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67 Companies | 59 Products |
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344 Diseases | |
342 Trials |  |
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- | dovitinib (TKI258) / Allarity Therap
Preclinical, Journal: Anti-Proliferative Role of the Tyrosine Kinase Inhibitors TKI-258 on Oral Squamous Cell Carcinoma In Vitro. (Pubmed Central) - May 4, 2021
It could be interesting to block multiples pathways such as FGFRs, PDGFRs and VEGFRs. Therefore, TKI-258 is a promising option for novel therapeutics for OSCC, especially if associated with PI3K inhibition.
- | Preclinical, Journal, IO biomarker: Hydrogen exerts neuroprotection by activation of the miR-21/PI3K/AKT/GSK-3β pathway in an in vitro model of traumatic brain injury. (Pubmed Central) - May 4, 2021
Both the miR-21 antagomir and PI3K blocker reversed the protective effect of hydrogen. In conclusion, hydrogen exerted a neuroprotective effect against neuronal apoptosis and impaired nerve regeneration through activation of miR-21/PI3K/AKT/GSK-3β signalling in this in vitro model of traumatic brain injury.
- | bortezomib / Generic mfg.
Journal: Inhibition of PLK4 might enhance the anti-tumour effect of bortezomib on glioblastoma via PTEN/PI3K/AKT/mTOR signalling pathway. (Pubmed Central) - May 4, 2021
Similar phenomenon was observed using in vitro experiments. Thus, we speculate that PLK4 inhibition may be a new therapeutic strategy for GBM.
- | Journal: MiR-210-3p-EphrinA3-PI3K/AKT axis regulates the progression of oral cancer. (Pubmed Central) - May 4, 2021
The miR-210-3p-EphrinA3-PI3K/AKT signalling axis plays an important role in the progress of OSCC. EphrinA3 may serve as a novel target for oral cancer treatment.
- | Journal: Oncogenic gene RGC-32 is a direct target of miR-26b and facilitates tongue squamous cell carcinoma aggressiveness through EMT and PI3K/AKT signalling. (Pubmed Central) - May 4, 2021
SIGNIFICANCE OF THE STUDY: We first uncovered that Response Gene to Complement-32 played a significantly pro-tumorigenic role in tongue squamous cell carcinoma (TSCC), which was closely regulated by downregulation of miR-26b and activations of epithelial-mesenchymal transition process and PI3K/AKT signalling. These findings contribute to better understand the molecular mechanism in carcinogenesis of TSCC, and shed some light on promising strategy for TSCC therapeutics.
- || buparlisib (BKM120) / Novartis, Adlai Nortye
Clinical, Journal, Combination therapy: Buparlisib in combination with tamoxifen in pretreated patients with hormone receptor-positive, HER2-negative advanced breast cancer molecularly stratified for PIK3CA mutations and loss of PTEN expression. (Pubmed Central) - May 4, 2021
P2
Further biomarker-stratified studies with isoform-specific PI3K inhibitors are warranted. EudraCT No: 2014-000599-24.
- | Journal: Tubeimoside‑1 induces apoptosis in human glioma U251 cells by suppressing PI3K/Akt‑mediated signaling pathways. (Pubmed Central) - May 4, 2021
In addition, TBMS1 triggered apoptosis via the PI3K/Akt‑mediated Bcl‑2 signaling pathway. These results demonstrated that TBMS1 prevented the progression of gliomas via the PI3K/Akt‑dependent pathway, which provided a theoretical basis for in vivo studies to use TBMS1 as potential therapy for the prevention of cancer.
- | Journal: Stromal Cell-Contact Dependent PI3K and APRIL Induced NF-κB Signaling Prevent Mitochondrial- and ER Stress Induced Death of Memory Plasma Cells. (Pubmed Central) - May 4, 2021
APRIL signaling, by the nuclear factor κB (NF-κB) pathway, blocks activation of the endoplasmic-reticulum-stress-associated initiator caspase 12. Thus, stromal-cell-contact-induced PI3K and APRIL-induced NF-κB signaling provide the necessary and complementary signals to maintain bone marrow memory plasma cells.
- | Journal: HGF-MET Signaling Shifts M1 Macrophages Toward an M2-Like Phenotype Through PI3K-Mediated Induction of Arginase-1 Expression. (Pubmed Central) - May 4, 2021
Finally, HGF-MET signaling also shifted the M1 macrophage intracellular metabolism toward an M2 phenotype, especially with respect to fatty acid metabolism. Our results suggested that HGF treatment not only promotes regeneration in epithelial cells, but also leads to tissue repair by altering M1 macrophages to an M2-like phenotype.
- | Journal: miR‑181d promotes cell proliferation via the IGF1/PI3K/AKT axis in glioma. (Pubmed Central) - May 4, 2021
Furthermore, miR‑181d enhanced the growth of glioma xenografts in vivo, promoted cell cycle progression and suppressed cellular apoptosis within glioma xenograft tissues. Therefore, this newly identified miR‑181d/IGF1/PI3K/AKT axis may provide novel insights into the pathogenesis of glioma.
- | Journal: PI3K Driver Mutations: A Biophysical Membrane-Centric Perspective. (Pubmed Central) - May 4, 2021
We provide a structural view of hotspot and weak driver mutations in PI3Kα activation, explain their mechanisms, compare these with mechanisms of Raf activation, and point to targeting cell-specific, chromatin-accessible, and parallel (or redundant) pathways to thwart the expected emergence of drug resistance. Collectively, our biophysical outlook delineates activation and highlights the challenges of drug resistance.
- | CYH33 / HaiHe Biopharma
Journal: Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of advanced solid tumors. (Pubmed Central) - May 4, 2021
Western blot analysis confirmed that compound 37 could inhibit phosphorylation of AKT in human cancer cells to modulate the cellular PI3K/AKT/mTOR pathway. And further evaluation in vivo against SKOV-3 xenograft models demonstrated that a dose-dependent antitumor efficacy was achieved.
- | Journal: Double-Targeted Knockdown of miR-21 and CXCR4 Inhibits Malignant Glioma Progression by Suppression of the PI3K/AKT and Raf/MEK/ERK Pathways. (Pubmed Central) - May 4, 2021
The inhibition effect was strongest in double-targeted knockdown of miR-21 and CXCR4 group, whose downstream pathways involved in AKT axis and ERK axis activation. In conclusion, our findings reported that double-targeted knockdown of miR-21 and CXCR4 could more effectively inhibit the proliferation, migration, invasion, and growth of transplanted tumor and promote cell apoptosis, which were involved in the PI3K/AKT and Raf/MEK/ERK signaling pathways.
- | Journal: Phytochemicals in Chinese Chive (Allium tuberosum) Induce the Skeletal Muscle Cell Proliferation via PI3K/Akt/mTOR and Smad Pathways in C2C12 Cells. (Pubmed Central) - May 4, 2021
In particular, compound 1 down-regulated the Smad pathways, which are negative regulators of skeletal muscle growth. Collectively, we suggest that major constituents of Chinese chive, flavonoids and amino acids, might be used in dietary supplements that aid skeletal muscle growth.
- | quercetin (LY294002) / Eli Lilly
Journal: ATF4-mediated GDF15 suppresses LPS-induced inflammation and MUC5AC in human nasal epithelial cells through the PI3K/Akt pathway. (Pubmed Central) - May 4, 2021
Collectively, we suggest that major constituents of Chinese chive, flavonoids and amino acids, might be used in dietary supplements that aid skeletal muscle growth. Our data suggest that GDF15 is regulated by ATF4 and suppresses LPS-induced inflammation and MUC5AC in human nasal epithelial cells through the PI3K/Akt pathway.
- | Biomarker, Journal: E2F2 drives glioma progression via PI3K/AKT in a PFKFB4-dependent manner. (Pubmed Central) - May 4, 2021
Our data suggest that GDF15 is regulated by ATF4 and suppresses LPS-induced inflammation and MUC5AC in human nasal epithelial cells through the PI3K/Akt pathway. E2F2-mediated transcriptional enhancement of PFKFB4 expression regulated the phosphorylation of PI3K/AKT to promote glioma malignancy progression.
- | Preclinical, Journal: Estrogen cholestasis induces gut and liver injury in rats involving in activating PI3K/Akt and MAPK signaling pathways. (Pubmed Central) - May 4, 2021
EC induces liver inflammation, both gut and liver oxidative stress and apoptosis, involving in activating PI3K/Akt and MAPK signaling pathways. Investigation of EC-induced gut and liver injury contributes to the development of new potential therapeutic strategies.
- | Biomarker, Journal: GALNT2 promotes cell proliferation, migration, and invasion by activating the Notch/Hes1-PTEN-PI3K/Akt signaling pathway in lung adenocarcinoma. (Pubmed Central) - May 4, 2021
Investigation of EC-induced gut and liver injury contributes to the development of new potential therapeutic strategies. Our data confirmed the cancer-promoting effect of GALNT2, and might provide a new approach for LUAD therapy.
- | Journal, IO biomarker: Antagonistic effect of nano-selenium on hepatocyte apoptosis induced by DEHP via PI3K/AKT pathway in chicken liver. (Pubmed Central) - May 4, 2021
Nevertheless, the addition of nano-selenium can reverse the above changes. Experimental results revealed that nano-selenium antagonizes the toxic effects of DEHP via the PI3K/AKT pathway.
- || Review, Journal: PI3K/AKT Signal Pathway: A Target of Natural Products in the Prevention and Treatment of Alzheimer's Disease and Parkinson's Disease. (Pubmed Central) - May 4, 2021
This article reviews the relationship between AKT signaling pathway and AD and PD, and discusses the potential natural products based on the PI3K/AKT signaling pathway to treat two diseases in recent years, hoping to provide guidance and reference for this field. Further development of Chinese herbal medicine is needed to treat these two diseases.
- | Journal: Luteolin Ameliorates Experimental Pulmonary Arterial Hypertension via Suppressing Hippo-YAP/PI3K/AKT Signaling Pathway. (Pubmed Central) - May 4, 2021
In conclusion, luteolin ameliorated experimental PAH, which was at least partly mediated through suppressing HIPPO-YAP/PI3K/AKT signaling pathway. Therefore, luteolin might become a promising candidate for treatment of PAH.
- | Journal: Id4 Suppresses the Growth and Invasion of Colorectal Cancer HCT116 Cells through CK18-Related Inhibition of AKT and EMT Signaling. (Pubmed Central) - May 4, 2021
Collectively, our study indicated Id4 may inhibit CRC growth and metastasis through inhibiting the PI3K/AKT pathway in a CK18-dependent manner and suppressing EMT. Id4 may become a target for the treatment of CRC.
- | quercetin (LY294002) / Eli Lilly
Journal: PHLDA3 inhibition attenuates endoplasmic reticulum stress-induced apoptosis in myocardial hypoxia/reoxygenation injury by activating the PI3K/AKT signaling pathway. (Pubmed Central) - May 4, 2021
An H/R injury model was constructed by treatment with hypoxia for 4 h followed by reoxygenation for 6 h. A PI3K/AKT inhibitor, LY294002, was supplemented in mechanistic studies...In conclusion, in the process of H/R injury, PHLDA3 inhibition reduced ERS-induced apoptosis and H/R injury by activating the PI3K/AKT pathway. PHLDA3 may be a therapeutic target for the treatment of MIRI.
- || Missed PI3K in that line. (Twitter) - May 1, 2021
- | Preclinical, Journal: Cornel Iridoid Glycoside Improves Cognitive Impairment Induced by Chronic Cerebral Hypoperfusion via Activating PI3K/Akt/GSK-3β/CREB Pathway in Rats. (Pubmed Central) - May 1, 2021
Collectively, CIG treatment improved learning and memory deficit induced by chronic cerebral hypoperfusion via increasing neurotrophic factors thus protecting glutamate receptors and activating PI3K/Akt/GSK3β/CREB signaling pathway in rats. These results suggest that CIG may be beneficial to VaD therapy.
- | Journal: NGF from pancreatic stellate cells induces pancreatic cancer proliferation and invasion by PI3K/AKT/GSK signal pathway. (Pubmed Central) - May 1, 2021
What's more, NGF/TrkA regulates the PC cell proliferation and invasion via activation of PI3K/AKT/GSK signalling. The present study demonstrated NGF/TrkA promoted the PC cell proliferation and invasion in the co-culture system by the activation of the PI3K/AKT/GSK signal cascade, providing a potential therapeutic target for PC patients.
- || Copiktra (duvelisib) / Secura Bio, Yakult Honsha
Clinical, P1/2 data, Journal, Combination therapy: A phase 1b/2 study of duvelisib in combination with FCR (DFCR) for frontline therapy for younger CLL patients. (Pubmed Central) - May 1, 2021
DFCR is active as initial therapy of younger CLL patients. Immune-mediated and infectious toxicities occurred and required active management.
- | Preclinical, Journal: Inhibition of PI3Kγ by AS605240 plus low-dose tissue plasminogen activator (tPA) combination improves thrombolytic therapy in a rat model of embolic stroke. (Pubmed Central) - May 1, 2021
Finally, AS605240 plus low-dose tPA combination improved long-term outcome for at least 35 days after stroke compared with the saline-treated group. Taken together, these findings suggest that PI3Kγ inhibition with AS605240 might act as an adjunct approach for enhancing tPA thrombolytic efficacy in acute ischemic stroke.
- | Journal: Astaxanthin suppresses lipopolysaccharide‑induced myocardial injury by regulating MAPK and PI3K/AKT/mTOR/GSK3β signaling. (Pubmed Central) - May 1, 2021
Furthermore, the treatment with ATX suppressed the LPS‑activated MAPK and PI3K/AKT signaling. ATX additionally exerted a protective effect on cardiac dysfunction caused by sepsis by inhibiting MAPK and PI3K/AKT signaling.
- | Journal: Long noncoding RNA Nespas inhibits apoptosis of epileptiform hippocampal neurons by inhibiting the PI3K/Akt/mTOR pathway. (Pubmed Central) - May 1, 2021
This report explored the function and regulatory mechanism of Nespas in epileptiform hippocampal neurons for the first time. Our findings revealed that Nespas suppressed the apoptosis of epileptiform hippocampal neurons by inhibiting the PI3K/Akt/mTOR pathway via upregulation of Psmd11 at a miR-615-3p dependent way, indicating that Nespas may offer a new direction for the treatment of epilepsy.
- | Journal: Plasminogen activator Inhibitor-2 inhibits pulmonary arterial smooth muscle cell proliferation in pulmonary arterial hypertension via PI3K/Akt and ERK signaling. (Pubmed Central) - May 1, 2021
PAI-2 attenuates PAH development by suppressing hPASMCs proliferation via the inhibition of PI3K/Akt and ERK pathways. PAI-2 may serve as a potential biomarker and therapeutic target for PAH.
- || Zydelig (idelalisib) / Gilead
Clinical, Journal: No increased bleeding events in patients with relapsed chronic lymphocytic leukemia and indolent non-Hodgkin lymphoma treated with idelalisib. (Pubmed Central) - May 1, 2021
P2, P3
The advent of novel B-cell receptor pathway targeting agents like ibrutinib dramatically changed management of B-cell malignancies...Data from two idelalisib trials (rituximab ± idelalisib in chronic lymphocytic leukemia [CLL] and idelalisib monotherapy in indolent non-Hodgkin lymphoma [iNHL]) were analyzed...Hemorrhagic risk is prevalent in these patients and an important consideration when evaluating available treatment options. ClinicalTrials.gov identifiers: NCT01539512 and NCT01282424.
- | Journal: Cancer/testis antigen LDHC promotes proliferation and metastasis by activating the PI3K/Akt/GSK-3β-signaling pathway and the in lung adenocarcinoma. (Pubmed Central) - May 1, 2021
PI3K inhibition also reversed cell proliferation-related and EMT-related proteins in LDHC-overexpressing A549 cells. In conclusion, LDHC promotes proliferation, migration, invasion, and EMT in LUAD cells via activation of the PI3K/Akt/GSK-3β pathway.
- | buparlisib (BKM120) / Novartis, Adlai Nortye, Lynparza (olaparib) / Merck (MSD), AstraZeneca
Journal: Discovery of novel PARP/PI3K dual inhibitors with high efficiency against BRCA-proficient triple negative breast cancer. (Pubmed Central) - May 1, 2021
Furthermore, compound 12 displayed good metabolic stability and high safety. Taken together, these results suggest that compound 12 as a novel PARP/PI3K dual inhibitor is worthy for further study.
- | omipalisib (GSK2126458) / GSK
Journal: Omipalisib inspired macrocycles as dual PI3K/mTOR inhibitors. (Pubmed Central) - May 1, 2021
Among them, MCX 83 presented remarkable selectivity against a panel of 468 kinases, high in vitro metabolic stability, and favorable pharmacokinetic parameters without significant CYP450 and h-ERG binding inhibition. This profile qualified this compound as a suitable candidate for future in vivo PK-PD and efficacy studies in mouse cancer models.
- | omipalisib (GSK2126458) / GSK
Preclinical, Journal: Structural optimization towards promising β-methyl-4-acrylamido quinoline derivatives as PI3K/mTOR dual inhibitors for anti-cancer therapy: The in vitro and in vivo biological evaluation. (Pubmed Central) - May 1, 2021
Besides, 14d displayed comparable anti-proliferative activity against both PC3 and U87MG cell lines to that of the positive reference GSK2126458 with respective GI value of 0.36 and 0.14 μM...Meanwhile, no overt loss of body weight was observed in the 14d-treated groups. Taken together, 14d, by virtue of its attractive performance, merits further development as a potential anti-tumor candidate.
- | doxorubicin hydrochloride / Generic mfg.
Journal, IO biomarker: Cardiac Protective Effect of Kirenol against Doxorubicin-Induced Cardiac Hypertrophy in H9c2 Cells through Nrf2 Signaling via PI3K/AKT Pathways. (Pubmed Central) - May 1, 2021
As a result, KRL is considered a potential agent against hypertrophy resulting from cardiac deterioration. The study results show that KRL not only activates the IGF-IR-dependent p-PI3K/p-AKT and Nrf2 signaling pathway, but also suppresses caspase-dependent apoptosis.
- | quercetin (LY294002) / Eli Lilly
Journal: Curcuma amarissima Extract Activates Growth and Survival Signal Transduction Networks to Stimulate Proliferation of Human Keratinocyte. (Pubmed Central) - May 1, 2021
Specifically, the CA-induced increase of cell monolayer wound healing was blocked by the MEK inhibitor (U0126) or the PI3K inhibitor (LY294002)...Taken together, our study provided convincing evidence that Curcuma amarissima can promote proliferation and survival of human keratinocyte through stimulating the MAPK and PI3K/Akt signaling cascades. These promising data emphasize the possibility to develop this plant as a wound healing agent for the potential application in regenerative medicine.
- | Journal: Novel Single Inhibitor of HDAC6/8 and Dual Inhibitor of PI3K/HDAC6 as Potential Alternative Treatments for Prostate Cancer. (Pubmed Central) - May 1, 2021
LASSBio-1911 and LASSBio-2208 demonstrated significant activity in reducing cell viability and migration. These compounds can be further used as prototypes for the development of new potential anticancer alternative treatments.
- | Preclinical, Journal: Ecklonia cava Extract and Its Derivative Dieckol Promote Vasodilation by Modulating Calcium Signaling and PI3K/AKT/eNOS Pathway in In Vitro and In Vivo Models. (Pubmed Central) - May 1, 2021
In conclusion, our findings suggest that dieckol modulates calcium transit through AchM3R, increases endothelial-dependent NO production, and efficiently enhances vasodilation. Thus, E. cava and its derivative, dieckol, can be considered as potential natural vasodilators.
- | bardoxolone methyl (RTA 402) / Kyowa Hakko Kirin, Reata
Preclinical, Journal: CDDO-Me Attenuates Astroglial Autophagy via Nrf2-, ERK1/2-SP1- and Src-CK2-PTEN-PI3K/AKT-Mediated Signaling Pathways in the Hippocampus of Chronic Epilepsy Rats. (Pubmed Central) - May 1, 2021
In addition, CDDO-Me ameliorated spontaneous seizure duration, but not seizure frequency and behavioral seizure severity. Therefore, our findings suggest that clasmatodendrosis may affect seizure duration in chronic epilepsy rats, and that CDDO-Me may attenuate autophagic astroglial degeneration by regulating various signaling pathways.
- | quercetin (LY294002) / Eli Lilly
Journal: Neuroprotective Effects of Salicin in a Gerbil Model of Transient Forebrain Ischemia by Attenuating Oxidative Stress and Activating PI3K/Akt/GSK3β Pathway. (Pubmed Central) - May 1, 2021
Notably, the neuroprotective effect of salicin was abolished by LY294002. Taken together, these findings clearly indicate that salicin protects against ischemic brain injury by attenuating oxidative stress and activating the PI3K/Akt/GSK3β pathway.
- | Journal: Mingmu Xiaomeng Tablets Restore Autophagy and Alleviate Diabetic Retinopathy by Inhibiting PI3K/Akt/mTOR Signaling. (Pubmed Central) - May 1, 2021
MMXM decreased GFAP expression in retinal Müller cells; restored electrophysiology indexes and retinal ultrastructures; and reduced serum levels of interleukin (IL)-1β, IL-4, IL-6, tumor necrosis factor-α, and vascular endothelial growth factor. MMXM may protect the diabetic retina by inhibiting PI3K/Akt/mTOR signaling and enhancing autophagy.
- | Preclinical, Journal: Neuroprotective Effects of Oxymatrine on PI3K/Akt/mTOR Pathway After Hypoxic-Ischemic Brain Damage in Neonatal Rats. (Pubmed Central) - May 1, 2021
However, these protective effects against HIBD could be suppressed when rapamycin, a specific inhibitor of mTOR, was included. Hence, the OMT exerted neuroprotective effects against HIBD by attenuating excessive autophagy by mediating the PI3K/Akt/mTOR pathway.
- | Journal: MicroRNA-191-5p promotes the development of osteosarcoma via targeting EGR1 and activating the PI3K/AKT signaling pathway. (Pubmed Central) - May 1, 2021
The Publisher apologizes for any inconvenience this may cause. https://www.europeanreview.org/article/17783.
- [VIRTUAL] Cardiac Phosphoinositide 3-Kinase (P110Α) as a Therapeutic Target for Diabetic Cardiomyopathy - An AAV-Mediated Gene Therapy Approach () - Apr 30, 2021 - Abstract #ASGCT2021ASGCT_978;
- [VIRTUAL] Cochlioquinone Derivative CoB1 Induces Cytostatic Autophagy of Lung Cancer through miRNA-125b and Foxp3 () - Apr 30, 2021 - Abstract #ASGCT2021ASGCT_528;
As showed in Graphic 2, CoB1, on the one hand, inhibited PI3K/Akt/mTOR axis, on the other hand, induced the expression of miR-125b by activating TAK1/ MKK4/ JNK/ Smad axis, thereby reducing Foxp3 expression. Through the combined effect of these two aspects, CoB1 induced cell autophagy and promoted A549 lung cancer cells death.
- [VIRTUAL] Insulin Resistance Negatively Impacts Early rAAV Transduction Events () - Apr 30, 2021 - Abstract #ASGCT2021ASGCT_310;
Insulin resistant cells and mice have a reduced quantity of insulin receptors and therefor have reduced uptake. Another potential factor for increased gene expression lies within the insulin receptor signaling cascade as shown by the potent effects of inhibiting GSK3.
- | Journal: Defining How Oncogenic and Developmental Mutations of PIK3R1 Alter the Regulation of Class IA Phosphoinositide 3-Kinases. (Pubmed Central) - Apr 30, 2021
In addition, we find that the R649W mutation in the cSH2 of PIK3R1 decreases sensitivity to activation by receptor tyrosine kinases. This work reveals unique insight into isoform-specific regulation of p110s by p85α.
- || Review, Journal: The PI3K/AKT/mTOR signaling pathway in osteoarthritis: a narrative review. (Pubmed Central) - Apr 30, 2021
This review highlights the role of PI3K/AKT/mTOR signaling in cartilage degradation, subchondral bone dysfunction, and synovial inflammation, and discusses how this signaling pathway affects development of the disease. We also summarize recent evidences of therapeutic approaches to treat OA by targeting the PI3K/AKT/mTOR pathway, and discuss potential challenges in developing these strategies for clinical treatment of OA.