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- | Preclinical, Journal: Physalin B ameliorates inflammatory responses in lipopolysaccharide-induced acute lung injury mice by inhibiting NF-κB and NLRP3 via the activation of the PI3K/Akt pathway. (Pubmed Central) - Mar 3, 2022
Furthermore, our findings provide a novel strategy for application of PB as a potential agent for treating patients with ALI. To the best of our knowledge, this is the first study to elucidate the underlying mechanism of action of PB against ALI.
- | sirolimus / Generic mfg.
Journal: Autophagy of spinal microglia affects the activation of microglia through the PI3K/AKT/mTOR signaling pathway. (Pubmed Central) - Mar 3, 2022
In conclusion, enhanced autophagy might be the mechanism of inhibited microglia activation by hypothermia treatment in ISCI rats and by rapamycin treatment in OGD-stimulated BV-2 cells. Autophagy could be enhanced through inhibiting the PI3K/AKT/mTOR pathway.
- | sirolimus / Generic mfg.
Journal: Artemisinin Inhibits the Migration and Invasion in Uveal Melanoma via Inhibition of the PI3K/AKT/mTOR Signaling Pathway. (Pubmed Central) - Mar 3, 2022
Artemisinin also induced mitochondrial membrane potential loss and apoptosis of UM cells, having no significant toxic effect on normal retinal neuronal cells RGC-5 and epithelial cells D407. These findings and the reported safety of artemisinin's clinical dosage strongly suggest the therapeutic potential of artemisinin in the prevention and treatment of uveal melanomas.
- | sirolimus / Generic mfg.
Journal: Selenium and Taurine Combination Is Better Than Alone in Protecting Lipopolysaccharide-Induced Mammary Inflammatory Lesions via Activating PI3K/Akt/mTOR Signaling Pathway by Scavenging Intracellular ROS. (Pubmed Central) - Mar 3, 2022
Inhibition of mTOR by Rapamycin counteracted the combined protection of SeMet and Tau against LPS-induced inflammatory damage, the inhibition of PI3K by LY294002 blocked the activation of mTOR, and the accumulation of ROS by the ROS agonist blocked the activation of PI3K. In conclusion, these findings suggested that Se and Tau combination was better than either substance alone in protecting LPS-induced mammary inflammatory lesions by upregulating the PI3K/Akt/mTOR signaling pathway.
- | PI-103 / Roche
Journal: Design, synthesis, and biological evaluation of new thieno[2,3-d] pyrimidine derivatives as targeted therapy for PI3K with molecular modelling study. (Pubmed Central) - Mar 3, 2022
Docking was carried out into PI3K active site which showed comparable binding mode to that of the PI-103 inhibitor. Compound VIb could be optimised to serve as a new chemical entity for discovering new anticancer agents.
- | LY294002 / Eli Lilly
Journal: Calycosin alleviates H O -induced astrocyte injury by restricting oxidative stress through the Akt/Nrf2/HO-1 signaling pathway. (Pubmed Central) - Mar 3, 2022
Furthermore, calycosin failed to increase Akt phosphorylation and mitigate H O -induced astrocyte damage in the presence of the LY294002 (a selective phosphatidylinositol 3-kinase inhibitor), indicating that calycosin-mediated regulation of oxidative-stress homeostasis involved Akt/Nrf2/HO-1 signaling. These findings demonstrated that calycosin protects against oxidative injury in brain astrocytes by regulating oxidative stress through the AKT/Nrf2/HO-1 signaling pathway.
- | acetylcysteine solution / Generic mfg.
Journal: Uranium induces kidney cells apoptosis via reactive oxygen species generation, endoplasmic reticulum stress and inhibition of PI3K/AKT/mTOR signaling in culture. (Pubmed Central) - Mar 3, 2022
Administration of antioxidant N-acetylcysteine (NAC) effectively blocked U-triggered ROS generation, ER stress, and apoptosis...Taken together, these data strongly suggest that U treatment induces NRK-52 cells apoptosis through ROS production, ER stress, and down-regulation of PI3K/AKT/mTOR signaling. Targeting ROS formation-, ER stress-, and PI3K/AKT/mTOR pathway-mediated apoptosis could be a novel approach for attenuating U-triggered nephrotoxicity.
- | atorvastatin / Generic mfg.
Preclinical, Journal: Atorvastatin ameliorates depressive behaviors via regulation of α7nAChR expression by PI3K/Akt-BDNF pathway in mice. (Pubmed Central) - Mar 1, 2022
The phosphatidylinositol-3 kinase (PI3K) inhibitor LY294002 reversed AV-induced increase of BDNF expression, newborn neurons and antidepressant behavior effects. Our study suggests that AV plays an antidepressant role by regulating synaptic plasticity of vHPC through PI3K/Akt-BDNF signaling pathway, which may be a good choice for depression treatment.
- | LY294002 / Eli Lilly
Preclinical, Journal: A Mixture of Baicalein, Wogonin, and Oroxylin-A Inhibits EMT in the A549 Cell Line via the PI3K/AKT-TWIST1-Glycolysis Pathway. (Pubmed Central) - Mar 1, 2022
Furthermore, stable isotope dimethyl-labeled proteomics technology was conducted to complement the follow-up mechanism that the EMT-inhibition process may be realized through the glycolysis pathway. In conclusion, we claim that TWIST1-targeted flavonoids could provide a new strategy to inhibit EMT progress for the treatment of NSCLC.
- | Journal: miR-129-5p inhibits oxidized low-density lipoprotein-induced A7r5 cell viability and migration by targeting HMGB1 and the PI3k/Akt signaling pathway. (Pubmed Central) - Mar 1, 2022
The present results demonstrated that miR-129-5p inhibited the viability, viability and migration of A7r5 cells induced by ox-LDL, and directly targeted HMGB1 to regulate the PI3k/Akt signaling pathway. In conclusion, miR-129-5p inhibited the PI3k/Akt signaling pathway by directly targeting HMGB1, and reduced the viability, viability and migration of A7r5 cells induced by ox-LDL.
- | Journal: Carboxyl-Functionalized Carbon Nanotubes Loaded with Cisplatin Promote the Inhibition of PI3K/Akt Pathway and Suppress the Migration of Breast Cancer Cells. (Pubmed Central) - Feb 27, 2022
MDA-MB-231 cells were exposed to various doses (0.01-2 µg/mL SWCNT-COOH and 0.00632-1.26 µg/mL CDDP) of SWCNT-COOH-CDDP and free components for 24 and 48 h. In vitro biological tests revealed that SWCNT-COOH-CDDP had a high cytotoxic effect, as shown by a time-dependent decrease in cell viability and the presence of a significant number of dead cells in MDA-MB-231 cultures at higher doses. Moreover, the nanoconjugates induced the downregulation of PI3K/Akt signaling, as revealed by the decreased expression of PI3K and p-Akt in parallel with PTEN activation, the promotion of Akt protein degradation, and inhibition of tumor cell migration.
- || Piqray (alpelisib) / Novartis, Zydelig (idelalisib) / Gilead, Copiktra (duvelisib) / Secura Bio, Yakult Honsha
Clinical, Review, Journal: Development of PI3K inhibitors: advances in clinical trials and new strategies (Review). (Pubmed Central) - Feb 26, 2022
Their corresponding structure characteristics and structures-activity relationship (SAR), together with the progress in the clinical application are mainly discussed. Additionally, the new PI3K inhibitory strategy, such as PI3K degradation agent, for the design of potential PI3K candidates to overcome drug resistance is referred as well.
- | Stivarga (regorafenib) / Bayer
Journal: Catalpol synergistically potentiates the anti-tumour effects of regorafenib against hepatocellular carcinoma via dual inhibition of PI3K/Akt/mTOR/NF-κB and VEGF/VEGFR2 signaling pathways. (Pubmed Central) - Feb 26, 2022
Catalpol and/or regorafenib markedly suppressed PI3K/p-Akt/mTOR/NF-κB and VEGF/VEGFR2 signaling pathways and consequently showed potent anti-tumour effects against HCC. Results encourage further pre-clinical and clinical studies of this novel combination as a promising targeted therapy for HCC management.
- | remifentanil / Generic mfg.
Journal: Remifentanil pretreatment ameliorates H/R-induced cardiac microvascular endothelial cell dysfunction by regulating the PI3K/Akt/HIF-1α signaling pathway. (Pubmed Central) - Feb 26, 2022
Inhibition of PI3K/Akt rescued REM-enhanced HCMEC function under H/R condition. Therefore, the present study demonstrated that REM pretreatment ameliorated H/R-induced HCMEC dysfunction by regulating the PI3K/Akt/HIF-1α signaling pathway.
- | Journal: Suppression of PI3K signaling is linked to autophagy activation and the spatiotemporal induction of the lens organelle free zone. (Pubmed Central) - Feb 26, 2022
RNAseq analysis revealed increased mRNA levels of the endogenous inhibitor of PI3K activation, PIK3IP1, in differentiating lens fiber cells preceding the induction of OFZ formation. Co-immunoprecipitation confirmed that PIK3IP1 associates with multiple PI3K p110 isoforms just prior to formation of the OFZ, providing a likely endogenous mechanism for blocking all PI3K signaling and activating the autophagy pathway required to form the OFZ during lens development.
- | Journal: Blue Light Alters the Composition of the Jejunal Microbiota and Promotes the Development of the Small Intestine by Reducing Oxidative Stress. (Pubmed Central) - Feb 26, 2022
Overall, these findings suggested that BL increased the relative abundance of Faecalibacterium, Ruminiclostridium_9 and butyrate production. Butyrate may act as one of the signals to mediate blue-light-induced small intestinal development and mucosal barrier integrity enhancement and promote cell proliferation via the GPR43/Gi/PI3K/AKT/p-GSK-3β/β-catenin pathway.
- | fimepinostat (CUDC-907) / Curis
Journal: Dual Targeting of PI3K and HDAC by CUDC-907 Inhibits Pediatric Neuroblastoma Growth. (Pubmed Central) - Feb 26, 2022
Furthermore, CUDC-907 significantly inhibits NB tumor growth in a 3D spheroid tumor model that recapitulates the in vivo tumor growth. Overall, our findings highlight that the dual inhibition of PI3K and HDAC by CUDC-907 is an effective therapeutic strategy for NB and other MYC-dependent cancers.
- || Venclexta (venetoclax) / Roche, AbbVie
Review, Journal, IO biomarker: Druggable Molecular Pathways in Chronic Lymphocytic Leukemia. (Pubmed Central) - Feb 26, 2022
Moreover, the restoration of apoptosis by the BCL2 inhibitor venetoclax offers meaningful clinical activity with a fixed-duration scheme...Other signaling cascades involved in CLL pathogenesis, in particular NOTCH signaling and NF-kB signaling, already provide biomarkers for a precision medicine approach to CLL and may represent potential druggable targets for the future. The aim of the present review is to discuss the druggable pathways of CLL and to provide the biological background of the high efficacy of targeted biological drugs in CLL.
- | Journal: Explore the Anti-Acne Mechanism of Licorice Flavonoids Based on Metabonomics and Microbiome. (Pubmed Central) - Feb 26, 2022
In summary, this study confirmed the anti-acne mechanism of LCF, namely by regulating metabolic balance and microbial balance. Therefore, this discovery will provide theoretical guidance for the preparation development and clinical application of the drug.
- | LY294002 / Eli Lilly
Journal, IO biomarker: DG-8d, a novel diosgenin derivative, decreases the proliferation and induces the apoptosis of A549 cells by inhibiting the PI3k/Akt signaling pathway. (Pubmed Central) - Feb 25, 2022
DG-8d could inhibit the proliferation and induce the apoptosis of the A549 cells, which maybe mainly because of the suppression of the PI3k/Akt pathways. Finally, we believe that DG-8d can be developed as a possible agent for carcinoma therapy.
- | LY294002 / Eli Lilly, PD98059 / Wayne State University
Journal: Concanavalin A promotes angiogenesis and proliferation in endothelial cells through the Akt/ERK/Cyclin D1 axis. (Pubmed Central) - Feb 25, 2022
Moreover, Con A (10 mg/kg) exhibited a repair effect in ischaemic hind-limb mice. This study will provide a new option for treating ischaemic disease by local injection with Con A.
- | CBT-1 (tetrandrine) / CBA Pharma, Nexavar (sorafenib) / Bayer, Amgen
Journal: Deciphering the molecular mechanism of tetrandrine in inhibiting hepatocellular carcinoma and increasing sorafenib sensitivity by combining network pharmacology and experimental evaluation. (Pubmed Central) - Feb 25, 2022
In the combination group, tumour volumes and weights were decreased to 202.3 ± 17.4 mm and 151.5 ± 25.8 mg compared with Sora (510.6 ± 48.2 mm and 396.7 ± 33.5 mg). TET enhances Sora sensitivity by inactivating PI3K/AKT/mTOR, suggesting the potential of TET as a chemosensitizer in HCC.
- | Journal: LncRNA GAS5/miR-137 Is a Hypoxia-Responsive Axis Involved in Cardiac Arrest and Cardiopulmonary Cerebral Resuscitation. (Pubmed Central) - Feb 25, 2022
Furthermore, over-expression of miR-137 attenuated microglial apoptosis and neuroinflammation in CA/CPR mice model, exhibiting significantly better behavioral tests after CA/CPR. LncRNA GAS5/miR-137 may be involved in the astrocyte-microglia communication that inhibits PI3K/Akt signaling activation via regulation of INPP4B during CA/CPR.
- Piqray (alpelisib) / Novartis
Recommendations for Management of PI3K alpha Inhibitor-Induced Hyperglycemia Based on Alpelisib Treatment Experiences From Two Academic Institutions (Anaheim Convention Center - Learning Hall: Poster Pavilion) - Feb 25, 2022 - Abstract #ONS2022ONS_203;
Identifying patients at risk of developing alpelisib-associated hyperglycemia and proactively tailoring management to the individual will likely result in increased patient compliance and better outcomes of this AE. Innovation: These recommendations for nurses may help optimize hyperglycemia management in patients treated with alpelisib, a relatively new agent.
- | Preclinical, Journal, IO biomarker: Effects of stem cell-derived exosomes on neuronal apoptosis and inflammatory cytokines in rats with cerebral ischemia-reperfusion injury via PI3K/AKT pathway-mediated mitochondrial apoptosis. (Pubmed Central) - Feb 24, 2022
SC-Exos can significantly ameliorate brain injury caused by cerebral ischemia-reperfusion. The mechanism may be a novel therapeutic target for ischemia-reperfusion injury.
- | Preclinical, Journal: Lactiplantibacillus plantarum HG20 Attenuates Ⅱ Type Collagen-induced Rheumatoid Arthritis in Rats via Anti-inflammatory and Inhibition of Apoptosis. (Pubmed Central) - Feb 24, 2022
The mechanism may be a novel therapeutic target for ischemia-reperfusion injury. These results revealed that HG20 could be used as a functional probiotic in the field of food and medical, and which played a potential role in the prevention and treatment of arthritis.
- || Clinical, Journal, PD(L)-1 Biomarker, IO biomarker: (-)-4-O-(4-O-β-D-glucopyranosylcaffeoyl) quinic acid enhanced the efficacy of anti-PD-L1 against esophageal carcinoma through inhibiting PI3K pathway. (Pubmed Central) - Feb 24, 2022
QA and anti-PD-L1 combination therapy significantly delayed tumor growth. Our results provide a scientific basis to develop combination therapies involving anti-PD-L1 and PI3K inhibitors to improve responses in patients with esophageal cancer.
- | Journal, IO biomarker: Upregulating microRNA-373-3p promotes apoptosis and inhibits metastasis of hepatocellular carcinoma cells. (Pubmed Central) - Feb 24, 2022
Additionally, TFAP4 enhanced IGF1 expression, and promoted IGF1R-PI3K/AKT pathway activation. Collectively, miR-373-3p functions as an anti-tumor gene in HCC by inhibiting TFAP4/PI3K/AKT pathway.
- | LY294002 / Eli Lilly
Journal: The Anti-Inflammatory and Uric Acid Lowering Effects of Si-Miao-San on Gout. (Pubmed Central) - Feb 24, 2022
These effects of SMS were inhibited when PI3K/Akt activation was blocked by LY294002 in the macrophages...Ecdysone and estrone might be the potentially effective ingredients of SMS. This research may provide evidence for the application of SMS in the treatment of gout.
- || 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) - Feb 24, 2022
P2, N=227, Active, not recruiting, Sponsor: Bayer
This research may provide evidence for the application of SMS in the treatment of gout. Trial completion date: Mar 2022 --> Mar 2023
- | lapatinib / Generic mfg., doxorubicin hydrochloride / Generic mfg.
Journal: Lapatinib induces mitochondrial dysfunction to enhance oxidative stress and ferroptosis in doxorubicin-induced cardiomyocytes via inhibition of PI3K/Akt signaling pathway. (Pubmed Central) - Feb 23, 2022
The activation of PI3K/AKT signaling reversed the detrimental effects of LAP on DOX-induced H9c2 cells. The data in this study showed for the first time that LAP aggravated Dox-induced cardiotoxicity by promoting oxidative stress and ferroptosis in cardiomyocytes via PI3K/AKT-mediated mitochondrial dysfunction, suggesting that PI3K/AKT activation is a promising cardioprotective strategy for DOX /LAX combination therapies.
- | LY294002 / Eli Lilly
Journal, IO biomarker: 24-Dehydrocholesterol Reductase alleviates oxidative damage-induced apoptosis in alveolar epithelial cells via regulating Phosphatidylinositol-3-Kinase/Protein Kinase B activation. (Pubmed Central) - Feb 23, 2022
DHCR24 was down-regulated in HO-induced ALI, and overexpression of DHCR24 could inhibit HO-induced oxidative stress and apoptosis of A549 cells by activating the Phosphatidylinositol-3-Kinase/Protein Kinase B (PI3K/AKT) signaling pathway. The above exhibited a protective effect of DHCR24 on alveolar epithelial cells exposed to oxidative stress-mediated apoptosis and provided a novel therapeutic method for ALI.
- | MK-2206 / Merck (MSD)
Journal: Insulin regulates Nedd4-2 via a PKB-dependent mechanism in HEI-OC1 auditory cells-crosstalks with sphingolipid and cAMP signaling. (Pubmed Central) - Feb 23, 2022
The SGK1 inhibitor GSK650394 prevented insulin-induced phosphorylation of NRDG1, but not of PKB and Nedd4-2, whereas the phosphatidylinositol 3-kinase (PI3K) inhibitor wortmannin and the PKB inhibitor MK2206 inhibited phosphorylation of all components...Sphingosine 1-phosphate might protect Nedd4-2 against ceramide-induced insulin resistance. Insulin-mediated regulation of Nedd4-2 might impact on inner ear sodium homeostasis with implications for diabetes-induced inner ear damage.
- || eganelisib (IPI-549) / Infinity Pharma
Clinical, Journal, Cancer stem cells: The efficacy of PI3Kγ and EGFR inhibitors on the suppression of the characteristics of cancer stem cells. (Pubmed Central) - Feb 23, 2022
Both Eganelisib and Gefitinib showed antitumor effects in vivo while Eganelisib displayed more significant therapeutic efficacy and less side effects than Gefitinib on all miPS-CSC models. Thus, these data suggest that the inhibitiors of PI3K and EGFR, especially PI3Kγ, might be a promising therapeutic strategy against CSCs defeating cancer in the near future.
- || Aliqopa (copanlisib) / Bayer
Trial initiation date, Combination therapy: Phase 2 Study of PI3K Inhibitor Copanlisib in Combination With Fulvestrant in Selected ER+ and/or PR+ Cancers With PI3K (PIK3CA, PIK3R1) and/or PTEN Alterations (clinicaltrials.gov) - Feb 23, 2022
P2, N=78, Not yet recruiting, Sponsor: M.D. Anderson Cancer Center
Thus, these data suggest that the inhibitiors of PI3K and EGFR, especially PI3Kγ, might be a promising therapeutic strategy against CSCs defeating cancer in the near future. Initiation date: Feb 2022 --> May 2022
- ||||| WATCH: Experts give takeaways from a discussion on best practices treating HR+/HER2- metastatic breast cancer with CDK4/6 inhibitors and PI3K therapies based on data presented at #ESMO21 @Neil_Iyengar @BCJoyceO @drsarahsam @DukeCancer @sloan_kettering https://t.co/oahGzWRWK8 (Twitter) - Feb 22, 2022
- | JQ-1 / Roche, dactolisib (RTB101) / Adicet Bio
Journal: BET protein inhibition evidently enhances sensitivity to PI3K/mTOR dual inhibition in intrahepatic cholangiocarcinoma. (Pubmed Central) - Feb 22, 2022
As a novel phosphoinositide 3-kinase (PI3K)/mTOR dual inhibitor, BEZ235, exerts antitumour activity by effectively and specifically blocking the dysfunctional activation of the PI3K/serine/threonine kinase (AKT)/mTOR pathway...However, Bromo- and extraterminal domain (BET) inhibition by JQ1 downregulates c-Myc and YAP transcription, which could enhance the efficacy of PI3K/mTOR inhibitors...Our data further confirmed that the combination of PI3K/mTOR dual inhibitor and BET inhibition induces M1 polarization and suppresses M2 polarization in macrophages by regulating the expression of HIF-1α. Our study provides a novel and efficient therapeutic strategy in treating primary ICC.
- | tetracycline / Generic mfg.
Preclinical, Journal: Matrine inhibits synovial angiogenesis in collagen-induced arthritis rats by regulating HIF-VEGF-Ang and inhibiting the PI3K/Akt signaling pathway. (Pubmed Central) - Feb 22, 2022
Matrine (Mat) is an alkaloid of tetracycline quinazine, and previous studies have demonstrated its specific effect on relieving rheumatoid arthritis (RA)...Therefore, Mat exerts an anti-angiogenesis effect by regulating the HIF-VEGF-Ang axis and inhibiting the PI3K/Akt signaling pathway. This inhibits the pathogenesis and improve the symptoms of RA, and may be offered as a candidate drug for the treatment of RA.
- | Journal, IO biomarker: miR-138 Reduces the Dysfunction of T Follicular Helper Cells in Osteosarcoma via the PI3K/Akt/mTOR Pathway by Targeting PDK1. (Pubmed Central) - Feb 22, 2022
The results of the dual-luciferase report experiment showed that miR-138 can target and negatively regulate PDK1, and PDK1 can reverse the effect of miR-138 on the function of Tfh cells and immature B cells. miR-138 inhibits the PI3K/Akt/mTOR pathway by targeting and negatively regulating PDK1 to alleviate the dysfunction of T follicular helper cells in OS.
- | Tukysa (tucatinib) / Seagen, Herceptin (trastuzumab) / Roche
Preclinical, Journal: Combination of tucatinib and neural stem cells secreting anti-HER2 antibody prolongs survival of mice with metastatic brain cancer. (Pubmed Central) - Feb 22, 2022
In addition, dual HER2 blockade using anti-HER2Ab LM008 NSCs and the tyrosine kinase inhibitor tucatinib significantly improved the survival of mice in a clinically relevant model of multiple HER2+ BCBM. These findings provide compelling evidence for the use of HER2Ab-secreting LM008 NSCs in combination with tucatinib as a promising therapeutic regimen for patients with HER2+ BCBM.
- | doxorubicin hydrochloride / Generic mfg.
Journal: Novel microtubule inhibitor SQ overcomes multidrug resistance in MCF-7/ADR cells by inhibiting BCRP function and mediating apoptosis. (Pubmed Central) - Feb 22, 2022
Therefore, in this study, we investigated the effect of SQ on adriamycin-resistant MCF-7 (MCF-7/ADR) cells and explored the underlying mechanism...In addition, SQ could block the cell cycle at G2/M phase in parental and MCF-7/ADR cells, thereby mediating cell apoptosis, which was related with the inhibition of PI3K-Akt-MDM2 pathway. Taken together, our findings indicate that SQ overcomes multidrug resistance in MCF-7/ADR cells by inhibiting BCRP function and mediating apoptosis through PI3K-Akt-MDM2 pathway inhibition.
- | Biomarker, Journal: KIR2DL4 promotes the proliferation of RCC cell associated with PI3K/Akt signaling activation. (Pubmed Central) - Feb 22, 2022
Taken together, our findings indicate that SQ overcomes multidrug resistance in MCF-7/ADR cells by inhibiting BCRP function and mediating apoptosis through PI3K-Akt-MDM2 pathway inhibition. Our results indicate that KIR2DL4 is also expressed by RCC cells, which promotes RCC progression associated with PI3K/AKT activation.
- | Panzem (2-methoxyestradiol) / CASI
Journal: 2-Methoxyestradiol combined with ascorbic acid facilitates the apoptosis of chronic myeloid leukemia cells via the microRNA-223/Fms-like tyrosine kinase 3/phosphatidylinositol-3 kinase/protein kinase B axis. (Pubmed Central) - Feb 22, 2022
Furthermore, 2-ME + AA suppressed CML xenograft growth in mice. Collectively, 2-ME + AA promoted miR-223 expression and suppressed FLT3 and the PI3K/AKT pathway, thereby facilitating the apoptosis of CML cells and inhibiting CML xenograft growth in mice.
- | Journal: Synthesis and Antitumor Evaluation of Menthone-Derived Pyrimidine-Urea Compounds as Potential PI3K/Akt/mTOR Signaling Pathway Inhibitor. (Pubmed Central) - Feb 22, 2022
Furthermore, the results of network pharmacology prediction and Western blot experiments indicated that compound 4i might inhibit Hela cells through inhibit PI3K/Akt/mTOR signaling pathway. The binding modes and the binding sites interactions between compound 4i and the target proteins were predicted preliminarily by the molecular docking method.
- | LY294002 / Eli Lilly
Preclinical, Journal, IO biomarker: Biphalin, a dimeric opioid peptide, reduces neonatal hypoxia-ischemia brain injury in mice by the activation of PI3K/Akt signaling pathway. (Pubmed Central) - Feb 19, 2022
These effects were also reversed by naloxone and Ly294002 respectively. In conclusion, biphalin protects against HI brain injury in neonatal mice, which might be through activation of the opioid receptor/phosphatidylinositol-3-kinase/Akt signaling pathway.
- | Journal, IO biomarker: Pseudo-ginsenoside Rh2 Induces Protective Autophagy in Hepatocellular Carcinoma HepG2 Cells. (Pubmed Central) - Feb 19, 2022
In conclusion, biphalin protects against HI brain injury in neonatal mice, which might be through activation of the opioid receptor/phosphatidylinositol-3-kinase/Akt signaling pathway. Pseudo-G-Rh2 could induce protective autophagy in HepG2 cells, at least in part, via AMPK and the PI3K/Akt/mTOR pathway.
- || Review, Journal, IO biomarker: BCL-2 Inhibition as Treatment for Chronic Lymphocytic Leukemia. (Pubmed Central) - Feb 19, 2022
At the end of the 1990s, with the advent of imatinib for chronic myeloid leukemia and rituximab for B cell lymphoproliferative diseases with CD20 expression, there was a great conceptual evolution in the treatment of onco-hematological diseases...In fit patients with immunoglobulin heavy chain mutation, it is still acceptable to use the chemotherapy regimen with fludarabine, cyclophosphamide, and rituximab (FCR) and, in those who do not fit or are not IgVH-mutated, bendamustine-rituximab regimen...In the second line, venetoclax, ibrutinib, and idelalisib have become the preferred treatments...This article will focus on the treatment approach of CLL patients with BCl2 antagonists. Treatment strategy (combined versus monotherapy; continuous versus limited duration therapy), toxicity profile, and future directions will be exposed in this review.
- | LY294002 / Eli Lilly
Journal: Puerarin attenuates intracerebral hemorrhage-induced early brain injury possibly by PI3K/Akt signal activation-mediated suppression of NF-κB pathway. (Pubmed Central) - Feb 19, 2022
However, LY294002 delivery could efficaciously weaken these neuroprotective effects of PUE. Overall, PUE could attenuate ICH-induced behavioral defects and EBI possibly by PI3K/Akt signal stimulation-mediated inhibition of the NF-κB pathway, and this made PUE a potential candidate as a promising therapeutic option for ICH-induced EBI.
- | 5-fluorouracil / Generic mfg.
Journal: Exosomal lncRNA FOXD3-AS1 upregulates ELAVL1 expression and activates PI3K/Akt pathway to enhance lung cancer cell proliferation, invasion, and 5-fluorouracil resistance. (Pubmed Central) - Feb 19, 2022
In conclusion, our study revealed that lung cancer cell-derived exosomal FOXD3-AS1 upregulated ELAVL1 expression and activated the PI3K/Akt pathway to promote lung cancer progression. Our findings provide a new strategy for lung cancer treatment.
- || ibrutinib / Generic mfg.
Review, Journal: Restoration of the immune function as a complementary strategy to treat Chronic Lymphocytic Leukemia effectively. (Pubmed Central) - Feb 19, 2022
In addition, we review the available evidence on how different treatment options for CLL including CIT regimens, small molecular inhibitors (i.e, BTK inhibitors, PI3K inhibitors, BCL-2 inhibitors) and T-cell therapies, affect the immune system and their clinical consequences. Finally, we propose that a dual therapeutic approach, acting directly against malignant B-cells and restoring the immune function is clinically relevant and should be considered when developing future strategies to treat patients with CLL.