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67 Companies | 59 Products |
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344 Diseases | |
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- | Biomarker, Journal: A Genome-Wide Screen for Wortmannin-Resistant Mutants in Schizosaccharomyces pombe: The Phosphorylation-Impaired Mutants Are Resistant to Signaling Defect. (Pubmed Central) - Dec 29, 2019
In addition, when we examined the pathways in which these 52 genes function, we determined that 9 genes were related to phosphorylation process. These results might provide new insights for better understanding of certain human diseases.
- | netupitant (Ro 67-3189) / Helsinn, Otsuka
Journal: Intracellular emetic signaling cascades by which the selective neurokinin type 1 receptor (NKR) agonist GR73632 evokes vomiting in the least shrew (Cryptotis parva). (Pubmed Central) - Dec 28, 2019
In addition, evoked ERK1/2 phosphorylation was sensitive to inhibitors of PKC and PI3K. These findings indicate that the LTCC/IPR-dependent PI3K/PKCα/βII-ERK1/2 signaling pathways are involved in NKR-mediated vomiting.
- | fasudil / Generic mfg., fenoterol / Generic mfg.
Journal: Regulation of the β-adrenergic receptor signaling pathway in sustained ligand-activated preconditioning. (Pubmed Central) - Dec 28, 2019
Here, we tested for induction of a protective β-AR/Gα/PKA signaling axis with SLP to ascertain whether signaling changes were PI3K-dependent (by sustained cotreatment with wortmannin), and whether the downstream PKA target Rho kinase (ROCK) participates in subsequent cardioprotection (by acute treatment with fasudil)...Nonetheless, functional sensitivities of β-ARs and adenylyl cyclase were unchanged based on concentration-response analyses for formoterol, fenoterol, and 6-[3-(dimethylamino)propionyl]-forskolin...While Akt phosphorylation was evident, PI3K activity appears non-essential to OR up-regulation of the β2-AR signal axis. This opioidergic remodeling of β2-AR signaling may explain β2-AR, Gαs and PKA dependence of SLP protection.
- | Keytruda (pembrolizumab) / Merck (MSD), Tecentriq (atezolizumab) / Roche
Journal, BRCA Biomarker, PARP Biomarker, PD(L)-1 Biomarker, IO Biomarker: Translational Highlights in Breast and Ovarian Cancer 2019 - Immunotherapy, DNA Repair, PI3K Inhibition and CDK4/6 Therapy. (Pubmed Central) - Dec 27, 2019
No association between efficacy and PD-L1 expression was found in a neoadjuvant study that included pembrolizumab in TNBC...Both the accumulation of PI3K mutations and also PTEN changes might play a part in planning subsequent therapies. This review article summarises these recent developments in breast cancer and in part also in ovarian cancer.
- | quercetin (LY294002) / Eli Lilly
Journal: Silencing of Long Non-coding RNA RP1-93H18.6 Acts as a Tumor Suppressor in Cervical Cancer through the Blockade of the PI3K/Akt Axis. (Pubmed Central) - Dec 27, 2019
The siRNA against RP1-93H18.6 or LY294002 exposure was observed to attenuate the effects induced by RP1-93H18.6 vectors. This study suggests that suppression of lncRNA RP1-93H18.6 exerts potent inhibitory effects on the development and progression of CC via blockade of the PI3K/Akt axis.
- | Zydelig (idelalisib) / Gilead
Journal: PI3Kδ inhibitors for the treatment of cancer: a patent review (2015-present). (Pubmed Central) - Dec 26, 2019
Moreover, there are still multiple small molecule selective PI3Kδ inhibitors at different stages of development. The research effort for development of PI3Kδ inhibitors is to manage the toxicity and lower side-effects.
- | Biomarker, Preclinical, Journal: Cinnamaldehyde ameliorates STZ-induced rat diabetes through modulation of IRS1/PI3K/AKT2 pathway and AGEs/RAGE interaction. (Pubmed Central) - Dec 26, 2019
Additionally, significant elevation in mRNA expression of insulin receptor substrate1 (IRS1), phosphatidylinositol 3-kinase regulatory subunit1 (PI3K-P85 subunit), and AKT serine/threonine kinase2 (AKT2); increased levels of P-AKT ser and aortic eNOS; and decrease in mRNA expression of NOX4 were detected in CIN-treated group when compared to diabetic group. This study suggests antidiabetic and antioxidant effects of CIN probably through upregulation of eNOS and IRS1/PI3K/AKT2 signaling pathway and alleviating AGEs, RAGE, and NOX4 elevation.
- | quercetin (LY294002) / Eli Lilly
Journal: ANXA4 promotes trophoblast invasion via the PI3K/AKT/eNOS pathway in preeclampsia. (Pubmed Central) - Dec 26, 2019
Our findings demonstrate that ANXA4 expression is downregulated in PE. ANXA4 may promote trophoblast invasion via the PI3K/AKT/eNOS pathway.
- | Journal: lncRNA GAS5 Restrains CCl-Induced Hepatic Fibrosis by Targeting miR-23a through the PTEN/PI3K/Akt Signaling Pathway. (Pubmed Central) - Dec 26, 2019
lncRNA GAS5 can be used as a sponge platform for miR-23a, to competitively decrease miR-23a expression levels. We revealed the role of the lncRNA GAS5/miR-23a/PTEN/PI3K/Akt/mTOR/Snail signaling pathway in hepatic fibrosis, providing molecular targets for the treatment of hepatic fibrosis.
- | Journal: Ascl1 Regulates Electric Field-Induced Neuronal Differentiation through PI3K/Akt Pathway. (Pubmed Central) - Dec 26, 2019
Moreover, we identified that the expression of Ascl1 positively regulated neuronal differentiation of NPCs and can be up-regulated by EF-stimulation through the activation of PI3K/Akt pathway. Therefore, this study provides new insights into the role of Ascl1 and its relevant PI3K/Akt pathway in regulating of EF-induced neuronal differentiation and pointed out that continuously express of Ascl1 in NPCs is required for EF-induced neuronal differentiation.
- | quercetin (LY294002) / Eli Lilly
Biomarker, Journal: Nobiletin ameliorates myocardial ischemia and reperfusion injury by attenuating endoplasmic reticulum stress-associated apoptosis through regulation of the PI3K/AKT signal pathway. (Pubmed Central) - Dec 26, 2019
Therefore, this study provides new insights into the role of Ascl1 and its relevant PI3K/Akt pathway in regulating of EF-induced neuronal differentiation and pointed out that continuously express of Ascl1 in NPCs is required for EF-induced neuronal differentiation. Nobiletin pre-treatment may alleviate MIRI probably via the attenuation of PI3K/AKT-mediated ERS-related myocardial apoptosis.
- | Journal: MicroRNA-183 affects the development of gastric cancer by regulating autophagy via MALAT1-miR-183-SIRT1 axis and PI3K/AKT/mTOR signals. (Pubmed Central) - Dec 26, 2019
MALAT1-miR-183-SIRT1 axis and PI3K/AKT/mTOR pathway may be mechanisms to mediate autophagy in GC. miR-183 may serve as a towardly therapeutic target for GC.
- || Aliqopa (copanlisib) / Bayer
Trial completion date: CHRONOS-1: Open-label, Uncontrolled Phase II Trial of Intravenous PI3K Inhibitor BAY80-6946 in Patients With Relapsed, Indolent or Aggressive Non-Hodgkin's Lymphomas (clinicaltrials.gov) - Dec 26, 2019
P2, N=227, Active, not recruiting, Sponsor: Bayer
miR-183 may serve as a towardly therapeutic target for GC. Trial completion date: Mar 2020 --> Mar 2021
- || leniolisib (CDZ173) / Pharming Group
Clinical, Journal: F-NMR based determination of the absorption, metabolism and excretion of the oral phosphatidylinositol-3-kinase (PI3K) delta inhibitor leniolisib (CDZ173) in healthy volunteers. (Pubmed Central) - Dec 25, 2019
No metabolites were abundant in plasma relative to the parent drug. An average mass balance of 66% was obtained, demonstrating that relatively extensive elimination/excretion data can be obtained by F-NMR in a first in human clinical study without use of a radiolabeled drug.
- | quercetin (LY294002) / Eli Lilly
Preclinical, Journal: Magnesium lithospermate B ameliorates microcirculation perfusion in rats by promoting vascular NO production via activating the PI3K/AKT pathway. (Pubmed Central) - Dec 25, 2019
Co-administration of the eNOS inhibitor L-NAME (20 mg/kg) abolished the protective effects of MLB against dextran-induced microcirculation dysfunction in rats, whereas pretreatment with PI3K inhibitor LY294002 (10 μM) prevented eNOS activation in MLB-treated HMEC-1 cells. Our results suggest that MLB can restore the microcirculation dysfunction via activating eNOS, and in turn enhancing the vascular nitric oxide production, which is medicated by MLB-caused activation of the PI3K/AKT pathway.
- || parsaclisib (INCB50465) / Incyte, Rituxan (rituximab) / Biogen, Zenyaku Kogyo, Roche
Clinical, Journal: Parsaclisib, a potent and highly selective PI3Kδ inhibitor, in patients with relapsed or refractory B-cell malignancies. (Pubmed Central) - Dec 25, 2019
P1/2
Phase 2 studies in relapsed or refractory B-cell NHL subtypes are ongoing. This trial was registered at www.clinicaltrials.gov as #NCT02018861.
- | Botox (onabotulinumtoxin A) / GSK, Allergan
Journal: Botulinum toxin type A prevents the phenotypic transformation of fibroblasts induced by TGF‑β1 via the PTEN/PI3K/Akt signaling pathway. (Pubmed Central) - Dec 25, 2019
On the whole, the findings of this study indicate that BTXA may inhibit fibroblast phenotypic transformation by regulating PTEN methylation and the phosphorylation of related pathways. The findings of this study can provide a theoretical basis for HS treatment.
- | quercetin (LY294002) / Eli Lilly
Preclinical, Journal: CDCA2 promotes the proliferation of colorectal cancer cells by activating the AKT/CCND1 pathway in vitro and in vivo. (Pubmed Central) - Dec 25, 2019
The findings of this study can provide a theoretical basis for HS treatment. This study demonstrates that overexpression of CDCA2 might target CCND1 to promote CRC cell proliferation and tumorigenesis through activation of the PI3K/AKT pathway.
- | Journal: Salvianolic acid A attenuates CCl-induced liver fibrosis by regulating the PI3K/AKT/mTOR, Bcl-2/Bax and caspase-3/cleaved caspase-3 signaling pathways. (Pubmed Central) - Dec 25, 2019
Mechanistically, the PI3K/AKT/mTOR signaling cascade was inhibited by SA-A to prevent the stimulation of hepatic stellate cell, as well as the synthesis of extracellular matrix, and regulated Bcl-2/Bax and caspase-3/cleaved caspase-3 signaling pathways to prevent hepatocyte apoptosis. The novel findings of this study suggested that SA-A could reduce liver fibrosis and the molecular mechanisms behind it are closely associated with the regulation of PI3K/AKT/mTOR, Bcl-2/Bax and caspase-3/cleaved caspase-3 signaling pathways.
- | Journal: Furosine Posed Toxic Effects on Primary Sertoli Cells through Regulating Cep55/NF-κB/PI3K/Akt/FOX01/TNF-α Pathway. (Pubmed Central) - Dec 25, 2019
Phosphatidylethanolamine (PE) (18:0/16:1) was upregulated by furosine both in mice testicle tissue and in primary sertoli cells, meanwhile, PE(18:0/16:1) was proved to activate Cep55/NF-κB/PI3K/Akt/FOX01/TNF-α pathway, and as a functional protein in dairy products, lactoferrin could inhibit expression of this pathway when combined with furosine. In conclusion, for the first time we validated that furosine posed toxic effects on mice sperms and testicle tissue through upregulating PE(18:0/16:1) and activating Cep55/NF-κB/PI3K/Akt/FOX01/TNF-α pathway.
- | chloroquine phosphate / Generic mfg., quercetin (LY294002) / Eli Lilly
Journal: Tetramethylprazine attenuates myocardial ischemia/reperfusion injury through modulation of autophagy. (Pubmed Central) - Dec 25, 2019
Additionally, the effects of TMP on the modulation of autophagy were inhibited by LY294002 (a PI3K inhibitor) in H/R cardiomyocytes. Our findings suggested TMP exerted cardioprotection against MI/R injury by decreasing Beclin-1 associated autophagy dysfunction through PI3K pathway.
- | Journal, Cancer stem cells: Gigantol Targets Cancer Stem Cells and Destabilizes Tumors via the Suppression of the PI3K/AKT and JAK/STAT Pathways in Ectopic Lung Cancer Xenografts. (Pubmed Central) - Dec 25, 2019
This study reveals novel insights into the anti-tumor mechanisms of gigantol focused on CSC targeting and destabilizing tumor integrity via suppression of the PI3K/AKT/mTOR and JAK/STAT pathways. This data supports the potential of gigantol to be further developed as a drug for lung cancer.
- The role of ROS levels on the activation of SMAD2 by TGFβ1 in corneal fibroblasts () - Dec 24, 2019 - Abstract #EVER2019EVER_432;
The inhibitory effect of some signal transduction pathways may occur indirectly through their effect of the redox cellular status. Inflammations or infections that increases ROS may delay the wound healing response.
- | quercetin (LY294002) / Eli Lilly
Preclinical, Journal: The bone marrow mononuclear cells reduce the oxidative stress of cerebral infarction through PI3K/AKT/NRF2 signaling pathway. (Pubmed Central) - Dec 24, 2019
Inflammations or infections that increases ROS may delay the wound healing response. BMMNCs can reduce the oxidative stress, apoptosis, and inflammatory reaction through PI3K/AKT/NRF2 signaling pathway, thus promoting the secretion of nerve and vascular cytokines, improving the neurological function and reducing the infarct scope.
- || samotolisib (LY3023414) / Eli Lilly
Clinical, P1 data, Journal: A First-in-Human Phase 1 Study of LY3023414, an Oral PI3K/mTOR Dual Inhibitor, in Patients with Advanced Cancer. (Pubmed Central) - Dec 24, 2019
Durable partial response was observed in an endometrial cancer patient harboring PIK3R1 and PTEN truncating mutations and 13 additional patients (28%) had decrease in their target lesions by up to 30%. LY3023414 has a tolerable safety profile and single agent activity in patients with advanced cancers. The RP2D of LY3023414 monotherapy is 200 mg BID based on safety, tolerability, and PK/Pharmacodynamic data.
- || parsaclisib (INCB50465) / Incyte
Enrollment closed: A Study of INCB050465 in Subjects With Relapsed or Refractory Marginal Zone Lymphoma (CITADEL-204) (clinicaltrials.gov) - Dec 23, 2019
P2, N=109, Active, not recruiting, Sponsor: Incyte Corporation
The RP2D of LY3023414 monotherapy is 200 mg BID based on safety, tolerability, and PK/Pharmacodynamic data. Recruiting --> Active, not recruiting
- | Legalon (silibinin) / Mylan, fluorouracil / Generic mfg.
Journal, Cancer stem cells, PARP Biomarker: Silibinin, A Natural Blend In Polytherapy Formulation For Targeting Cd44v6 Expressing Colon Cancer Stem Cells. (Pubmed Central) - Dec 23, 2019
Importantly, 5FU+ Silibinin could inhibit PI3K/MAPK dual activation and arrest the cell cycle at G0/G1 phase. Thus, our study suggests that inhibition of CD44v6 attenuates stemness of colon cancer stem cells and holds a prospect of potent therapeutic target.
- | Journal: Annexin A1-suppressed autophagy promotes nasopharyngeal carcinoma cell invasion and metastasis by PI3K/AKT signaling activation. (Pubmed Central) - Dec 23, 2019
Lastly, we showed that inhibition of autophagy restored the ability of tumor cell migration and invasion, epithelial-mesenchymal transition (EMT)-like alterations and in vivo metastasis in the ANXA1 knockdown NPC cells with autophagy activation; ANXA1-suppresed autophagy induced EMT-like alterations possibly by inhibiting autophagy-mediated degradation of Snail. Our data suggest that ANXA1-suppressed autophagy promotes NPC cell migration, invasion and metastasis by activating PI3K/AKT signaling pathway, highlighting that the activation of autophagy may inhibit metastasis of NPC with high ANXA1 expression.
- | Journal: Down-regulation of LncRNA NR027113 inhibits cell proliferation and metastasis via PTEN/PI3K/AKT signaling pathway in hepatocellular carcinoma. (Pubmed Central) - Dec 23, 2019
Our data suggest that ANXA1-suppressed autophagy promotes NPC cell migration, invasion and metastasis by activating PI3K/AKT signaling pathway, highlighting that the activation of autophagy may inhibit metastasis of NPC with high ANXA1 expression. A brand new lncRNA NR027113 was found, which can promote the proliferation, invasion and metastasis of HCC via the PTEN/PI3K/AKT signaling pathway, and may be a potential therapeutic target in the future treatment of HCC.
- | Talzenna (talazoparib) / Pfizer, Mektovi (binimetinib) / Ono Pharma, Pierre Fabre, Pfizer
Journal, PARP Biomarker: Integrated Genomic, Epigenomic, and Expression Analyses of Ovarian Cancer Cell Lines. (Pubmed Central) - Dec 23, 2019
Genome-wide rearrangements provided an improved measure of sensitivity to PARP inhibition. This study provides a comprehensive and broadly accessible resource of molecular information for the development of therapeutic avenues in ovarian cancer.
- | quercetin (LY294002) / Eli Lilly, PD98059 / Wayne State University
Journal, IO Biomarker: Pretreatment with Total Flavonoid Extract from Dracocephalum Moldavica L. Attenuates Ischemia Reperfusion-induced Apoptosis. (Pubmed Central) - Dec 23, 2019
TFDM cardio-protection was influenced by LY294002 (PI3K inhibitor) and PD98059 (ERK1/2 inhibitor). Taken together, these results provide convincing evidence of the benefit of TFDM pretreatment due to inhibited myocardial apoptosis as mediated by the PI3K/Akt/GSK-3β and ERK1/2 signaling pathways.
- | Journal, IO biomarker: IDO1 and kynurenine pathway metabolites activate PI3K-Akt signaling in the neoplastic colon epithelium to promote cancer cell proliferation and inhibit apoptosis. (Pubmed Central) - Dec 23, 2019
Together, these data define a novel cell-autonomous function and mechanism by which IDO1 activity promotes CRC progression. These findings may have implications for the rational design of new clinical trials which exploit a synergy of IDO1 inhibitors with conventional cancer therapies for which Akt activation provides resistance such as radiation.
- || Zydelig (idelalisib) / Gilead, Copiktra (duvelisib) / Verastem
Biomarker, Clinical, PK/PD data, Journal: Characterizing Pharmacokinetic-Pharmacodynamic Relationships and Efficacy of PI3Kδ-inhibitors in Respiratory Models of TH2 and TH1 Inflammation. (Pubmed Central) - Dec 23, 2019
Additional studies in an A. alternata rat model, a sheep Ascaris-sensitive sheep model and a TH1 driven rat ozone exposure model did not challenge our hypothesis, suggesting that an IC50 level of TE sustained for 24 hours is required to produce efficacy in these traditional models. We conclude that the PK/PD observations in our animal models appear to align with clinical results associated with a TH2 airway disease.
- | fasudil / Generic mfg.
Journal: Rho-kinase is a negative regulator of red blood cell eNOS under basal conditions. (Pubmed Central) - Dec 23, 2019
The mechanism we described here gives first evidences about Rho-kinase mediated eNOS regulation in RBC under basal conditions. This pathway could also be more important under disease states.
- | Torin1 / InvivoGen
Journal: FAM83D inhibits autophagy and promotes proliferation and invasion of ovarian cancer cells via PI3K/AKT/mTOR pathway. (Pubmed Central) - Dec 23, 2019
Mechanistically, overexpression of FAM83D activated the PI3K/AKT/mTOR pathway, and Torin1 could suppress FAM83D-induced cell proliferation and invasion...Overall, FAM83D promoted ovarian cancer cell invasion and proliferation, while inhibited autophagy via the PI3K/AKT/mTOR signaling pathway. Our results suggest that FAM83D may be a candidate oncogene in ovarian cancer, which provides a fresh perspective of FAM83D in ovarian cancer.
- | paclitaxel / Generic mfg.
Preclinical, Journal: Spinal blockage of CXCL1 and its receptor CXCR2 inhibits paclitaxel-induced peripheral neuropathy in mice. (Pubmed Central) - Dec 23, 2019
Overall, the data indicates that the up-regulation of CXCL1 is important for the development and maintenance of PTX-induced neuropathic pain in mice. Therefore, the spinal blockage of CXCL1/CXCR2 signalling might be a new innovative therapeutic approach to treat this clinical side effect of PTX.
- | Preclinical, Journal: MicroRNA-24 attenuates vascular remodeling in diabetic rats through PI3K/Akt signaling pathway. (Pubmed Central) - Dec 23, 2019
Therefore, the spinal blockage of CXCL1/CXCR2 signalling might be a new innovative therapeutic approach to treat this clinical side effect of PTX. The up-regulation of miR-24 significantly attenuated vascular remodeling both in balloon-injured diabetic rats and HG-stimulated VSMCs via suppression of proliferation, migration and collagen deposition by acting on PIK3R1 gene that modulated the PI3K/Akt/mTOR axes.
- | quercetin (LY294002) / Eli Lilly
Journal, IO Biomarker: Baicalin ameliorates neuroinflammation-induced depressive-like behavior through inhibition of toll-like receptor 4 expression via the PI3K/AKT/FoxO1 pathway. (Pubmed Central) - Dec 23, 2019
The up-regulation of miR-24 significantly attenuated vascular remodeling both in balloon-injured diabetic rats and HG-stimulated VSMCs via suppression of proliferation, migration and collagen deposition by acting on PIK3R1 gene that modulated the PI3K/Akt/mTOR axes. Collectively, these results demonstrate that baicalin ameliorated neuroinflammation-induced depressive-like behaviors through the inhibition of TLR4 expression via the PI3K/AKT/FoxO1 pathway.
- | Preclinical, Journal: MicroRNA-486-5p targeting PTEN Protects Against Coronary Microembolization-Induced Cardiomyocyte Apoptosis in Rats by activating the PI3K/AKT pathway. (Pubmed Central) - Dec 23, 2019
Overexpression of miR-486-5p reduced cardiomyocyte apoptosis and improved cardiac function through inhibition of PTEN and activation of the PI3K/Akt pathway in rat CME models. Overexpression of miR-486-5p, which targets PTEN, protects against CME-induced cardiomyocyte apoptosis and improves cardiac function in rats by activating the PI3K/Akt pathway.
- | quercetin (LY294002) / Eli Lilly
Journal: Colon Cancer Cell Secretes EGF to Promote M2 Polarization of TAM Through EGFR/PI3K/AKT/mTOR Pathway. (Pubmed Central) - Dec 23, 2019
Besides, we established that colon cancer cells exerted their stimulatory effect on M2 polarization of macrophage from monocyte THP-1 using EGFR antibody mAb225 and PI3K inhibitor LY294002. We provide evidence that EGF which are secreted by colon cancer cells play contributory role in M2 polarization of macrophages, which support the notion that tumor environment, including tumor-associated macrophages, can be targeted to develop effective strategies for treating cancer.
- | Copiktra (duvelisib) / Verastem
Journal: Duvelisib: a new phosphoinositide-3-kinase inhibitor in chronic lymphocytic leukemia. (Pubmed Central) - Dec 23, 2019
Nevertheless, the correct management of adverse events, eventually including dose modification, allows patients to remain on treatment. In conclusion, duvelisib represents a promising treatment in chronic lymphocytic leukemia and a salvage therapy after ibrutinib.
- | Decadron (dexamethasone) / Merck (MSD)
Preclinical, Journal: Dexamethasone suppresses osteogenesis of osteoblast via the PI3K/Akt signaling pathway in vitro and in vivo. (Pubmed Central) - Dec 23, 2019
Moreover, downregulation of ALP and OCN expressions by LY294002 can mimic the suppressive effects of Dex. These data together reveal that the suppressed PI3K/Akt pathway is involved in the regulatory action of Dex on osteogenesis.
- | Adomet (S-adenosyl-L-methionine) / Abbott
Review, Journal: Alterations of Methionine Metabolism as Potential Targets for the Prevention and Therapy of Hepatocellular Carcinoma. (Pubmed Central) - Dec 23, 2019
Different alterations of the methionine cycle leading to a decrease of S-adenosylmethionine (SAM) occur in hepatitis, liver steatosis, liver cirrhosis, and HCC...However, although SAM prevents experimental tumors, it is not curative against already established experimental and human HCCs. The recent observation that the inhibition of MAT2A and MAT2B expression by miRNAs leads to a rise of endogenous SAM and strong inhibition of cancer cell growth could open new perspectives to the treatment of HCC.
- | quercetin (LY294002) / Eli Lilly
Preclinical, Journal: Sphingosine-1-Phosphate Improves the Biological Features of Mouse Bone Marrow-Derived EPCs Partially through PI3K/AKT/eNOS/NO Pathway. (Pubmed Central) - Dec 23, 2019
The inhibitor of LY294002 inhibited S1P-stimulated activation of phosphorylated protein kinase B (AKT) (p-AKT) and endothelial nitric oxide synthase (eNOS) (p-eNOS), and down-regulated the level of eNOS significantly. The results suggest that S1P improves the biological features of EPCs partially through PI3K/AKT/eNOS/NO signaling pathway.
- || paclitaxel / Generic mfg.
Clinical, Journal: Inhibition of Phosphatidylinositol 3-kinase (PI3K) Signaling Synergistically Potentiates Antitumor Efficacy of Paclitaxel and Overcomes Paclitaxel-Mediated Resistance in Cervical Cancer. (Pubmed Central) - Dec 23, 2019
In addition, PI3K inhibition also suppressed tumor migration and invasion by targeting β-catenin and matrix metalloproteinase-2/9. The authors suggest that the combination of a PI3K inhibitor with paclitaxel may enhance antitumor activity through a cascade of PI3K signaling events.
- | Journal, IO Biomarker: LY404039 Inhibits Proliferation and Metastasis of Osteosarcoma Cells via PI3K Signaling Pathway. (Pubmed Central) - Dec 23, 2019
Also, the activity of the downstream proteins such as p70S6K and Cyclin D1 were also significantly decreased. LY404039 could inhibit proliferation and metastasis of osteosarcoma cells, which might be attributed to the enhancement of apoptosis via PI3K pathway.
- | Zydelig (idelalisib) / Gilead
Journal: Theoretical studies on the selectivity mechanisms of PI3Kδ inhibition with marketed idelalisib and its derivatives by 3D-QSAR, molecular docking, and molecular dynamics simulation. (Pubmed Central) - Dec 23, 2019
Taken together, the results provided by this study may facilitate the rational design of novel and selective PI3Kδ inhibitors. Graphical abstract .
- | Preclinical, Journal: A preliminary report: genistein attenuates cerebral ischemia injury in ovariectomized rats via regulation of the PI3K-Akt-mTOR pathway. (Pubmed Central) - Dec 23, 2019
And we found that genistein treatment in ovariectomized rats significantly improved neurological outcomes, reduced infarct volumes, decreased neuronal damage and cell apoptosis, and increased the activity of PI3K-Akt-mTOR signal pathway. Our findings indicated that treatment genistein could alleviate neuronal apoptosis induced by cerebral ischemia in ovariectomized rats via promoting the activity of PI3K-Akt-mTOR signal pathway, which provides a new molecular mechanism for the neuroprotective effects of genistein against stroke.
- | Journal: Leptin Modulates the Expression of miRNAs-Targeting POMC mRNA by the JAK2-STAT3 and PI3K-Akt Pathways. (Pubmed Central) - Dec 22, 2019
Importantly, we show that leptin inhibits these miRNAs expression by different transduction pathways. Taken together, these results allowed us to highlight the miRNA involvement in the regulation of POMC expression downstream of the leptin signaling and satiety signal integration.
- | Journal: Knockdown of lncRNA TDRG1 Inhibits Tumorigenesis in Endometrial Carcinoma Through the PI3K/AKT/mTOR Pathway. (Pubmed Central) - Dec 22, 2019
Moreover, TDRG1 silencing decreased the protein levels of p-AKT, p-PI3K, and p-mTOR of EC cells. Our data underlined the implication of TDRG1 in EC progression, proposing that targeting TDRG1 might be a potential therapeutic avenue in EC.