- |||||||||| LY294002 / Eli Lilly
Journal: Leonurine pretreatment protects the heart from myocardial ischemia-reperfusion injury. (Pubmed Central) - Dec 21, 2023 In addition, the upregulation of p-Akt, Bcl-2/Bax induced by SCM-198 treatment were blocked by PI3K inhibitor LY294002, and the total protein level of Akt was not affected by SCM-198 pretreatment. Our experimental results indicated that SCM-198 could have a cardioprotective effect on I/R injury, which confirmed the utility of SCM-198 preconditioning as a strategy to prevent I/R injury.
- |||||||||| Aliqopa (copanlisib) / Bayer
Enrollment change, Trial completion date, Trial termination, Trial primary completion date: Window Trial to Evaluate Molecular Response to PI3K Inhibition With Copanlisib in r/r Adult B-cell ALL (clinicaltrials.gov) - Dec 21, 2023 P1, N=3, Terminated, Our experimental results indicated that SCM-198 could have a cardioprotective effect on I/R injury, which confirmed the utility of SCM-198 preconditioning as a strategy to prevent I/R injury. N=10 --> 3 | Trial completion date: May 2024 --> Apr 2023 | Recruiting --> Terminated | Trial primary completion date: May 2024 --> Apr 2023; Sponsor halted clinical development of study drug
- |||||||||| Preclinical, Journal: Recapitulation of anti-aging phenotypes by global overexpression of PTEN in mice. (Pubmed Central) - Dec 20, 2023
These changes in fat, macrophages, liver, muscle, hippocampus, and plasma may be considered "aging rate indicators" in that they seem to be consistently changed across many of the long-lived mouse models and may help to extend lifespan by delaying many forms of late-life illness. Our new findings show that PTENOE mice can be added to the group of long-lived mice that share this multi-tissue suite of biochemical characteristics.
- |||||||||| Monjuvi (tafasitamab-cxix) / Incyte, parsaclisib (INCB50465) / Incyte
Phase classification, Trial completion date, Trial primary completion date, Combination therapy, Pan tumor: topMIND: A Study Evaluating Safety, PK, and Efficacy of Tafasitamab and Parsaclisib in Participants With Relapsed/Refractory Non Hodgkin Lymphoma (R/R NHL) or Chronic Lymphocytic Leukemia (CLL) (clinicaltrials.gov) - Dec 19, 2023 P1/2, N=54, Active, not recruiting, BFGF may provide a potential avenue for CAVD therapy. Phase classification: P1b/2a --> P1/2 | Trial completion date: Oct 2023 --> Dec 2024 | Trial primary completion date: Oct 2023 --> Dec 2024
- |||||||||| LY294002 / Eli Lilly
Journal: LncRNA MALAT1 Expression Regulates Breast Cancer Progression via PI3K/AKT/mTOR Pathway Modulation. (Pubmed Central) - Dec 19, 2023 The study also investigated the cross-talk of lncRNA MALAT1 and PI3K pathway genes by inhibiting it with PI3K inhibitor (LY294002) in MDA-MB-231 cell line...Moreover, the study proposes a mechanism of action of MALAT1, demonstrating that its inhibition can reduce the expression of the PI3K/AKT/mTOR axis. These findings emphasize the potential significance of targeting MALAT1 as a therapeutic strategy for breast cancer, and further exploration of this interaction is warranted to gain deeper insight into the molecular mechanism of this lncRNA.
- |||||||||| VS-5584 / Verastem
Preclinical, Journal: The lncRNA expression profile signature of leukemia stem cells is altered upon PI3K/mTOR inhibition: an in vitro and in silico study. (Pubmed Central) - Dec 18, 2023 We suppressed PI3K/Akt/mTOR signaling in LSC and HSC cell-lines by specific PI3K/mTOR dual-inhibitor (VS-5584) and confirmed the inhibition by antibody-array...SRA was predicted to interact with CREB1, RARA, and PPARA. The possible DELs' targets were predicted to form six ontological groups, be highly enriched for phosphoprotein, and be involved in "PPAR signaling pathway" and "ChREBP regulation by carbohydrates and cAMP." These results will help to elucidate the roles of lncRNAs in the mechanisms that provide selective advantages to leukemia stem cells.
- |||||||||| Journal: New Dipyrroloquinones from a Plant-Derived Endophytic Fungus Talaromyces sp. (Pubmed Central) - Dec 17, 2023
"Switching" between apoptosis and autophagy using PI3K and Raf inhibitors with Bcl-2:beclin-1 complex formation opens new therapeutic perspectives against gliomas. As a result, 1-3 inhibited the LPS-stimulated NO production in macrophage RAW264.7 cells, with IC values of 20.3, 30.7, and 20.6
- |||||||||| Journal: Melatonin Inhibits Testosterone Synthesis in Rooster Leydig Cells by Targeting CXCL14 through miR-7481-3p. (Pubmed Central) - Dec 17, 2023
Interference with CXCL14 significantly inhibited the phosphorylation level of PI3K and AKT, and the inhibited PI3K/AKT signal pathway could reverse the inhibitory effect of CXCL14 on testosterone synthesis and the expression of StAR, CYP11A1 and 3?-HSD in rooster Leydig cells. Our results indicated that melatonin inhibits testosterone synthesis by targeting miR-7481-3p/CXCL14 and inhibiting the PI3K/AKT pathway.
- |||||||||| buparlisib (AN2025) / Novartis, Adlai Nortye
Journal: Insulin feedback is a targetable resistance mechanism of PI3K inhibition in glioblastoma. (Pubmed Central) - Dec 17, 2023 Reducing insulin feedback improves the efficacy of PI3K inhibition in GBM in mice, and hyperglycemia worsens progression-free survival in patients with GBM treated with PI3K inhibition. These findings indicate that hyperglycemia is a critical resistance mechanism associated with PI3K inhibition in GBM and that anti-hyperglycemic therapy may enhance PI3K inhibitor efficacy in GBM patients.
- |||||||||| Epidaza (chidamide) / Chipscreen, Meiji Seika, Eisai, HUYA Bioscience, parsaclisib (INCB50465) / Incyte
Enrollment open: PI3K? Inhibitor Parsaclisib Combined With Chidamide for the Treatment of Relapsed/Refractory Peripheral T-cell Lymphoma (clinicaltrials.gov) - Dec 12, 2023 P1/2, N=28, Recruiting, These results suggested that AS-IV may promote angiogenesis after ischemic stroke through increasing the expression of VEGF via PI3K/Akt/mTOR pathway, which unveils novel therapeutic effects of AS-IV and suggests promising application of AS-IV in ischemic stroke. Not yet recruiting --> Recruiting
- |||||||||| Piqray (alpelisib) / Novartis
Journal: Alpelisib decreases nevocytes of congenital melanocytic nevi. (Pubmed Central) - Dec 10, 2023 Alpelisib is an approved drug with an adequate safety profile used in another mosaicism affecting PI3K (PROS). Further studies are needed to evaluate its efficacy in treating CMN and potentially, their complications, either with local or systemic administration, alone or in combination.
- |||||||||| sirolimus / Generic mfg.
Journal: FilGAP regulates tumor growth in Glioma through the regulation of mTORC1 and mTORC2. (Pubmed Central) - Dec 9, 2023 The mechanistic target of rapamycin (mTOR) is a serine/threonine protein kinase that forms the two different protein complexes, known as mTORC1 and mTORC2...Finally, we showed that depletion of FilGAP in KINGS-1 and U-87MG cells significantly reduced spheroid growth. These results suggest that FilGAP may contribute to tumor growth in glioma by regulating mTORC1/2 activities.
- |||||||||| LY294002 / Eli Lilly
Journal: Emodin exhibits anti-acne potential by inhibiting cell growth, lipogenesis, and inflammation in human SZ95 sebocytes. (Pubmed Central) - Dec 7, 2023 In addition, emodin could decrease the secretion of pro-inflammatory cytokines IL-6 and IL-8, and suppress the expression of NLRP3, capase-1, IL-1?, and IL-18 in SZ95 sebocytes exposed to Cutibacterium acnes. Overall, our study provides preliminary evidence supporting the anti-growth, anti-lipogenic and anti-inflammatory properties of emodin, indicating the potential therapeutic application of emodin for acne treatment.
- |||||||||| Review, Journal: Emerging treatment approaches for triple-negative breast cancer. (Pubmed Central) - Dec 5, 2023
These advancements present a promising frontier for tailored interventions with the potential to significantly improve outcomes for TNBC patients. Interestingly, while TNBC poses a complex challenge, it also serves as a paradigm and an opportunity for translational research and innovative therapies in the field of oncology.
- |||||||||| Piqray (alpelisib) / Novartis
Journal: Mutant PIK3CA is a targetable driver alteration in histiocytic neoplasms. (Pubmed Central) - Dec 4, 2023 Alpelisib demonstrated a tolerable safety profile at a dose of 750mg/week and clinical and metabolic complete remission in a PIK3CA-mutated LCH patient. These data demonstrate PIK3CA as a targetable non-canonical driver of LCH and underscore the importance of mutational analysis-based personalized treatment in histiocytic neoplasms.
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