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  • ||||||||||  Simultaneous Measurement of PIP2 and KV7.2 Current in Single Cells (MCP Hall A) -  Aug 22, 2024 - Abstract #Neuroscience2024Neuroscience_889;    
    We conclude that real-time correlation of KV7.2 current with intracellular PIP2 levels measured in single cells using a fluorescent biosensor is feasible. This approach will have value in studies of ion channel regulation by PIP2.
  • ||||||||||  sirolimus / Generic mfg.
    Microelectrode array (MEA) for assessing neuronal network restoration in PTEN knockdown primary hippocampal neurons. (MCP Hall A) -  Aug 22, 2024 - Abstract #Neuroscience2024Neuroscience_490;    
    A structured statistical framework was applied to evaluate the activity of rapamycin, accounting for experimental variability and potential neurotocixity over time. Applying the MEA assay to complement other measures of PTEN loss in neurons provides data that may further discriminate between inhibitors of PI3K signaling as drug repurposing candidates.
  • ||||||||||  Piqray (alpelisib) / Novartis
    Journal:  A Perspective of PI3K/AKT/mTOR Pathway Inhibitors to Overcome Drug-resistance in Breast Cancer Therapy. (Pubmed Central) -  Aug 22, 2024   
    Therefore, utilizing PI3K/mTOR/AKT inhibitors in combination with currently available strategies could be an optimistic approach to overcoming drug resistance and resensitizing drug-resistant tumor cells of BC. Here, in this perspective, BC cancer therapies related to drug resistance, the involvement of PI3K/AKT/mTOR pathway in drug resistance and multi-drug resistance, and the role of PI3K/AKT/mTOR inhibitors in getting rid of drug resistance have been illuminated.
  • ||||||||||  alendronate / Generic mfg.
    Journal:  Epimedin A inhibits the PI3K/AKT/NF-?B signalling axis and osteoclast differentiation by negatively regulating TRAF6 expression. (Pubmed Central) -  Aug 17, 2024   
    AYR may promote CRC cell apoptosis by suppressing the PI3K/AKT signaling pathway, which provides a basis for further research on the safe and effective use of AYR for the treatment of CRC. The findings indicated that EA can negatively regulate osteoclastogenesis by inhibiting the TRAF6/PI3K/AKT/NF-?B axis and that ameliorating ovariectomy-induced osteoporosis in rats with EA may be a promising potential therapeutic strategy for the treatment of osteoporosis.
  • ||||||||||  Review, Journal:  Molecular mechanisms of PTEN in atherosclerosis: A comprehensive review. (Pubmed Central) -  Aug 17, 2024   
    Previous studies have shown that PTEN is closely related to atherosclerosis. This article reviews the role of PTEN in atherosclerosis from the perspectives of autophagy, apoptosis, inflammation, proliferation, and angiogenesis.
  • ||||||||||  Review, Journal:  Targeting the RAS upstream and downstream signaling pathway for Cancer treatment. (Pubmed Central) -  Aug 17, 2024   
    Furthermore, inhibitors of PI3K (e.g., apitolisib, copanlisib), AKT (e.g., ipatasertib, perifosine), and mTOR (e.g., sirolimus, temsirolimus) exhibit promising efficacy against various cancers such as Invasive Breast Cancer, Lymphoma, Neoplasms, and hematological malignancies. This review offers an overview of small molecule inhibitors targeting specific proteins within the RAS upstream and downstream signaling pathways in cancer.
  • ||||||||||  AZD8186 / AstraZeneca
    Journal:  Systematic analysis of TREM2 and its carcinogenesis in pancreatic cancer. (Pubmed Central) -  Aug 15, 2024   
    In conclusion, our comprehensive analysis identified that TREM2 expression level was correlated with the TME and the immunosuppressive effects. In particular, our study indicated that TREM2 was involved in the progression of pancreatic cancer.
  • ||||||||||  Journal:  SMYD5 methylation of rpL40 links ribosomal output to gastric cancer. (Pubmed Central) -  Aug 14, 2024   
    Finally, combining SMYD5 depletion with PI3K-mTOR inhibition and chimeric antigen receptor T?cell administration cures an otherwise lethal in vivo mouse model of aggressive GAC-derived peritoneal carcinomatosis. Together, our work uncovers a ribosome-based epigenetic mechanism that facilitates the evolution of malignant GAC and proposes SMYD5 targeting as part of a potential combination therapy to treat this cancer.
  • ||||||||||  inavolisib (GDC-0077) / Roche
    Journal:  Discovery of Unprecedented Human Stercobilin Conjugates. (Pubmed Central) -  Aug 14, 2024   
    Two unique metabolites (M18 and M19) were detected in feces of human volunteers dosed orally with [14C]inavolisib with a molecular ion of parent plus 304 Da...These conjugates were confirmed by generating them using in vitro fecal homogenate incubation via non-enzymatic and possibly enzymatic reactions. Given the unique nature of the conjugate, it is plausible that it may have been overlooked with other small molecule drugs in prior studies.
  • ||||||||||  Zyclara (imiquimod) / Mochida, Viatris, Bausch Health
    Preclinical, Journal:  Unlocking milk thistle's anti-psoriatic potential in mice: Targeting PI3K/AKT/mTOR and KEAP1/NRF2/NF-?B pathways to modulate inflammation and oxidative stress. (Pubmed Central) -  Aug 13, 2024   
    This study aimed to investigate the role of MT extract topical application as a potential treatment for imiquimod (IMQ)-induced psoriatic lesions in mice with particular emphasis on phosphoinositol-3 Kinase (PI3K)/ protein kinase B (AKT)/ mammalian target of rapamycin (mTOR) and Kelch-like ECH-associated protein 1 (KEAP1)/ nuclear factor erythroid-2-related factor (NRF2)/ nuclear factor-kappa B (NF-?B) molecular cascades involvement...Such improvements were confirmed by alleviating the histopathological alteration. Thus, MT extract could be a promising therapeutic agent for psoriasis treatment by inhibiting PI3K/AKT/mTOR cascade, along with NRF2 signaling activation.
  • ||||||||||  Opdivo (nivolumab) / BMS, Copiktra (duvelisib) / Secura Bio, Yakult Honsha
    Enrollment closed, Enrollment change, Trial completion date, Trial primary completion date, Combination therapy, Metastases:  Duvelisib in Combination With Nivolumab in Patients With Advanced Unresectable Melanoma (clinicaltrials.gov) -  Aug 9, 2024   
    P1/2,  N=13, Active, not recruiting, 
    The use of immunohistochemical staining intensity and cell scoring with ROC cut-off is effective to elaborate the effects of PTEN in colorectal cancer (PTEN value?>?199.0 was classified as strong and???199.0 as weak). Recruiting --> Active, not recruiting | N=42 --> 13 | Trial completion date: Oct 2029 --> Dec 2028 | Trial primary completion date: Apr 2028 --> Feb 2024
  • ||||||||||  Journal:  PTEN-Long inhibits the biological behaviors of glioma cells. (Pubmed Central) -  Aug 8, 2024   
    inhibitor IPI549 has a suppressive role in host inflammation and alleviates cerebral pathology, which supports IPI549 as a new malaria treatment option with potential therapeutic implications for cerebral malaria. PTEN-Long inhibits the proliferation, migration, and invasion and induces apoptosis in glioma cells by inhibiting PI3K-AKT-NF-?b signaling, implying that PTEN-Long may be a new target for glioma treatment.
  • ||||||||||  dexamethasone / Generic mfg.
    Journal:  KLF9 regulates osteogenic differentiation of mesenchymal stem cells. (Pubmed Central) -  Aug 7, 2024   
    Finally, we discovered that KLF9 expression can be induced by dexamethasone which is an essential component in osteogenic induction medium. Taken together, our study provides new insights into the regulatory role of KLF9 in osteogenic differentiation of MSCs.
  • ||||||||||  Preclinical, Journal:  miR-144-3p Targets GABRB2 to Suppress Thyroid Cancer Progression In Vitro. (Pubmed Central) -  Aug 2, 2024   
    GABRB2 overexpression partially mitigated the tumor-suppressive effect of miR-144-3p overexpression. In conclusion, miR-144-3p targets GABRB2 to inhibit PI3K/AKT activation, thereby inhibiting the progression of thyroid cancer in vitro.