Glioma Cells. (Pubmed Central) -  Jul 29, 2022   
    The extent of the DNA damage response remained high in the DNA-PKcs deficient cells following exposure to radiation, indicating their inability to repair the newly formed DNA-DSBs. On the other hand, radioresistant M059K cells showed more DNA damage response only when autophagy inhibitors were used with radiation, suggesting that the combination of autophagy inhibitors with radiation may interfere with DNA repair efficiency.
  • ||||||||||  parsaclisib (INCB50465) / Incyte
    Trial completion date:  A Study of INCB050465 in Subjects With Relapsed or Refractory Marginal Zone Lymphoma (CITADEL-204) (clinicaltrials.gov) -  Jul 29, 2022   
    P2,  N=110, Active, not recruiting, 
    On the other hand, radioresistant M059K cells showed more DNA damage response only when autophagy inhibitors were used with radiation, suggesting that the combination of autophagy inhibitors with radiation may interfere with DNA repair efficiency. Trial completion date: Jul 2022 --> Mar 2023