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67 Companies | 59 Products |
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59 Products | |
344 Diseases | |
342 Trials |  |
12240 News |  |
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- | Trintellix (vortioxetine) / Lundbeck, Takeda
Journal: Vortioxetine induces apoptosis and autophagy of gastric cancer AGS cells via the PI3K/AKT pathway. (Pubmed Central) - Nov 25, 2021
Further investigation indicated that vortioxetine regulated apoptosis and autophagy through activation of the PI3K/AKT pathway. Taken together, our data suggest that vortioxetine has cytotoxic effects against GC AGS cells by inhibiting proliferation, invasion and migration, as well as by inducing apoptosis and autophagy through the PI3K/AKT pathway.
- | Journal: Jagged2 progressively increased expression from Stage I to III of Bladder Cancer and Melatonin-mediated downregulation of Notch/Jagged2 suppresses the Bladder Tumorigenesis via inhibiting PI3K/AKT/mTOR/MMPs signaling. (Pubmed Central) - Nov 25, 2021
The cellular (MMPs/Notch/Jagged2) and protein (Notch/Jagged2/PI3K/p-AKT/mTOR/MMPs) exhibited a similar trend, whereas the PTEN protein level exhibited an opposite pattern of PI3K among three groups (all p<0.0001). Notch/Jagged-PI3K/p-AKT/mTOR/MMPs is one essential signaling pathway for BC survival, proliferation and invasion that were remarkably suppressed by Mel treatment.
- | Journal: SHIP2 inhibition alters redox-induced PI3K/AKT and MAP kinase pathways via PTEN over-activation in cervical cancer cells. (Pubmed Central) - Nov 25, 2021
Pharmacological targeting or RNAi-mediated knockdown of PTEN rescue ERK and AKT activation. Using a series of pharmacological and biochemical approaches, I provide evidence that crosstalk between SHIP2 and PTEN occurs upon an increase in oxidative stress to modulate the activity of MAPK and PI3/ATK pathways.
- | Journal: Osteopontin Regulates Endometrial Stromal Cell Migration in Endometriosis through the PI3K Pathway : Osteopontin Regulates Endometrial Cell Migration in Endometriosis. (Pubmed Central) - Nov 25, 2021
Meanwhile, activation of the PI3K pathway promoted the migration ability of ectopic ESCs. OPN may regulate the expression of uPA through the PI3K signal pathway to affect the migration ability of ESCs, indicating that OPN, uPA, and the PI3K pathway may be potential targets for interrupting development of endometriosis.
- || Clinical, Journal: High follicle-stimulating hormone levels accelerate cartilage damage of knee osteoarthritis in postmenopausal women through the PI3K/AKT/NF-κB pathway. (Pubmed Central) - Nov 25, 2021
Moreover, we used Western blotting in ATDC5 cells to demonstrate that FSH decreased type II collagen and increased p-PI3K/PI3K, p-AKT/AKT, p-NFκB/NFκB and p-IKB/IKB in a concentration-dependent manner. Our results suggest that increased FSH levels are associated with KOA for postmenopausal women aged 50-60 and that high FSH levels might damage the cartilage tissues via the PI3K/AKT/NF-κB pathway.
- | Journal: Nesfatin-1 Promotes Proliferation, Migration and Invasion of HTR-8/SVneo Trophoblast Cells and Inhibits Oxidative Stress via Activation of PI3K/AKT/mTOR and AKT/GSK3β Pathway. (Pubmed Central) - Nov 25, 2021
Nesfatin-1 promoted the activation of PI3K/AKT/mTOR or GSK3β pathway, blocking of which reversed the promotive effects on trophoblast invasion and the inhibitory effects on oxidative stress of Nesfatin-1 in HTR-8/SVneo cells. In short, this study revealed that Nesfatin-1 promoted trophoblast cell proliferation, migration, invasion, and EMT and suppressed oxidative stress by activating PI3K/AKT/mTOR and AKT/GSK3β signaling pathway, laying the foundation for the development of therapeutic strategy for PE by targeting Nesfatin-1.
- | medroxyprogesterone / Generic mfg., estradiol valerate / Generic mfg.
Journal, IO biomarker: Zihuai recipe alleviates cyclophosphamide-induced diminished ovarian reserve via suppressing PI3K/AKT-mediated apoptosis. (Pubmed Central) - Nov 25, 2021
ZHR improved the ovarian reserve in CTX-induced DOR rats. The mechanisms of ZHR on DOR may be mediated through the regulation of gonadal hormones of the hypothalamic-pituitary-ovarian axis (HPOA), and the inhibition of PI3K/AKT-mediated apoptosis in granulosa cells.
- | everolimus / Generic mfg., gemcitabine / Generic mfg.
Journal, IO biomarker: Everolimus regulates the activity of gemcitabine-resistant pancreatic cancer cells by targeting the Warburg effect via PI3K/AKT/mTOR signaling. (Pubmed Central) - Nov 25, 2021
The mechanisms of ZHR on DOR may be mediated through the regulation of gonadal hormones of the hypothalamic-pituitary-ovarian axis (HPOA), and the inhibition of PI3K/AKT-mediated apoptosis in granulosa cells. Evr treatment may be a promising strategy to target the growth and activity of GEM-resistant pancreatic cancer cells by regulating glucose metabolism via inactivation of PI3K/AKT/mTOR signaling.
- | Kengreal (cangrelor) / Chiesi
Journal: Ginsenosides Rb2 and Rd2 isolated from Panax notoginseng flowers attenuate platelet function through P2Y-mediated cAMP/PKA and PI3K/Akt/Erk1/2 signaling. (Pubmed Central) - Nov 25, 2021
Co-incubation of the P2Y12 antagonist cangrelor with either G-Rb2 or G-Rd2 did not show significant additive inhibitory effects...Interestingly, G-Rd2 generally exhibited more potent inhibitory effects on platelet function and thrombus formation than G-Rb2. Thus, our data suggest that PNF-derived G-Rb2 and G-Rd2 effectively attenuate platelet hyperactivity through modulating signaling pathways downstream of P2Y12, which indicates G-Rb2 and G-Rd2 may play important preventive roles in thrombotic diseases.
- | Preclinical, Journal: Anemarrhena Saponins Attenuate Insulin Resistance in Rats with High-Fat Diet-Induced Obesity via the IRS-1/PI3K/AKT Pathway. (Pubmed Central) - Nov 25, 2021
Thus, our data suggest that PNF-derived G-Rb2 and G-Rd2 effectively attenuate platelet hyperactivity through modulating signaling pathways downstream of P2Y12, which indicates G-Rb2 and G-Rd2 may play important preventive roles in thrombotic diseases. These findings suggest that anemarrhena saponins could promote insulin signal transduction through the IRS-1/PI3K/AKT pathway, thereby reducing the damage caused by insulin resistance.
- | Preclinical, Journal: IGF-1 activates the PI3K pathway through S1P/S1PR1 signaling to promote the migration of mouse alveolar epithelial cells (Pubmed Central) - Nov 24, 2021
When S1PR1 in AECs was blocked or interfered, the effect of IGF-1 on accelerating AEC migration and promoting AEC p-Akt expression was partially reduced. Conclusion IGF-1 activates the PI3K pathway through S1P-S1PR1 signal to promote the migration of AECs.
- | Journal: CircMYOF triggers progression and facilitates glycolysis via the VEGFA/PI3K/AKT axis by absorbing miR-4739 in pancreatic ductal adenocarcinoma. (Pubmed Central) - Nov 24, 2021
Mechanistically, RNA pull-down and luciferase reporter experiments elucidated that circMYOF, as a competing endogenous RNA for miR-4739, facilitated glycolysis via the VEGFA/PI3K/AKT pathway. Taken together, our findings indicate that circMYOF may work as a desirable biomarker and therapeutic target for PDA patients.
- Copiktra (duvelisib) / Secura Bio, Yakult Honsha
PI3K δ /γ Inhibition Enhances the Expansion and Anti-Tumor Cytotoxicity of CART Cells for CLL Patients () - Nov 24, 2021 - Abstract #ASH2021ASH_6662;
T cells were negatively selected using MACS beads and transduced with CD19 CAR lentivirus (encoding CD28 or 41BB co-stimulatory domains) and stimulated with anti-CD3/CD28 beads in media containing 30 U/mL interleukin-2 with or without the PI3Kδ/γ inhibitor duvelisib (Duv) for 15 days... Inhibition of PI3Kd/g during CART cell culture decreased the expression of immune checkpoint molecules and enhanced in vivo expansion leading to greater efficacy in eliminating CLL.
- ipatasertib (GDC-0068) / Roche, GSK2334470 / GSK, Zydelig (idelalisib) / Gilead
PI3K/AKT Activation Mediates B-Cell Transformation By the "T" Splice-Variant of Fyn Kinase () - Nov 24, 2021 - Abstract #ASH2021ASH_6521;
These results suggest that AKT, PI3K, and PDK1 are important targets downstream of FYN, and that the PI3K/AKT pathway is the key survival mechanism in lymphomagenesis mediated by FYN. We show that WT and activating mutants of the FYN T spliceoform specifically, but not FYN B, induce drug-sensitive B lymphocyte malignant transformation by activating PI3K/AKT/MTORC1 signaling.
- Comparing the PI3K Inhibitors in Hematological Malignancies: Review of Faers () - Nov 24, 2021 - Abstract #ASH2021ASH_6412;
The overall rates of serious adverse effects are comparable between the 3 PI3KI, though diarrhea is most common with duvelisib, pneumonitis, and rash with copanlisib. As these drugs are mainly used in the relapsed refractory setting, many more years of follow-up are needed to get a better idea of real-world data as we have more experience with these drugs.
- | Journal: Thrombospondin 2 Promotes IL-6 Production in Osteoarthritis Synovial Fibroblasts via the PI3K/AKT/NF-κB Pathway. (Pubmed Central) - Nov 24, 2021
Finally, in the result of rat ACLT surgical model, we found that TSP2 neutralizing antibody had protective effects in cartilage destruction during OA progression. Thrombospondin-2 palys an important role in osteoarthritis pathogenesis and provides an opportunity to deal with osteoarthritis.
- | chloroquine phosphate / Generic mfg.
Preclinical, Journal: JieZe-1 Alleviates HSV-2 Infection-Induced Genital Herpes in Balb/c Mice by Inhibiting Cell Apoptosis via Inducing Autophagy. (Pubmed Central) - Nov 24, 2021
After then, under autophagy inhibitor chloroquine application, we measured the levels of cell apoptosis and autophagy and investigated the relationship between enhanced autophagy and cell apoptosis...Additionally, PI3K/Akt/mTOR signaling pathway was also downregulated by JZ-1 administration. Our data demonstrated that JZ-1 can alleviate HSV-2 infection-induced GH in balb/c mice by inhibiting cell apoptosis via inducing autophagy, and the underlying mechanisms may be associated with the inhibition of PI3K/Akt/mTOR pathway.
- | Journal: Ampelopsin Inhibits Cell Viability and Metastasis in Renal Cell Carcinoma by Negatively Regulating the PI3K/AKT Signaling Pathway. (Pubmed Central) - Nov 24, 2021
Moreover, Ampelopsin was only cytotoxic to RCC cells. Ampelopsin inhibits cell viability and metastasis in RCC by negatively regulating the PI3K/AKT signaling pathway.
- | Journal: Synthesis and antitumor evaluation of (aryl)methyl-amine derivatives of dehydroabietic acid-based B ring-fused-thiazole as potential PI3K/AKT/mTOR signaling pathway inhibitors. (Pubmed Central) - Nov 24, 2021
The primary bioassay showed that compounds 5r and 5s presented certain inhibitory activity against cancer cells, weak cytotoxic activity against normal cells, and inhibitory activity against PI3K/AKT/mTOR signaling pathway. The binding modes and the binding site interactions between the active compounds and the target proteins were predicted preliminarily by the molecular docking method.
- | Preclinical, Journal: Postnatal overfeeding induces hepatic microRNA-221 expression and impairs the PI3K/AKT pathway in adult male rats. (Pubmed Central) - Nov 24, 2021
The binding modes and the binding site interactions between the active compounds and the target proteins were predicted preliminarily by the molecular docking method. We first report postnatal overfeeding induces hepatic miR-221 expression.Postnatal overfeeding impairs PI3K/AKT pathway in the liver of adult rats.Postnatal overfeeding induces obesity and high blood glucose.Avoidance of overfeeding during early postnatal life may prevent obesity and T2DM.
- | Preclinical, Journal: MiR-199a-3p inhibits the proliferation, migration, and invasion of endothelial cells and retinal pericytes of diabetic retinopathy rats through regulating FGF7 via EGFR/PI3K/AKT pathway. (Pubmed Central) - Nov 24, 2021
Our findings revealed that in the DR rat model, miR-199a-3p inhibited cell proliferation, migration, and invasion of EC and RP through targeting FGF7 and inhibiting the activation of the EGFR/PI3K/AKT pathway. This study may provide a new direction for the search for the treatment of DR.
- | Lumakras (sotorasib) / Amgen
Preclinical, Journal: Epithelial to mesenchymal transition is a cause of both intrinsic and acquired resistance to KRAS G12C inhibitor in KRAS G12C mutant non-small cell lung cancer. (Pubmed Central) - Nov 24, 2021
This study may provide a new direction for the search for the treatment of DR. Our findings suggest that EMT is a cause of both intrinsic and acquired resistance by activating the PI3K pathway in the presence of KRAS G12C inhibitor.
- | Journal: Multiplex immunofluorescence in formalin-fixed paraffin-embedded tumor tissue to identify single cell-level PI3K pathway activation. (Pubmed Central) - Nov 24, 2021
Our findings suggest that EMT is a cause of both intrinsic and acquired resistance by activating the PI3K pathway in the presence of KRAS G12C inhibitor. Our novel pathway-focused approach to quantifying single cell-level immunofluorescence in FFPE tissue identifies prostate tumors with PI3K pathway activation that are more aggressive and may respond to pathway inhibitors.
- | Journal, IO biomarker: Gonadotroph tumours with a low SF-1 labelling index are more likely to recur and are associated with enrichment of the PI3K-AKT pathway. (Pubmed Central) - Nov 24, 2021
We speculate that patchy SF-1 labelling in GT reflects intratumoural heterogeneity and are less differentiated tumours than diffusely staining GT. SF-1 immunolabeling patterns may have prognostic significance in GT, but confirmatory studies are needed for further validation.
- | bleomycin / Generic mfg.
Journal: A long-acting isomer of Ac-SDKP attenuates pulmonary fibrosis through SRPK1-mediated PI3K/AKT and Smad2 pathway inhibition. (Pubmed Central) - Nov 24, 2021
In vivo, Ac-SD K P exhibited significantly greater protective effects against bleomycin-induced pulmonary fibrosis than Ac-SDKP in mice...Our data suggest that long-acting Ac-SD K P may potentially be an effective drug for the treatment of pulmonary fibrosis. The interacting molecule and antifibrotic mechanism of Ac-SDKP/Ac-SD K P were also identified, providing an experimental and theoretical foundation for the clinical application of the drug.
- | Preclinical, Journal: Potential role of TrkB agonist in neuronal survival by promoting CREB/BDNF and PI3K/Akt signaling in vitro and in vivo model of 3-nitropropionic acid (3-NP)-induced neuronal death. (Pubmed Central) - Nov 24, 2021
Akt phosphorylation additionally phosphorylates Bad at serine-136 and inhibits its translocation to mitochondria thereby promoting mitochondrial biogenesis, enhanced ATP production and inhibit apoptosis mediated neuronal death. These aforementioned findings help in strengthening our hypothesis and has come up with a novel neuroprotective mechanism of 7,8-DHF against 3-NP induced neuronal death.
- | MK-2206 / Merck (MSD), LY294002 / Eli Lilly
Journal: The Potential Role of CERS1 in Autophagy Through PI3K/AKT Signaling Pathway in Hypophysoma. (Pubmed Central) - Nov 24, 2021
In addition, shCERS1 could reverse the process. The above results indicate that CERS1 is possibly able to enhance autophagy in hypophysoma through the PI3K/AKT signaling pathway.
- | cisplatin / Generic mfg.
Journal: Periostin Secreted by Carcinoma-Associated Fibroblasts Promotes Ovarian Cancer Cell Platinum Resistance Through the PI3K/Akt Signaling Pathway. (Pubmed Central) - Nov 24, 2021
Functional studies revealed that periostin could decrease cisplatin (DDP)-induced apoptosis in EOC...We generated periostin-overexpressing fibroblasts and found that EOC cells were resistant to DDP when co-cultured with periostin-overexpressing fibroblasts. The findings of the present study indicated that periostin secreted by cancer-associated stromal cells may be a potential therapeutic target for EOC.
- | Journal: Effect of PI3K/AKT/mTOR Signaling Pathway on Regulating and Controlling the Anti-Invasion and Metastasis of Hepatoma Cells by Bufalin. (Pubmed Central) - Nov 24, 2021
The present study shows that the anti-tumor effect of Bufalin mainly inhibit proliferation, extracellular matrix degradation and angiogenesis of HCC by influencing autophagy. These findings confirm the capability of Bufalin in inhibiting metastasis of HCC and in parallel to current patents, could be applied as a novel therapeutic strategy in the prevention of metastasis of HCC.
- | Journal: Upregulation of Long Noncoding RNA_GAS5 Suppresses Cell Proliferation and Metastasis in Laryngeal Cancer via Regulating PI3K/AKT/mTOR Signaling Pathway. (Pubmed Central) - Nov 24, 2021
Mechanistically, our data showed that the overexpression of lncRNA GAS5 significantly regulated the PI3K/AKT/mTOR signaling pathway. LncRNA GAS5 might act as a suppressor gene during laryngeal cancer development, as it suppressed cell proliferation and metastasis by regulating the PI3K/AKT/mTOR signaling pathway; thus, lncRNA GAS5 is a promising therapeutic biomarker for the treatment of laryngeal cancer.
- | Journal: PI3K/BCL2: illusion or promise for RS? (Pubmed Central) - Nov 24, 2021
LncRNA GAS5 might act as a suppressor gene during laryngeal cancer development, as it suppressed cell proliferation and metastasis by regulating the PI3K/AKT/mTOR signaling pathway; thus, lncRNA GAS5 is a promising therapeutic biomarker for the treatment of laryngeal cancer. No abstract available
- | MK-2206 / Merck (MSD), pictilisib (GDC-0941) / Roche
Journal: PI3K regulates the activation of NLRP3 inflammasome in atherosclerosis through part-dependent AKT signaling pathway. (Pubmed Central) - Nov 24, 2021
Therefore, PI3K inhibition can retard the progress of atherosclerosis. Besides, there may be other AKT-independent pathways that regulate the formation of atherosclerosis.
- | Journal: T-lymphoma invasion and metastasis 1 promotes invadopodia formation and is regulated by the PI3K/Akt signaling pathway in hepatocellular carcinoma. (Pubmed Central) - Nov 24, 2021
We also confirmed that PIP2 facilitates this effect. In summary, these findings reveal that Tiam1 plays an important role in invadopodia formation in HCC.
- | Biomarker, Journal: Human α-Defensin 5 suppressed Colon Cancer Growth by Targeting PI3K pathway. (Pubmed Central) - Nov 24, 2021
Mechanistically, DEFA5 directly binds to the subunits of PI3K complex, thus attenuates the downstream signaling transduction, leads to delayed cell growth and metastasis. Collectively, we concluded that DEFA5 showed an inhibitory effect in colon cancer cell growth and may serve as a potential tumor suppressor in colon cancer.
- | LY294002 / Eli Lilly
Journal: Apelin-13 Reverses Bupivacaine-Induced Cardiotoxicity via the Adenosine Monophosphate-Activated Protein Kinase Pathway. (Pubmed Central) - Nov 24, 2021
Apelin-13 treatment reduced bupivacaine-induced oxidative stress, attenuated mitochondrial morphological changes and mitochondrial DNA damage, enhanced mitochondrial energy metabolism, and ultimately reversed bupivacaine-induced cardiotoxicity. Our results suggest a role for the AMPK in apelin-13 reversal of bupivacaine-induced cardiotoxicity.
- | LY294002 / Eli Lilly, PD98059 / Wayne State University
Journal, IO biomarker: The Potential Role of Osteopontin in the Pathogenesis of Graves' Ophthalmopathy. (Pubmed Central) - Nov 24, 2021
OPN promoted proliferation and migration of OFs and induced VEGF and collagen I mRNA expression in OFs through PI3K/Akt signaling pathway. This suggested a role for OPN in the pathogenesis of GO through the activation of OFs.
- | Journal, IO biomarker: Fumonisin B1 exposure induces apoptosis of human kidney tubular epithelial cells through regulating PTEN/PI3K/AKT signaling pathway via disrupting lipid raft formation. (Pubmed Central) - Nov 24, 2021
Also, FB1 could disrupt lipid raft by decreasing sphingomyelin level. In conclusion, FB1 exposure induces apoptosis of HK-2 cells through regulating PTEN/PI3K/AKT signaling pathway via disrupting lipid raft formation.
- |||| Fyarro (nanoparticle albumin-bound rapamycin) / Aadi Biosci
Clinical, FDA event: Hear ye hear ye! These patients have PI3K pathway alterations FDA Approves Nab-Sirolimus for Locally Advanced Unresectable or Metastatic PEComa https://t.co/MDGYCA47o3 (Twitter) - Nov 23, 2021
- ||| parsaclisib (INCB50465) / Incyte
Trial completion date, Combination therapy: CITADEL-310: A Study of Parsaclisib, a PI3K? Inhibitor, in Combination With Bendamustine and Rituximab in Patients With Newly Diagnosed Mantle Cell Lymphoma (clinicaltrials.gov) - Nov 23, 2021
P3, N=516, Not yet recruiting, Sponsor: Incyte Corporation
In conclusion, FB1 exposure induces apoptosis of HK-2 cells through regulating PTEN/PI3K/AKT signaling pathway via disrupting lipid raft formation. Trial completion date: Oct 2031 --> May 2034
- | Journal: Choline Kinase Alpha Promoted Glioma Development by Activating PI3K/AKT Signaling Pathway. (Pubmed Central) - Nov 22, 2021
The authors demonstrated that CHKA was significantly elevated in glioma tissues. Mechanism analysis indicated that CHKA could promote glioma development by activating PI3K/AKT signaling pathway, suggesting that CHKA is promising to be a biomarker and therapeutic strategy for prognostic prediction of patients with glioma.
- || Herceptin (trastuzumab) / Roche
Review, Journal: Cardiotoxicity of Epidermal Growth Factor Receptor 2-Targeted Drugs for Breast Cancer. (Pubmed Central) - Nov 21, 2021
Measuring NT-proBNP is non-invasive, inexpensive and reproducible, therefore is worthy of the attention of clinicians. The aim of this review is to discuss the potential mechanisms, clinical features, diagnostic strategies, and intervention strategies related to cardiotoxicity of ErbB2-targeting drugs.
- | Journal: The RNA Methyltransferase METTL3 Promotes Endothelial Progenitor Cell Angiogenesis in Mandibular Distraction Osteogenesis via the PI3K/AKT Pathway. (Pubmed Central) - Nov 21, 2021
In vivo, METTL3-overexpressing EPCs were additionally transplanted into the DO callus, significantly enhancing bone regeneration as evidenced by improved radiological and histological manifestations in a canine mandibular DO model after consolidation over a 4-week period. Overall, these results indicate that METTL3 accelerates bone regeneration during DO by enhancing EPC angiogenesis via the PI3K/AKT pathway.
- | LY294002 / Eli Lilly
Journal: Achyranthes bidentata polypeptide alleviates neurotoxicity of lipopolysaccharide-activated microglia via PI3K/Akt dependent NOX2/ROS pathway. (Pubmed Central) - Nov 21, 2021
Moreover, LY294002 (a specific PI3K inhibitor) and SC79 (a specific Akt activator) were used to further reveal the underlying mechanism...Specific Akt activator could inhibit LPS-induced NOX2 expression, ROS production and glutamate release. The present results suggested that ABPPk could alleviate neurotoxicity of LPS-activated microglia via PI3K/Akt dependent NOX2/ROS pathway.
- | Avastin (bevacizumab) / Roche
Journal: Metformin alleviates bevacizumab-induced vascular endothelial injury by up-regulating GDF15 and activating the PI3K/AKT/FOXO/PPARγ signaling pathway. (Pubmed Central) - Nov 21, 2021
Lastly, the PI3K inhibitor exhibited similar effects to those of GDF15 siRNA in bevacizumab-treated HUVECs. Metformin protected against bevacizumab-induced vascular endothelial injury via activation of GDF15 and the PI3K/AKT/FOXO/PPARγ signaling pathway.
- | AUM302 / AUM Biosci
Journal: Macrocyclization as a Source of Desired Polypharmacology. Discovery of Triple PI3K/mTOR/PIM Inhibitors. (Pubmed Central) - Nov 21, 2021
We report the medicinal chemistry exploration and biological characterization of a series of thieno[3,2-d]pyrimidine MCXs, which led to the discovery of IBL-302 (31), a potent, selective, and orally bioavailable triple PI3K/mTOR/PIM inhibitor...Additionally, during the course of our experiments, we observed that macrocyclization was essential to obtain the desired multitarget profile. As a matter of example, the open precursors 35-37 were inactive against PIM whereas MCX 28 displayed low nanomolar activity.
- | Journal: Long non-coding RNA DDX11-AS1 promotes non-small cell lung cancer development via regulating PI3K/AKT signaling. (Pubmed Central) - Nov 21, 2021
These results indicated that DDX11-AS1 exacerbated NSCLC progression via activating PI3K/AKT signaling pathway. All in all, DDX11-AS1 promotes NSCLC development via regulating PI3K/AKT signaling.
- | cisplatin / Generic mfg.
Journal: FOXD1-AS1 regulates FOXD1 translation and promotes gastric cancer progression and chemoresistance by activating the PI3K/AKT/mTOR pathway. (Pubmed Central) - Nov 21, 2021
In conclusion, FOXD1-AS1 aggravates GC progression and chemoresistance by promoting FOXD1 translation via PIK3CA/PI3K/AKT/mTOR signaling. These findings highlight a novel target for treatment of patients GC, particularly patients with cisplatin-resistance.
- | Journal: Circular RNA CirCHIPK3 promotes cell proliferation and invasion of breast cancer by sponging miR-193a/HMGB1/PI3K/AKT axis. (Pubmed Central) - Nov 21, 2021
These findings highlight a novel target for treatment of patients GC, particularly patients with cisplatin-resistance. CirCHIPK3 regulated miR-193a/HMGB1/PI3K/AKT signaling to facilitate BC development and progression, providing a novel therapeutic target for BC.
- | LY294002 / Eli Lilly
Journal: TGF-β is associated with poor prognosis and promotes osteosarcoma progression via PI3K/Akt pathway activation. (Pubmed Central) - Nov 21, 2021
Pretreatment with 25 µM LY294002, a PI3K-specific inhibitor, further enhanced the si-TGF-β-induced suppression of osteosarcoma progression. Taken together, these results reveal a novel role for TGF-β in osteosarcoma progression and modulation of stemness-related traits and indicate that TGF-β may be of value as a therapeutic target for the treatment of osteosarcoma.
- | Journal: LncUBE2R2-AS1 acts as a microRNA sponge of miR-302b to promote HCC progression via activation EGFR-PI3K-AKT signaling pathway. (Pubmed Central) - Nov 21, 2021
Regarding the mechanism, UBE2R2-AS1/miR-302b/EGFR established the ceRNA network involved in the modulation of cell progression of HCC cells via activation of PI3K-AKT signaling pathway. Overall, UBE2R2-AS1 may exhibit an oncogenic function in HCC via acting as a sponge for miR-302b to up-regulate EGFR, and may serve as a potential therapeutic target and a prognostic biomarker for HCC patients.