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67 Companies | 59 Products |
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343 Trials |  |
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- | quercetin (LY294002) / Eli Lilly
Journal: Neuroprotective effect of ginkgetin in experimental cerebral ischemia/reperfusion via apoptosis inhibition and PI3K/Akt/mTOR signaling pathway activation. (Pubmed Central) - Sep 17, 2020
Taken together, these results for the first time suggest that ginkgetin antagonizes cerebral IR-induced injury by inhibiting apoptosis in rats, and this effect was attenuated by the activation of PI3K/Akt/mTOR signaling pathway.
- | Journal: Active PKG II inhibited the growth and migration of ovarian cancer cells through blocking Raf/ MEK and PI3K/Akt signaling pathways. (Pubmed Central) - Sep 16, 2020
Our results suggested that PKG II activated by L-Arg could inhibit proliferation and migration and promote the apoptosis of ovarian cancer cells. Based on the above results and our previous data, It is speculated that PKG II is an inhibitor of cancer with extensive effects.
- | quercetin (LY294002) / Eli Lilly, AG1478 / IDT Australia
Journal: Human chorionic gonadotropin-induced amphiregulin stimulates aromatase expression in human granulosa-lutein cells: a mechanism for estradiol production in the luteal phase. (Pubmed Central) - Sep 16, 2020
This work was also supported by an operating grant from the National Natural Science Foundation of China (81820108016) to Ying-Pu Sun. All authors declare no conflict of interest.
- | Preclinical, Journal: Geniposide attenuates neonatal mouse brain injury after hypoxic-ischemia involving the activation of PI3K/Akt signaling pathway. (Pubmed Central) - Sep 16, 2020
Geniposide treatment after neonatal HI insult attenuated HI-induced cell apoptosis, IgG leakage, microgliosis, astrogliosis, pericytes loss and junction protein degradation. Geniposide could protect against HI-induced brain injury, which might be through the activation of PI3K/Akt signaling pathway.
- | Preclinical, Journal: Parenterally Delivered Methionyl-Methionine Dipeptide During Pregnancy Enhances Mammogenesis and Lactation Performance Over Free Methionine by Activating PI3K-AKT Signaling in Methionine-Deficient Mice. (Pubmed Central) - Sep 16, 2020
Geniposide could protect against HI-induced brain injury, which might be through the activation of PI3K/Akt signaling pathway. Met-Met is more effective than Met in promoting mammogenesis and lactogenesis mainly by activation of PI3K-AKT signaling in Met-deficient mice.
- | Journal: Direct Current Electric Field Stimulates Nitric Oxide Production and Promotes NO-Dependent Angiogenesis: Involvement of the PI3K/Akt Signaling Pathway. (Pubmed Central) - Sep 16, 2020
Thus, activation of eNOS appears to be one of the key signaling pathways necessary for EF-mediated angiogenesis. These novel findings suggest that NO signaling may have an important role in EF-mediated endothelial cell function.
- | paclitaxel / Generic mfg.
Journal: A Nuclear lncRNA Linc00839 as a Myc target to promote breast cancer chemoresistance via PI3K/AKT Signaling Pathway. (Pubmed Central) - Sep 16, 2020
Knockdown of Linc00839 significantly suppressed proliferation, invasion, and migration, sensitized cells to paclitaxel in vitro and inhibited transplant tumor development in vivo...Taken together, for the first time, we showed that Linc00839 was activated by Myc and promoted proliferation and chemoresistance in BC through binding with Lin28B. These findings provide new insight into the regulatory mechanism of Linc00839, and propose a Myc/Linc00839/Lin28B feedback loop that could be used as a novel therapeutic target for breast cancer.
- | MK-2206 / Merck (MSD), dexamethasone / Generic mfg.
Journal: Melatonin rescues glucocorticoid-induced inhibition of osteoblast differentiation in MC3T3-E1 cells via the PI3K/AKT and BMP/Smad signalling pathways. (Pubmed Central) - Sep 16, 2020
These findings provide new insight into the regulatory mechanism of Linc00839, and propose a Myc/Linc00839/Lin28B feedback loop that could be used as a novel therapeutic target for breast cancer. These findings suggest that melatonin rescues Dex-induced inhibition of osteoblast differentiation in MC3T3-E1 cells via the PI3K/AKT and BMP/Smad signalling pathways and that PI3K/AKT signalling may be the upstream signal of BMP/Smad signalling.
- | quercetin (LY294002) / Eli Lilly
Journal, IO Biomarker: CPA4 Promotes EMT in Pancreatic Cancer via Stimulating PI3K-AKT-mTOR Signaling. (Pubmed Central) - Sep 16, 2020
However, LY294002 reversed CPA4 overexpression-stimulated cell proliferation and drug resistance in vitro in Bcl2/Bax and caspase3-dependent apoptosis. CPA4 overexpression contributes to aggressive clinical stage of PC patients and promotes EMT in vitro via activation of PI3K-AKT-mTOR signaling.
- | Journal: NF-κB-dependent Mechanism of Action of c-Myc Inhibitor 10058-F4: Highlighting a Promising Effect of c-Myc Inhibition in Leukemia Cells, Irrespective of p53 Status. (Pubmed Central) - Sep 16, 2020
In addition, we found that the anti-leukemic effect of 10058-F4 was overshadowed, at least partially, through the compensatory activation of the PI3K signaling pathway; highlighting a plausible attenuating role of this axis on 10058-F4 cytotoxicity. In conclusion, the results of the present study shed light on the favorable anti-leukemic effect of 10058-F4, especially in combination with PI3K inhibitors in acute promyelocytic leukemia; however, further investigations should be accomplished to determine the efficacy of the inhibitor, either as a single agent or in a combined-modal strategy, in leukemia treatment.
- | Journal: Long non-coding RNA LINC00473 acts as a microRNA-29a-3p sponge to promote hepatocellular carcinoma development by activating Robo1-dependent PI3K/AKT/mTOR signaling pathway. (Pubmed Central) - Sep 16, 2020
Notably, LINC00473 could competitively bind to miR-29a-3p to upregulate Robo1 expression. LINC00473 might be involved in HCC progression by acting as a miR-29a-3p sponge to upregulate the expression of Robo1 that activates the PI3K/AKT/mTOR signaling pathway, which leads to enhanced cell proliferation, migration, invasion, tumor progression, and metastasis in HCC.
- | Journal: Exosomes derived from human amniotic epithelial cells accelerate diabetic wound healing via PI3K-AKT-mTOR-mediated promotion in angiogenesis and fibroblast function. (Pubmed Central) - Sep 16, 2020
Further functional studies demonstrated that the PI3K-AKT-mTOR pathway was necessary for the induced biological effects of hAECs-Exos on HFBs and HUVECs, as well as on wound healing, in diabetic mice. Our findings demonstrated that hAECs-Exos represent a promising, novel strategy for diabetic wound healing by promoting angiogenesis and fibroblast function via activation of the PI3K-AKT-mTOR pathway.
- || Clinical, Journal, Tumor Mutational Burden, IO Biomarker: Evolving Landscape of Molecular Prescreening Strategies for Oncology Early Clinical Trials. (Pubmed Central) - Sep 16, 2020
The substantial increase of immunotherapy trials had a major impact in target prioritization and guided clinical implementation of new markers, such as tumor mutational burden, with larger exon-based NGS assays and gene expression signatures to capture microenvironment infiltration patterns. This new multiomics era of precision oncology is expected to increase the opportunities for early clinical trial matching.
- |||||||||| Jakafi (ruxolitinib) / Incyte, parsaclisib (INCB50465) / Incyte
New P3 trial: To Evaluate Efficacy and Safety of Parsaclisib and Ruxolitinib in Participants With Myelofibrosis Who Have Suboptimal Response to Ruxolitinib (LIMBER-304) (clinicaltrials.gov) - Sep 15, 2020
P3, N=212, Not yet recruiting, Sponsor: Incyte Corporation
- |||||||||| Jakafi (ruxolitinib) / Novartis, Incyte, parsaclisib (INCB50465) / Incyte
New P3 trial: To Evaluate the Efficacy and Safety of Parsaclisib and Ruxolitinib in Participants With Myelofibrosis (LIMBER-313) (clinicaltrials.gov) - Sep 15, 2020
P3, N=440, Not yet recruiting, Sponsor: Incyte Corporation
- ||| Initiative for Molecular Profiling and Advanced Cancer Therapy (IMPACT): An MD Anderson Precision Study: Tsimberidou, targeting PI3K when MEK pathway alterations present is ineffective even in presence of PI3K path alterations https://t.co/25Ne92izv4 (Twitter) - Sep 15, 2020
- | dactolisib (RTB101) / resTORbio
Journal: Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. (Pubmed Central) - Sep 13, 2020
For the effective treatment of chronic immunological disorders such as rheumatoid arthritis, it is essential to develop isoform selective PI3Kδ inhibitors. Structure guided optimization of an imidazo-quinolinones based pan-PI3K/m-TOR inhibitor (Dactolisib) led to the discovery of a potent and orally bioavailable PI3Kδ isoform selective inhibitor (10h), with an improved efficacy in the animal models.
- | Journal: Smooth muscle cells-derived CXCL10 prevents endothelial healing through PI3Kγ-dependent T cells response. (Pubmed Central) - Sep 13, 2020
Altogether, these findings expose an unforeseen cellular cross-talk within the arterial wall whereby a PI3Kγ-dependent T-cell response leads to CXCL10 production by smooth muscle cells which in turn inhibits endothelial healing. Therefore, both PI3Kγ and the IFNγ/CXCL10 axis provide novel strategies to promote endothelial healing.
- | Journal: miR-26a-5p enhances cells proliferation, invasion and apoptosis resistance of fibroblast-like synoviocytes in rheumatoid arthritis by regulating PTEN/PI3K/AKT pathway. (Pubmed Central) - Sep 13, 2020
Our study suggested that miR-26a-5p has a complementary role in cells proliferation, invasion and apoptosis of RA-FLS, which may be attributed to its activation effect on PI3K/AKT signaling pathway via targeting PTEN. miR-26a-5p is likely to be a clinically helpful target for novel therapeutic strategies in RA.
- | Journal: Overexpression of long non-coding RNA LINC00982 suppresses cell proliferation and tumor growth of papillary thyroid carcinoma through PI3K-ATK signaling pathway. (Pubmed Central) - Sep 13, 2020
Moreover, in vivo assay showed that overexpression of LINC00982 could suppress the growth of PTC. Finally, LINC00982 could regulate the activity of PI3K/AKT signaling pathway in vitro and in vivo Taken together, our findings demonstrated that overexpression of LINC00982 could suppress cell proliferation and induce cell apoptosis by regulating PI3K/AKT signaling pathway in papillary thyroid carcinoma.
- | Journal, IO Biomarker: Resveratrol delays 6-hydroxydopamine-induced apoptosis by activating the PI3K/Akt signaling pathway. (Pubmed Central) - Sep 13, 2020
Compared with those in the model group, the number of dopaminergic neurons cells and the expression of PI3K-110α, p-Akt Ser473, and pro-caspase-3 in the Res 30 mg/kg group were significantly increased, and the Bax/Bcl-2 ratio and the level of activated caspase-3 was decreased. The results indicate that Res ameliorates 6-OHDA-induced apoptosis and motor dysfunction via activating the PI3K/Akt signaling pathway, delaying the progression of Parkinson's disease (PD) symptoms in this model.
- || tamoxifen / Generic mfg., taselisib (GDC-0032) / Roche
Clinical, P1 data, Journal: POSEIDON phase 1b results: safety, efficacy and ctDNA response of taselisib combined with tamoxifen in hormone receptor positive metastatic breast cancer patients. (Pubmed Central) - Sep 13, 2020
Preliminary evidence of anti-tumor activity was seen in both PIK3CAmutant and wild-type cancers. The randomized phase 2 part of POSEIDON (testing tamoxifen plus taselisib or placebo) is currently recruiting.
- | Journal: NOV/CCN3 induces cartilage protection by inhibiting PI3K/AKT/mTOR pathway. (Pubmed Central) - Sep 13, 2020
Additionally, recombinant CCN3 or CCN3 overexpression attenuated the activation of PI3K/AKT/mTOR pathway induced by IL-1β. Our study presents new mechanisms of CCN3 in osteoarthritis and indicates that CCN3 can serve as a novel potential therapeutic target for osteoarthritis.
- | erlotinib / Generic mfg.
Journal: Identification of Resistance Pathways Specific to Malignancy Using Organoid Models of Pancreatic Cancer. (Pubmed Central) - Sep 13, 2020
The lack of ERBB hyperactivation in normal organoids suggests a larger therapeutic index. In our models pan-ERBB inhibition was synergistic with dual inhibition of MEK and AKT and the combination of a pan-ERBB inhibitor with MEK antagonists showed the highest activity both in vitro and in vivo.
- | aspirin / Generic mfg.
Preclinical, Journal: Aspirin inhibits adipogenesis of tendon stem cells and lipids accumulation in rat injury tendon through regulating PTEN/PI3K/AKT signalling. (Pubmed Central) - Sep 13, 2020
In conclusion, by down-regulating PTEN/PI3K/AKT signalling, aspirin inhibited adipogenesis of TSCs and fatty infiltration in injury tendon, promoted biomechanical properties and decreased rupture risk of injury tendon. All these provided new therapeutic potential and medicine evidence of aspirin in treating tendon injury and tendinopathy.
- | Journal: Lanatoside C Induces G2/M Cell Cycle Arrest and Suppresses Cancer Cell Growth by Attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR Signaling Pathways. (Pubmed Central) - Sep 13, 2020
Using Real-time PCR, western blot, and immunofluorescence studies, we observed that (i) Lanatoside C inhibited cell proliferation and induced apoptosis in cell-specific and dose-dependent manner only in cancer cell lines; (ii) Lanatoside C exerts its anti-cancer activity by arresting the G2/M phase of cell cycle by blocking MAPK/Wnt/PAM signaling pathways; (iii) it induces apoptosis by inducing DNA damage and inhibiting PI3K/AKT/mTOR signaling pathways; and finally, (iv) molecular docking analysis shows significant evidence on the binding sites of Lanatoside C with various key signaling proteins ranging from cell survival to cell death. Our studies provide a novel molecular insight of anti-cancer activities of Lanatoside C in human cancer cells.
- | ibrutinib / Generic mfg.
Journal: Resistance to BTK inhibition by ibrutinib can be overcome by preventing FOXO3a nuclear export and PI3K/AKT activation in B-cell lymphoid malignancies. (Pubmed Central) - Sep 13, 2020
These data demonstrate that reactivation of FOXO3a nuclear function enhances the efficacy of ibrutinib and overcomes acquired resistance to ibrutinib. Together, these findings reveal a novel mechanism that confers ibrutinib resistance via aberrant nuclear/cytoplasmic subcellular localization of FOXO3a and could be exploited by rational therapeutic combination regimens for effectively treating lymphoid malignancies.
- | MK-2206 / Merck (MSD), quercetin (LY294002) / Eli Lilly
Journal: PI3K/Akt/FoxO pathway mediates glycolytic metabolism in HepG2 cells exposed to triclosan (TCS). (Pubmed Central) - Sep 13, 2020
The PI3K/Akt/FoxO pathway was identified to play a pivot role in TCS-induced glycolysis, which was further confirmed by inhibitor tests using specific inhibitors LY294002 and MK2206. In general, TCS can induce oxidative stress, cause oxidative damages and promote glycolysis in HepG2 cells, which was mediated by the PI3K/Akt/FoxO pathway.
- [VIRTUAL] Combining Radiotherapy with PI3K Isoform-Selectivity Inhibitor Increases Radiosensitivity and Suppresses Tumor Growth in Glioblastoma Cells (Poster Hall) - Sep 13, 2020 - Abstract #ASTRO2020ASTRO_1283;
Also, GBM tumor growth was markedly suppressed and increased immunogenic marker such as PD1. Combining radiotherapy with the PI3K-α isoform inhibitor would be a potential strategy for overcoming radioresistance in GBM, but further study should be necessary.
- quercetin (LY294002) / Eli Lilly
[VIRTUAL] CMTM7 Knockout Decreases the Radiosensitivity of A549 Non-Small Cell Lung cancer Cells by Increasing Akt Signaling (Poster Hall) - Sep 13, 2020 - Abstract #ASTRO2020ASTRO_1240;
Together, we found that knockout of CMTM7 decreased the radiosensitivity of A549 cells in vitro and in vivo. The mechanism of radioresistance might be that the constitutive activation of Akt decreased the repair of DNA damage induced by IR, consequently leading to radiotherapy resistance.
- PF-04691502 / Pfizer
[VIRTUAL] Synergistic Cytotoxic Effect of a Novel mTOR/PI3K Dual Inhibitor PF-04691502 and Radiation Therapy on Neurondocrine Tumor Cells () - Sep 13, 2020 - Abstract #ASTRO2020ASTRO_1215;
The mechanism of radioresistance might be that the constitutive activation of Akt decreased the repair of DNA damage induced by IR, consequently leading to radiotherapy resistance. Embargoed Information
- | Journal: LNK deficiency decreases obesity-induced insulin resistance by regulating GLUT4 through the PI3K-Akt-AS160 pathway in adipose tissue. (Pubmed Central) - Sep 12, 2020
LNK adipose tissue showed activated reactivity for IRS1/PI3K/Akt/AS160 signaling, and administration of a PI3K inhibitor impaired glucose uptake. In conclusion, LNK plays a pivotal role in adipose glucose transport by regulating insulin-mediated IRS1/PI3K/Akt/AS160 signaling.
- || Clinical, Journal: 20(S)-Ginsenoside Rh2 displays efficacy against T-cell acute lymphoblastic leukemia through the PI3K/Akt/mTOR signal pathway. (Pubmed Central) - Sep 12, 2020
Finally, 20(S)-GRh2 alleviated symptoms of leukemia and reduced the number of white blood cells and CD3 staining in the spleen of xenograft mice, indicating antitumor effects against T-ALL invivo. These findings indicate that 20(S)-GRh2 exhibits beneficial effects against T-ALL through the PI3K/Akt/mTOR pathway and could be a natural product of novel target for T-ALL therapy.
- | Journal, PARP Biomarker, IO Biomarker: Gambogic acid affects ESCC progression through regulation of PI3K/AKT/mTOR signal pathway. (Pubmed Central) - Sep 12, 2020
Further investigation showed that GA down-regulated the levels of PI3K, p-AKT and p-mTOR, while promoted PTEN expression in ESCC cells. Taken together, we provided the first demonstration that GA exerts anti-tumor effects on ESCC cells presumably through regulating PTEN-PI3K-AKT-mTORpathway, suggestive of a therapeutic potential for ESCC.
- | quercetin (LY294002) / Eli Lilly
Journal: Elabela alleviates myocardial ischemia reperfusion-induced apoptosis, fibrosis and mitochondrial dysfunction through PI3K/AKT signaling. (Pubmed Central) - Sep 12, 2020
After treatment with Elabela or Elabela combined with LY294002, the levels of oxidative stress and apoptosis were examined...Within inhibition of PI3K pathway, the protective effects of Elabela was reversed. Taken together, these findings demonstrated that Elabela could protect against fibrosis, apoptosis and oxidative stress via PI3K/ATK signaling pathway in cardiac ischemia reperfusion.
- | Journal: Methylxanthine derivatives promote autophagy in gastric cancer cells targeting PTEN. (Pubmed Central) - Sep 11, 2020
In nude mice treated with caffeine or theophylline, MGC-803 cell tumours injected with siPTEN were larger than those injected with negative control siRNA. These results show that the methylxanthine derivatives (caffeine and theophylline) effectively induce gastric cancer cell apoptosis and autophagy by PTEN activation and PI3K/Akt/mTOR pathway suppression and strongly support the use of methylxanthine derivatives as potential anticancer therapeutics.
- | Journal: Up-regulated circular RNA hsa_circ_0067934 contributes to glioblastoma progression through activating PI3K-AKT pathway. (Pubmed Central) - Sep 11, 2020
These results show that the methylxanthine derivatives (caffeine and theophylline) effectively induce gastric cancer cell apoptosis and autophagy by PTEN activation and PI3K/Akt/mTOR pathway suppression and strongly support the use of methylxanthine derivatives as potential anticancer therapeutics. Hsa_circ_0067934 is overexpressed and plays an oncogenic role in GBM by promoting cancer cell proliferation and metastasis via upregulation of PI3K-AKT pathway, which suggests that hsa_circ_0067934 is likely to serve as an efficient therapeutic approach in respect of GBM treatment.
- | Biomarker, Journal: Research on miR-126 in glioma targeted regulation of PTEN/PI3K/Akt and MDM2-p53 pathways. (Pubmed Central) - Sep 11, 2020
Hsa_circ_0067934 is overexpressed and plays an oncogenic role in GBM by promoting cancer cell proliferation and metastasis via upregulation of PI3K-AKT pathway, which suggests that hsa_circ_0067934 is likely to serve as an efficient therapeutic approach in respect of GBM treatment. The miR-126 expression is abnormally low in glioma cells, and miR-126 inhibits the course of glioma through targeted regulation of PTEN/PI3K/Akt and MDM2-p53 pathways, which, therefore, can be used as a new potential biomarker for the diagnosis, treatment and prognosis of glioma.
- | Journal: Design and synthesis of novel 1-phenyl-3-(5-(pyrimidin-4-ylthio)-1,3,4-thiadiazol- 2-yl)urea derivatives with potent anti-CML activity throughout PI3K/AKT signaling pathway. (Pubmed Central) - Sep 11, 2020
Compound 7 also displayed very good induced-apoptosis effect for human CML cell line K562 and exerted its effect via a significantly reduced protein phosphorylation of PI3K/Akt signal pathway by Human phospho-kinase array analysis. In vitro results indicate that 1-phenyl-3-(5-(pyrimidin-4-ylthio)-1,3,4- thiadiazol-2-yl)urea derivatives are lead molecules for further development as treatment of chronic myeloid leukemia and cancer.
- | Journal, IO Biomarker: Lycium barbarum Polysaccharide Induced Apoptosis and Inhibited Proliferation in Infantile Hemangioma Endothelial Cells via Down-regulation of PI3K/AKT Signaling Pathway. (Pubmed Central) - Sep 10, 2020
Our study suggests that the effectiveness of LBP in IHs may be associated with its potent anti-proliferative and apoptotic activities in HemECs. Thus, our findings may provide an effective medicine for IHs treatment.
- | quercetin (LY294002) / Eli Lilly
Journal: Liraglutide Inhibits the Apoptosis of Human Nucleus Pulposus Cells Induced by High Glucose through PI3K/Akt/caspase-3 Signaling Pathway. (Pubmed Central) - Sep 10, 2020
Pretreatment of cells with the Phosphoinositide 3-kinase (PI3K) inhibitor LY294002 and siRNAs GLP-1R abrogated the liraglutide-induced activation of Akt and the protective effects on NPCs apoptosis. In conclusion, liraglutide could directly protect NPCs against high glucose-induced apoptosis by inhibiting oxidative stress and activating the PI3K/Akt/caspase-3 signaling pathway via GLP-1R.
- | Journal: In situ biosynthesized gold nanoclusters inhibiting cancer development via the PI3K-AKT signaling pathway. (Pubmed Central) - Sep 10, 2020
With the help of the RNA-seq analysis, we found that the in situ biosynthesized Au NCs could significantly inhibit the PI3K-AKT signaling pathway, thus effectively impeding tumor development. This facile and effective tumor targeting theranostics in vivo can effectively cure cancers in future clinical applications.
- | Journal: Co-enzyme Q10 protects primary chicken myocardial cells from heat stress by upregulating autophagy and suppressing the PI3K/AKT/mTOR pathway. (Pubmed Central) - Sep 10, 2020
Treatment with 20 μM Q10 also decreased the activation of the PI3K/Akt/mTOR pathway. Our results showed that co-enzyme Q10 can protect primary chicken myocardial cells by upregulating autophagy and suppressing the PI3K/Akt/mTOR pathway during heat stress.
- | Journal: Plastrum Testudinis Extract Mitigates Thiram Toxicity in Broilers via Regulating PI3K/AKT Signaling. (Pubmed Central) - Sep 10, 2020
The PTE administration significantly increased (p < 0.05) growth performance, vascularization, AKT (serine/threonine-protein kinase), and PI3K expressions and the number of hepatocytes and chondrocytes with intact nuclei were enhanced. In conclusion, PTE has the potential to heal TD lesions and act as an antioxidant and anti-inflammatory drug in chickens exposed to thiram via the upregulation of AKT and PI3K expressions.
- || paclitaxel / Generic mfg.
Review, Journal: PI3K Inhibitors in Breast Cancer Therapy. (Pubmed Central) - Sep 10, 2020
The high frequency of genetic alterations in the PI3K pathway has provided the rationale for development of inhibitors targeting PI3K/AKT. Despite initial disappointment with several randomized trials of pan-PI3K inhibitors in HR-positive breast cancer, there has been continued effort to more precisely target PI3K isoforms, which has led to clinical benefit for patients with advanced breast cancer.
- | Journal: Activated PI3Kδ breaches multiple B cell tolerance checkpoints and causes autoantibody production. (Pubmed Central) - Sep 10, 2020
However, within the germinal center, peripheral tolerance was still enforced, and there was selection against B cells with high affinity for self-antigen. These data show that the strength of PI3K signaling is a key regulator of pregerminal center B cell self-tolerance and thus represents a druggable pathway to treat antibody-mediated autoimmunity.
- | Preclinical, Journal: The regulatory effect of microRNA-21a-3p on the promotion of telocyte angiogenesis mediated by PI3K (p110α)/AKT/mTOR in LPS induced mice ARDS. (Pubmed Central) - Sep 10, 2020
TCs exerted protective effects under inflammatory conditions by promoting angiogenesis via miR-21a-3p. The PI3K p110α subunit and transcriptional factor E2F8 could be involved in this process.
- | Spherazole (itraconazole) / RA Chem, JW Pharma, Spherics, itraconazole / Generic mfg.
Journal: VEGF/VEGFR-2 system exerts neuroprotection against Phoneutria nigriventer spider envenomation through PI3K-AKT-dependent pathway. (Pubmed Central) - Sep 10, 2020
Collectively, the data confirmed VEGFR-2 signaling via serine-threonine kinase Akt as neuroprotective pathway against PNV-induced damage. Further studies are needed to elucidate mechanisms underlying PNV effects.
- | quercetin (LY294002) / Eli Lilly
Journal: Artesunate Ameliorates Sepsis-Induced Acute Lung Injury by Activating the mTOR/AKT/PI3K Axis. (Pubmed Central) - Sep 10, 2020
The rats were randomly assigned into 4 groups: Sham, LPS, LPS + AS, and LPS + AS + LY294002...AS could partially protect against LPS-induced ALI by inhibiting apoptosis and inflammatory mediator production, and this function is perhaps associated with the regulation of the mTOR/AKT/PI3K axis. These findings suggest that AS may possess certain beneficial characteristics in protecting the lungs from sepsis.
- || Verzenio (abemaciclib) / Eli Lilly
Clinical, Journal: PI3K p110α Blockade Enhances Anti-Tumor Efficacy of Abemaciclib in Human Colorectal Cancer Cells. (Pubmed Central) - Sep 10, 2020
Dual blockade of PI3K p110α and CDK4/6 showed synergistic anti-tumor effects in vivo and in vitro in human colorectal cancer cell lines. This combination could be a promising candidate for the treatment of patients with advanced colorectal cancer.