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67 Companies | 59 Products |
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344 Diseases | |
343 Trials |  |
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- | dubermatinib (TP-0903) / Sumitomo Dainippon
Journal: Gas6 attenuates lipopolysaccharide‑induced TNF‑α expression and apoptosis in H9C2 cells through NF‑κB and MAPK inhibition via the Axl/PI3K/Akt pathway. (Pubmed Central) - Feb 7, 2020
Pretreatment with TP‑0903 and Wortmannin abrogated the effects of Gas6 on phosphorylated‑IκB‑α, IκB‑α, NF‑κB, ERK1/2, JNK and p38 MAPK. These findings suggested that activation of Axl/PI3K/Akt signaling by Gas6 may inhibit LPS‑induced TNF‑α expression and apoptosis, as well as MAPK and NF‑κB activation.
- | Journal: Complement factor H‑related 3 overexpression affects hepatocellular carcinoma proliferation and apoptosis. (Pubmed Central) - Feb 7, 2020
Western blotting revealed that CFHR3 significantly inhibited the protein expression levels of phosphorylated (p)‑phosphoinositide 3‑kinase (PI3K), p‑protein kinase B (Akt) and p‑mammalian target of rapamycin (mTOR). Overexpression of CFHR3 suppressed proliferation and promoted apoptosis of HCC cells by inhibiting the PI3K/Akt/mTOR signaling pathway.
- | Preclinical, Journal, IO Biomarker: Structural Characterization and Antioxidant Activity of Polysaccharides from Athyrium multidentatum (Doll.) Ching in d-Galactose-Induced Aging Mice via PI3K/AKT Pathway. (Pubmed Central) - Feb 7, 2020
Overexpression of CFHR3 suppressed proliferation and promoted apoptosis of HCC cells by inhibiting the PI3K/Akt/mTOR signaling pathway. AMC polysaccharides attenuated d-galactose-induced oxidative stress and cell apoptosis by activating the PI3K/AKT pathway, which might in part contributed to their anti-aging activity.
- | Journal: Descending-SHIP2-mediated radiosensitivity enhancement through PI3K/Akt signaling pathway in laryngeal squamous cell carcinoma. (Pubmed Central) - Feb 7, 2020
This enhancement effect cause by SHIP2 knockdown derive from the inactivation of PI3K/Akt signaling pathway along with its downstream proteins. Our finding revealed a novel mechanism for sensitivity to radiotherapy caused by SHIP2 knockdown that called descending-SHIP2-mediated radiosensitivity enhancement (DSMRSE).
- MK-2206 / Merck (MSD), vistusertib (AZD2014) / AstraZeneca, gedatolisib (PF-05212384) / Curie Institute, Pfizer
Assessing the potential role of RICTOR expression as predictive factor of response to PI3K/mTOR pathway inhibitors in preclinical models of squamous cell lung cancer (Hall Bordeaux) - Feb 7, 2020 - Abstract #TAT2020TAT_58;
While CNG of RICTOR corresponded to increased protein expression, no correlation was observed with PI3K/mTOR pathway activity and drug sensitivity in vitro. We complemented this with genetic perturbation analyses, whose results aligned with pharmacological findings and suggest that Rictor does not represent a predictive biomarker of response towards PI3K/mTOR directed therapy.
- | quercetin (LY294002) / Eli Lilly
Journal: Propofol Reduces Inflammatory Brain Injury after Subarachnoid Hemorrhage: Involvement of PI3K/Akt Pathway. (Pubmed Central) - Feb 7, 2020
We complemented this with genetic perturbation analyses, whose results aligned with pharmacological findings and suggest that Rictor does not represent a predictive biomarker of response towards PI3K/mTOR directed therapy. These results suggest that propofol attenuates SAH-induced EBI by inhibiting inflammatory reaction and oxidative stress, which might be associated with the activation of PI3K/Akt signaling pathway.
- | Journal, IO Biomarker: Bovine ephemeral fever virus triggers autophagy enhancing virus replication via upregulation of the Src/JNK/AP1 and PI3K/Akt/NF-κB pathways and suppression of the PI3K/Akt/mTOR pathway. (Pubmed Central) - Feb 7, 2020
Furthermore, degradation of p62 was observed by immunoblotting, suggesting that BEFV infection triggers a complete autophagic response. Disruption of autophagosome-lysosome fusion by depleting LAMP2 resulted in reduction of virus yield, suggesting that formation of autolysosome benefits virus production.
- Piqray (alpelisib) / Novartis
Worsening Diabetes Control in Breast Cancer Patients Treated with Alpelisib (ENDOExpo) - Feb 7, 2020 - Abstract #ENDO2020ENDO_3070;
It can cause severe hyperglycemia and potential worsening of diabetes. Blood glucose should be monitored closely in patients with diabetes who are treated with alpelisib.
- glimepiride / Generic mfg.
Breast Cancer Treatment Causes Diabetes (ENDOExpo) - Feb 7, 2020 - Abstract #ENDO2020ENDO_2689;
Abstract: Introduction: Alpelisib (BYL719) a PI3K p110alpha inhibitor, was recently FDA approved to treat postmenopausal women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, PIK3CA gene mutation positive, advanced or metastatic breast cancer following progression on endocrine-based regimen...She was resuscitated with IV saline and started on glimepiride 2mg oral twice daily, glargine 5 units at bedtime with correctional insulin regimen...As more patients with cancer are approved for treatment with PI3K inhibitors, clinicians need to be more aware of the mechanism of hyperglycemia to effectively manage it. More evidence based consensus is needed on management of hyperglycemia with PI3K inhibition.
- | Ultane (sevoflurane) / Generic mfg.
Preclinical, Journal: Hemin treatment protects neonatal rats from sevoflurane-induced neurotoxicity via the phosphoinositide 3-kinase/Akt pathway. (Pubmed Central) - Feb 7, 2020
Our study demonstrates that hemin plays a protective role in anaesthesia-induced neurotoxicity by both inhibiting apoptosis via the PI3K/Akt pathway and increasing the expression of antioxidant enzymes, reducing oxidative damage. The results provide mechanistic insight into the effects of sevoflurane anaesthesia on the developing brain and suggest that hemin could help avoid these effects.
- | Journal: Epithelial PI3K-δ Promotes House Dust Mite-Induced Allergic Asthma in NLRP3 Inflammasome-Dependent and -Independent Manners. (Pubmed Central) - Feb 6, 2020
The results provide mechanistic insight into the effects of sevoflurane anaesthesia on the developing brain and suggest that hemin could help avoid these effects. The results of this study suggest that PI3K-δ-isoform can promote HDM-induced allergic airway inflammation via NLRP3 inflammasome-dependent response as well as via NLRP3 inflammasome-independent epithelial cell activation.
- | Journal: TREM2 Regulates Heat Acclimation-Induced Microglial M2 Polarization Involving the PI3K-Akt Pathway Following EMF Exposure. (Pubmed Central) - Feb 6, 2020
These results indicate that TREM2 and PI3K-Akt pathway are involved in the cross-tolerance protective effect of HA in microglial polarization towards the EMF exposure. This finding inspires future studies that aim to explore the non-drug approaches underlying EMF stimulation and other central nervous system (CNS) inflammatory diseases.
- | Journal: FeO Nanoparticles Attenuated Salmonella Infection in Chicken Liver Through Reactive Oxygen and Autophagy via PI3K/Akt/mTOR Signaling. (Pubmed Central) - Feb 6, 2020
The redox balance and inflammation response appeared normal in the process, as did the expression of the PI3K/Akt/mTOR signaling pathways. Taken together, our research demonstrate that the bacteriostatic activity of FeO-NPs in chickens is avaliable and safe, which can be an alternative to antibiotics for bacterial inhibition in poultry industry.
- | Journal: Strophanthidin Attenuates MAPK, PI3K/AKT/mTOR, and Wnt/β-Catenin Signaling Pathways in Human Cancers. (Pubmed Central) - Feb 6, 2020
Our in silico studies revealed that strophanthidin can interact with several key proteins from various pathways. Taken together, this study demonstrates the viability of strophanthidin as a promising anticancer agent, which may serve as a new anticancer drug.
- | cisplatin / Generic mfg.
Journal: miR-1269b Drives Cisplatin Resistance of Human Non-Small Cell Lung Cancer via Modulating the PTEN/PI3K/AKT Signaling Pathway. (Pubmed Central) - Feb 6, 2020
Further study demonstrated that miR-1269b targeted PTEN to modulate PI3K/AKT signaling pathway. In conclusion, these findings suggest that the miR-1269b/PTEN/PI3K/AKT-mediated network might promote cisplatin resistance in NSCLC, and that miR-1269b can be a potential therapeutic target for chemoresistance in NSCLC patients.
- | Journal: SPOCD1 accelerates ovarian cancer progression and inhibits cell apoptosis via the PI3K/AKT pathway. (Pubmed Central) - Feb 6, 2020
PI3K/AKT pathway was inhibited by knockdown of SPOCD1 in SKOV3 and CAOV3 cells. Our data suggest that SPOCD1 may act as a carcinogenesis factor by activating the PI3K/AKT pathway to restrained cell apoptosis in OC.
- | Journal: Propofol Inhibits the Migration and Invasion of Glioma Cells by Blocking the PI3K/AKT Pathway Through miR-206/ROCK1 Axis. (Pubmed Central) - Feb 6, 2020
The rescue assay indicated that the miR-206/ROCK1 axis was involved in propofol-induced inhibition on the migration, invasion, and PI3K/AKT pathway activation in glioma cells. Propofol inhibited the migration and invasion of glioma cells by blocking the PI3K/AKT pathway through the miR-206/ROCK1 axis, suggesting an effective clinical implication for the anesthetic to prevent the metastasis of glioma.
- ||| our review article on dual PI3K / mTOR inhibitors in #lymphoma is now out in the International Journal of Molecular Sciences. @AnastasiosStat2 @USI_university @USI_en @MDPIOpenAccess @EnteOspedaliero https://t.co/m48FfIZ23L (Twitter) - Feb 5, 2020
- | Journal: Retraction: Downregulation of uPAR and Cathepsin B Induces Apoptosis via Regulation of Bcl-2 and Bax and Inhibition of the PI3K/Akt Pathway in Gliomas. (Pubmed Central) - Feb 3, 2020
Propofol inhibited the migration and invasion of glioma cells by blocking the PI3K/AKT pathway through the miR-206/ROCK1 axis, suggesting an effective clinical implication for the anesthetic to prevent the metastasis of glioma. No abstract available
- Hydrophobic bile acids promote proliferation and activation of hepatic stellate cells by pi3k-dependent mechanisms (Poster Area) - Feb 2, 2020 - Abstract #EASLILC2020EASL-ILC_1301;
- | Journal: HSP70/HSF1 axis, regulated via a PI3K/AKT pathway, is a druggable target in Chronic Lymphocytic Leukemia. (Pubmed Central) - Feb 1, 2020
These data demonstrate that the HSP70 expression is regulated by the modulation of HSF1 activity through the activation of RAS-regulated pathways and suggest the HSP70/HSF1 interplay as an interesting target for anti-leukemic therapies. Finally, inhibition of PI3K, that activates AKT, reduced the expression of HSF1 and HSP70.
- | Journal: Low-dose Ionizing Radiation Attenuates Mast Cell Migration through Suppression of Monocyte Chemoattractant Protein-1 (MCP-1) Expression by Nr4a2. (Pubmed Central) - Feb 1, 2020
We further demonstrated that direct blockade of MCP-1 using neutralizing antibodies inhibits mast cell migration. Low-dose ionizing radiation inhibits mast cell migration through the regulation production of MCP-1 by Nr4a2 in the activated mast cell system.
- | Journal: The Phenylethanol Glycoside Liposome Inhibits PDGF-Induced HSC Activation via Regulation of the FAK/PI3K/Akt Signaling Pathway. (Pubmed Central) - Feb 1, 2020
Moreover, 29.45 μg/mL of CPhG liposomes could decrease the expression of the FAK protein and the phosphorylated PI3K and Akt protein downstream of FAK by overexpression of the FAK gene. This experiment suggests that CPhG liposomes may inhibit the activation of HSCs by inhibiting FAK and then reducing the expression of phosphorylated Akt/PI3K, thereby providing new insights into the application of CPhGs for liver fibrosis.
- || Review, Journal: PI3K inhibitors in thrombosis and cardiovascular disease. (Pubmed Central) - Feb 1, 2020
This review will discuss the PI3K enzymes and their roles in cardiovascular physiology and disease, with a particular focus on platelet function and thrombosis. The current progress and future potential of targeting the PI3K enzymes for therapeutic benefit in cardiovascular disease will be considered, while the challenges of developing drugs against these master cellular regulators will be discussed.
- | Journal: HIV-1 mediated suppression of IFN-α production is associated with inhibition of IRF-7 translocation and PI3K/akt pathway in Plasmacytoid Dendritic cells. (Pubmed Central) - Jan 30, 2020
The findings suggest that HIV-1 may alter AKT phosphorylation to inhibit translocation of IRF-7 into pDC nucleus, leading to IFN-α suppression and this may be the reason for IFN-α abrogation observed in recently infected HIV patients. Understanding of interactions between HIV-1 and signaling pathways leading to IFN-α secretion may provide targets for immune intervention.
- | MK-2206 / Merck (MSD), quercetin (LY294002) / Eli Lilly
Journal: Effect of PI3K/Akt Signaling Pathway on PRAS40Thr246 Phosphorylation in Gastric Cancer Cells. (Pubmed Central) - Jan 30, 2020
The levels of PI3K/Akt signaling pathway related proteins and p-PRAS40Thr246 were significantly increased in gastric cancer cells. p-PRAS40-Thr246 was able to reflect the activation of the PI3K/Akt signaling pathway, reflecting the sensitivity of the PI3K/AKT signaling pathway to inhibitors.
- | Istodax (romidepsin) / Astellas, BMS
Journal: EGFR-vIII downregulated H2AZK4/7AC though the PI3K/AKT-HDAC2 axis to regulate cell cycle progression. (Pubmed Central) - Jan 30, 2020
EGFR-vIII mutation downregulates H2AZK4/7AC and H3K27AC, inhibiting USP11 expression though the PI3K/AKT-HDAC1/2 axis. FK228 is an effective and promising treatment for GBM with EGFR-vIII mutation.
- Dissecting PI3K/AKT/mTOR pathway in mTNBC (Berlin hall) - Jan 30, 2020 - Abstract #ESMOBC2020ESMO_BC_62;
- PI3K alterations as a mechanism of escape (Berlin hall) - Jan 30, 2020 - Abstract #ESMOBC2020ESMO_BC_14;
- || Aditi, my kids are seriously slacking in the PI3K department! I need to get them up to speed! (Twitter) - Jan 30, 2020
- | quercetin (LY294002) / Eli Lilly
Preclinical, Journal: 2,5-hexanedione Mediates Neuronal Apoptosis Through Suppression of NGF via PI3K/Akt Signaling in the Rat Sciatic Nerve. (Pubmed Central) - Jan 29, 2020
However, LY294002 blocked these effects of NGF. Collectively, our results demonstrate that mitochondrial-dependent apoptosis is induced by HD through NGF suppression via the PI3K/Akt pathway both in vivo and in vitro.
- | Sprycel (dasatinib) / BMS, Otsuka, Inhibikase
Journal: Dasatinib inhibition of cSRC prevents the migration and metastasis of canine mammary cancer cells with enhanced Wnt and HER signaling. (Pubmed Central) - Jan 29, 2020
However, inhibition of cSRC resulted in a strong inhibition of Wnt activity and cell migration and metastasis. Further studies are needed to unravel the mechanism of cSRC activation and cSRC inhibition to restore sensitivity to HER-inhibitors in HER2/3-positive breast cancer.
- | chloroquine phosphate / Generic mfg.
Journal, Combination therapy: Combination Therapy with a PI3K/mTOR Dual Inhibitor and Chloroquine Enhances Synergistic Apoptotic Cell Death in Epstein-Barr Virus-Infected Gastric Cancer Cells. (Pubmed Central) - Jan 29, 2020
The combination of CMG002 plus CQ synergistically increased apoptotic cell death in EBV-infected GC cell lines when compared with CMG002 alone ( P < 0.05). Our results suggest that the new PI3K/mTOR dual inhibitor, CMG002, when used in combination with the autophagy inhibitor, CQ, provides enhanced therapeutic efficacy against EBVaGC.
- | Journal: Limonin provokes hepatocellular carcinoma cells with stemness entry into cycle via activating PI3K/Akt signaling. (Pubmed Central) - Jan 29, 2020
qRT-PCR and western blot obtained the consistent results. Overall, these data suggest that limonin attenuates the stemness of HCC cells by reducing cellular quiescence through activating PI3K/Akt signaling.
- | Journal: Vanillic acid attenuates cartilage degeneration by regulating the MAPK and PI3K/AKT/NF-κB pathways. (Pubmed Central) - Jan 29, 2020
In vivo, VA alleviated osteoarthritis progression in a rat OA model. Collectively, our results demonstrate that VA could potentially be a new candidate for OA therapy.
- | Preclinical, Journal: Antidiabetic effects of pterostilbene through PI3K/Akt signal pathway in high fat diet and STZ-induced diabetic rats. (Pubmed Central) - Jan 29, 2020
Furthermore, PTE treatment significantly increased the protein expression of PPARγ, PI3K, p-Akt, GLUT4 and IRS-1 in adipose tissues of diabetic rats. This study suggests that PTE can exert antidiabetic effects via the PI3K/Akt signaling pathway.
- | Journal: Post-surgical inhibition of phosphatidylinositol 3-kinase attenuates the plantar incision-induced postoperative pain behavior via spinal Akt activation in male mice. (Pubmed Central) - Jan 29, 2020
We concluded that post-surgical inhibition of PI3K could attenuate the pain-related behaviors induced by plantar incision, by suppressing the activation of spinal Akt in male mice. This finding might be used in clinical studies to reach a better understanding of POP mechanisms and optimal treatment.
- | JQ-1 / Roche
Journal: BET Inhibition-Induced GSK3β Feedback Enhances Lymphoma Vulnerability to PI3K Inhibitors. (Pubmed Central) - Jan 29, 2020
In a mouse xenograft DLBCL model, BETi decrease MYC, UBE2C, and UBE2T and increase phospho-GSK3β S9 levels, enhancing the anti-proliferative effect of PI3K inhibitors. Our study reveals prosurvival feedbacks induced by BETi involving GSK3β regulation, providing a mechanistic rationale for combination strategies.
- | Preclinical, Journal: Extracellular glucose-dependent IPSC enhancement by leptin in fast-spiking to pyramidal neuron connections via JAK2-PI3K pathway in the rat insular cortex. (Pubmed Central) - Jan 29, 2020
However, leptin enhanced uIPSCs under application of low glucose with an AMPK inhibitor. These results suggest that leptin suppresses IC excitation by facilitating GABA release in FSN→PN connections, which may not occur under a hunger state.
- | Journal: Chlorogenic acid inhibits proliferation and induces apoptosis in A498 human kidney cancer cells via inactivating PI3K/Akt/mTOR signalling pathway. (Pubmed Central) - Jan 28, 2020
Our research firstly reports the efficacy of CA against RCC cells and elucidates the underlying molecular mechanisms. These findings indicate that CA is a potential agent for treating RCC.
- | Journal: Hyperosmotic stress induces unconventional autophagy independent of the Ulk1 complex. (Pubmed Central) - Jan 28, 2020
Finally, autophagy proceeded even in MEFs deficient in FIP200 or Atg13, which are components of the Ulk1 complex. These data suggest that hyperosmotic stress-induced autophagy represents an unconventional type of autophagy that bypasses Ulk1 signaling.
- | Journal: Atractylenolide III Attenuates Muscle Wasting in Chronic Kidney Disease via the Oxidative Stress-Mediated PI3K/AKT/mTOR Pathway. (Pubmed Central) - Jan 28, 2020
To further reveal the relevant mechanism, the oxidative stress-mediated PI3K/AKT/mTOR pathway was assessed, which showed that a reduced expression of p-PI3K, p-AKT, and p-mTOR in C2C12 myoblast atrophy induced by TNF-α could be upregulated by ATL-III; however, after the overexpression of Nox2 to increase ROS production, the attenuated effect was reversed. Our findings indicated that ATL-III is a potentially protective drug against muscle wasting via activation of the oxidative stress-mediated PI3K/AKT/mTOR pathway.
- | Preclinical, Journal: The protective effect of ligustrazine on rats with cerebral ischemia-reperfusion injury via activating PI3K/Akt pathway. (Pubmed Central) - Jan 28, 2020
Ligustrazine also improved the damage of rat brain tissue caused by I/R, but wortmannin reversed the improvement. Ligustrazine plays a neuroprotective role in rats with cerebral I/R injury through the activation of PI3K/Akt pathway.
- | simvastatin / Generic mfg.
Journal: EGFR-targeted immunoliposomes as a selective delivery system of simvastatin, with potential use in treatment of triple-negative breast cancers. (Pubmed Central) - Jan 28, 2020
However, the results were not statistically significant. The experiments described above allowed us to test the possibility of using immunoliposomes as simvastatin carriers delivering increased amounts of the drug to tumour cells.
- | Journal: Perilla oil regulates intestinal microbiota and alleviates insulin resistance through the PI3K/AKT signaling pathway in type-2 diabetic KKAy mice. (Pubmed Central) - Jan 28, 2020
Additionally, PerO treatment distinctly decreased the abundance of Aerococcus and facilitated the richness of Alloprevotella in the intestine, as well as accelerated the restoration of the gut microflora diversity. Thus, PerO regulates intestinal microbiota and alleviates insulin resistance through the PI3K/AKT signaling pathway in type-2 diabetic KKAy mice and may be a potential functional food for diabetic treatment.
- | quercetin (LY294002) / Eli Lilly
Journal: Protective effects and mechanisms of Xingnaojing Injection on early global brain ischemic-induced deep coma in rats (Pubmed Central) - Jan 28, 2020
Xingnaojing Injection could significantly improve deep coma induced by global brain ischemia in rat, which is related to inducing PI3K/Akt-dependent protein phosphorylation of CREB, and reducing hippocampal damage. The protective effect of Xingnaojing Injection is synergistically enhanced by naloxone.
- || Clinical, Journal: A Discovery of Clinically Approved Formula FBRP for Repositioning to Treat HCC by Inhibiting PI3K/AKT/NF-κB Activation. (Pubmed Central) - Jan 28, 2020
Co-treatment of FBRP with PI3K inhibitor exhibited an additive inhibitory effect on PI3K/AKT/NF-κB activation. Collectively, our data showed the potentials of FBRP in hepatic fibrosis microenvironment regulation and tumor prevention, suggesting that FBRP may be a promising candidate drug for reduction of fibrogenesis and prevention of HCC.
- | sirolimus / Generic mfg.
Preclinical, Journal: The ginsenoside Rk3 exerts anti-esophageal cancer activity in vitro and in vivo by mediating apoptosis and autophagy through regulation of the PI3K/Akt/mTOR pathway. (Pubmed Central) - Jan 27, 2020
In conclusion, the present study is the first to clarify that Rk3 can inhibit Eca109 and KYSE150 cell proliferation through activating apoptosis and autophagy by blocking the PI3K/Akt/mTOR pathway, suggesting that Rk3 may be a promising antitumor agent for esophageal cancer. In addition, this study provides ideas and an experimental basis for further research on the anti-esophageal cancer effects of the ginsenoside Rk3 and its mechanism.
- || Clinical, Journal: PTPN1 promotes the progression of glioma by activating the MAPK/ERK and PI3K/AKT pathways and is associated with poor patient survival. (Pubmed Central) - Jan 27, 2020
In conclusion, it was demonstrated that PTPN1 is upregulated in glioma tissue and the overexpression of PTPN1 predicted the poor prognosis of patients with glioma. PTPN1 promotes the progression of glioma by activating the MAPK/ERK and PI3K/AKT pathways.
- | Journal: Epithelial membrane protein 1 promotes glioblastoma progression through the PI3K/AKT/mTOR signaling pathway. (Pubmed Central) - Jan 27, 2020
Finally, it was demonstrated, using an intracranial GBM animal model, that EMP1 knockdown significantly inhibits tumor growth in vivo and increases overall survival in tumor‑bearing animals. Our research provides new insights into the molecular mechanisms underlying EMP1 knockdown‑mediated inhibition of GBM cell invasion and raises the possibility that targeting of EMP1 may represent a promising strategy for the treatment of GBM.