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- | Journal: NLRP6 potentiates PI3K/AKT signalling by promoting autophagic degradation of p85? to drive tumorigenesis. (Pubmed Central) - Sep 28, 2023
degradation via selective autophagy to drive tumorigenesis, and the interaction between NLRP6 and p85? can be a promising therapeutic target for tumour treatment.
- | LY294002 / Eli Lilly
Preclinical, Journal: Unleashing lactoferrin's antidepressant potential through the PI3K/Akt/mTOR pathway in chronic restraint stress rats. (Pubmed Central) - Sep 28, 2023
Interestingly, LF therapy significantly improved CRS-induced behavioral and biochemical aberrations, an effect which was suppressed upon pretreatment with LY294002 (PI3K inhibitor)...Furthermore, LF succeeded in restoring 5-HT and corticosterone levels, diminishing oxidative stress and ameliorating the inflammatory cascades. Therefore, and for the first time, LF might serve as a promising antidepressant drug through targeting the PI3K/Akt/mTOR pathway.
- | Journal: Myeloid-specific knockout of SHP2 regulates PI3K/PLC? signaling pathway to protect against early myocardial infarction injury. (Pubmed Central) - Sep 28, 2023
Myeloid-specific knockout of SHP2 regulates PI3K/PLC? signaling pathway to protect against early myocardial infarction injury.
- | Journal: Theabrownin from Dark Tea Ameliorates Insulin Resistance via Attenuating Oxidative Stress and Modulating IRS-1/PI3K/Akt Pathway in HepG2 Cells. (Pubmed Central) - Sep 28, 2023
Treatment with the PI3K inhibitor demonstrated a favorable correlation between PI3K activation and TB action on glycolipid metabolism. Notably, we observed that TB2 had a greater effect on improving insulin resistance compared with TB1, which, due to its prolonged fermentation time, increased the degree of oxidative polymerization of TB.
- | LY294002 / Eli Lilly, PD98059 / Wayne State University
Preclinical, Journal: Cerebroprotective Effect of 17?-Estradiol Replacement Therapy in Ovariectomy-Induced Post-Menopausal Rats Subjected to Ischemic Stroke: Role of MAPK/ERK1/2 Pathway and PI3K-Independent Akt Activation. (Pubmed Central) - Sep 28, 2023
Thus, these results suggested that E2 pretreatment in ovariectomized female rats modulates MAPK/ERK1/2 and activates Akt independently of PI3K to promote cerebroprotection in ischemic stroke. A better understanding of the mechanisms and the influence of E2 in the female sex paves the way for the design of future successful hormone replacement therapies.
- | Journal: Piperine Induces Apoptosis and Autophagy in HSC-3 Human Oral Cancer Cells by Regulating PI3K Signaling Pathway. (Pubmed Central) - Sep 28, 2023
We also confirmed that piperine inhibits oral cancer tumor growth in vivo via antitumor effects related to apoptosis and PI3K signaling pathway inhibition. Therefore, we suggest that piperine can be considered a natural anticancer agent for human oral cancer.
- | tamoxifen / Generic mfg.
Biomarker, Journal, PD(L)-1 Biomarker, IO biomarker: The immune microenvironment characterisation and dynamics in hormone receptor-positive breast cancer before and after neoadjuvant endocrine therapy. (Pubmed Central) - Sep 28, 2023
NET influences the composition and functional state of the infiltrating immune cells. Furthermore, changes in the immune microenvironment are also associated with treatment response.
- || Rituxan (rituximab) / Biogen, Zenyaku Holdings, Roche
Review, Journal, IO biomarker: Targeted Therapy in Follicular Lymphoma: Towards a Chemotherapy-Free Approach. (Pubmed Central) - Sep 28, 2023
Targeted therapies represent a paradigm shift in the treatment of FL. Further studies are needed to directly compare these targeted therapies and their combinations, as well as to investigate biomarkers predictive of response.
- Kadcyla (ado-trastuzumab emtansine) / Roche, Enhertu (fam-trastuzumab deruxtecan-nxki) / Daiichi Sankyo, AstraZeneca
Upregulation of metabolism enzymes mediatesADC resistance in a HER2-positive cancer cell line (Exhibit Hall B) - Sep 27, 2023 - Abstract #SITC2023SITC_1464;
Conclusions In this study, we established an Enhertu resistant N87 cell line and investigated the mechanism of drug resistance. Our results showed increased expression of HER2 downstream signals containing PI3K-AKT signal and MAPK signal lead to resistance of N87-R cells and inhibition of PI3K signal or MAPK signal reversed the resistance of tumor cells both in vitro and in vivo.
- PIK3IP1/TrIP immune regulation on CD8+ T cells restricts anti-tumor immunity (Exhibit Hall B) - Sep 27, 2023 - Abstract #SITC2023SITC_1334;
Our results showed increased expression of HER2 downstream signals containing PI3K-AKT signal and MAPK signal lead to resistance of N87-R cells and inhibition of PI3K signal or MAPK signal reversed the resistance of tumor cells both in vitro and in vivo. Our affinity stimulation studies suggest TrIP
- | Journal: Identification of phytochemical as a dual inhibitor of PI3K and mTOR: a structure-based computational approach. (Pubmed Central) - Sep 26, 2023
Therefore, the present study identifies new molecules and provides evidence for salvianolic acid A for dual inhibition. Further experiments must be performed both in vitro and in vivo to support the predictions of these computational tools.
- | LY294002 / Eli Lilly
Journal: Osteopontin promotes gastric cancer progression via phosphatidylinositol-3-kinase/protein kinase B/mammalian target of rapamycin signaling pathway. (Pubmed Central) - Sep 25, 2023
These results suggested that OPN though PI3K/AKT/mammalian target of rapamycin signal pathway to up-regulate MMP-2 and VEGF expression, which contribute SGC-7901 cells to proliferation, invasion and migration. Thus, our results demonstrate that OPN may serve as a novel prognostic biomarkers as well as a potential therapeutic targets for GC.
- | Journal: Sanguisorba officinalis ethyl acetate extract attenuates ulcerative colitis through inhibiting PI3K-AKT/NF-?B/ STAT3 pathway uncovered by single-cell RNA sequencing. (Pubmed Central) - Sep 25, 2023
Thus, our results demonstrate that OPN may serve as a novel prognostic biomarkers as well as a potential therapeutic targets for GC. By integrating the chemical information of SOEA derived from UPLC-Q-Orbitrap-HRMS with single-cell transcriptomic data extracted from scRNA-seq, this study demonstrates that SOEA exerts the therapeutic effect through suppressing PI3K-AKT/NF-B/STAT3 pathway to improve clinical symptoms, inflammatory response, mucosal barrier, and intercellular interactions in UC, and effectively eliminates the interference of cellular heterogeneity.
- | Journal, IO biomarker: Silencing POLE2 promotes apoptosis and inhibits proliferation of oral squamous cell carcinomas by inhibiting PI3K/AKT signaling pathway. (Pubmed Central) - Sep 25, 2023
In addition, POLE2 regulates OSCC progression by inhibiting the PI3K/AKT pathway. POLE2 is closely related to the progression of OSCC, and POLE2 may be a potential target for OSCC treatment.
- || Imjudo (tremelimumab) / AstraZeneca, Pfizer, Erleada (apalutamide) / J&J, Farxiga (dapagliflozin) / Ono Pharma, AstraZeneca
Clinical, Observational data, Retrospective data, Review, Clinical Trial,Phase II, Journal, Checkpoint inhibition: Immune checkpoint inhibitor- and phosphatidylinositol-3-kinase inhibitor-related diabetes induced by antineoplastic drugs: two case reports and a literature review. (Pubmed Central) - Sep 25, 2023
Case 2 was diagnosed with PI3Ki-related diabetes mellitus, and her blood glucose level returned to normal with the use of metformin and dapagliflozin. We systematically searched the PubMed database for articles on ICI- and PI3Ki-related diabetes mellitus and characterized the differences in clinical features and treatment between these two forms of diabetes.
- | Preclinical, Journal, IO biomarker: Parthenolide repressed endometriosis induced surgically in rats: Role of PTEN/PI3Kinase/AKT/GSK-3?/?-catenin signaling in inhibition of epithelial mesenchymal transition. (Pubmed Central) - Sep 25, 2023
Our findings showed that parthenolide in a dose dependent manner inhibited PI3K/AKT/GSK-3?/n?-catenin cascade via enhancement of PTEN with subsequent inhibition of EMT evidenced by elevation of the epithelial marker, E-cadherin and reduction of mesenchymal marker, vimentin, of the endometriotic implants in addition to reversal of invasion and migration properties of epithelial endometriotic cell lines. These findings provide a valuable therapeutic approach for treatment of endometriosis.
- | GLG-302 / GLG Pharma
Preclinical, Journal: Ciliary neurotrophic factor stimulates stem/progenitor Leydig cell proliferation but inhibits differentiation into its lineage in rats. (Pubmed Central) - Sep 25, 2023
These findings provide a valuable therapeutic approach for treatment of endometriosis. Ciliary neurotrophic factor stimulates proliferation but blocks the differentiation of stem/progenitor Leydig cells.
- Patient Selection and Sequencing of New and Emerging Options For R/R FL: PI3K Inhibitors (Marriott Marquis San Diego Marina, Pacific Ballroom Salons 18-19; Virtual) - Sep 23, 2023 - Abstract #ASH2023ASH_491;
Supported by Educational grants from Genentech, a member of the Roche Group; Genmab; Ipsen Biopharmaceuticals, Inc; and Regeneron Pharmaceuticals, Inc. Provided by Clinical Care Options, LLC.
- Clinical Impact of PTEN as a Marker for Diabetes-Associated Osteoarthritis (Poster Hall; in person) - Sep 23, 2023 - Abstract #ACRConvergence2023ACR_Convergence_2977;
Further studies of this homeostasis mechanism in OA associated to diabetes might elucidate its relevance in the progression of disease. 1.
- | Journal, PD(L)-1 Biomarker, IO biomarker: Platycodin D induces neutrophil apoptosis by downregulating PD-L1 expression to inhibit breast cancer pulmonary metastasis. (Pubmed Central) - Sep 23, 2023
In conclusion, the administration of PlaD inhibited the PI3K/Akt signaling pathway by reducing the expression of PD-L1 in neutrophils. PlaD promoted neutrophil apoptosis, thereby inhibiting the establishment of a premetastatic niche and ultimately blocking the development of pulmonary metastasis.
- | Journal: Network pharmacology and experimental verification reveal the mechanism of safranal against glioblastoma (GBM). (Pubmed Central) - Sep 22, 2023
In vivo experiments showed that safranal could inhibit GBM cell growth alone and in combination with TMZ. This study revealed that safranal inhibits GBM cell growth in vivo and in vitro, promotes GBM cell apoptosis and G2/M phase arrest, inhibits the PI3K/AKT/mTOR axis and cooperate with TMZ.
- | Caprelsa (vandetanib) / Sanofi
Journal, Cancer stem: Vandetanib alters the tumoricidal capacity of human breast cancer stem cells via inhibiting vasculogenic capacity. (Pubmed Central) - Sep 22, 2023
This study revealed that safranal inhibits GBM cell growth in vivo and in vitro, promotes GBM cell apoptosis and G2/M phase arrest, inhibits the PI3K/AKT/mTOR axis and cooperate with TMZ. The concurrent treatment (PI3K, inhibitor+ 1, 5
- | Journal: New Horizons in Cancer Treatment: A Closer Look at Novel PI3K? Inhibitors. (Pubmed Central) - Sep 22, 2023
Future research promises innovative therapeutic strategies targeting PI3K in managing cancer, aging, and neurodegenerative diseases. This Patent Highlight showcases compounds and compositions that may enlarge the PI3K inhibitory therapeutic window-effectively inhibiting the target in cancer cells while reducing toxicity in patients.
- NCI60 HTS384: The next phase of the NCI60 screen (Level 2, Exhibit Hall D) - Sep 22, 2023 - Abstract #AACRNCIEORTC2023AACR_NCI_EORTC_678;
- The Protective Effects of Ang-(1-7) on Myocardial I/r Injury Through Depression Endoplasmic Reticulum Stress (Zone 1, Science and Technology Hall, Level 2) - Sep 21, 2023 - Abstract #AHA2023AHA_8334;
Ang-(1-7) improves SERCA activity, maintains cellular calcium homeostasis, inhibits ERS and reduces ERS-induced apoptosis by activating the PI3K/Akt pathway, and acts through the Mas receptor. Ang-(1-7) exerts a protective effect on MIRI and may provide a new way to effectively prevent MIRI.
- | LY294002 / Eli Lilly
Journal, PARP Biomarker: Pseudolaric acid B induces apoptosis associated with the mitochondrial and PI3K/AKT/mTOR pathways in triple?negative breast cancer. (Pubmed Central) - Sep 19, 2023
Overall, the present results demonstrated that PAB induced apoptosis via mitochondrial apoptosis and the PI3K/AKT/mTOR pathway in triple?negative breast cancer. It also inhibited cellular proliferation, migration and invasion, suggesting that PAB may be a useful phytomedicine for the treatment of triple?negative breast cancer.
- | Journal: Nrf3 promotes the proliferation and migration of triple?negative breast cancer by activating PI3K/AKT/mTOR and epithelial?mesenchymal transition. (Pubmed Central) - Sep 18, 2023
Furthermore, PI3K inhibitors partially decreased the proliferation and migration of the Nrf3 overexpressing TNBC cells. In conclusion, Nrf3 enhances cellular proliferation and migration by activating PI3K/AKT/mTOR signaling pathways, highlighting a novel therapeutic target for TNBC.
- | pentylenetetrazole (BTD-001) / Balance Therap, Copiktra (duvelisib) / Secura Bio, Yakult Honsha
Preclinical, Journal: Effect of Duvelisib, a Selective PI3K Inhibitor on Seizure Activity in Pentylenetetrazole-Induced Convulsions Animal Model. (Pubmed Central) - Sep 18, 2023
The results showed that pretreatment with DUV prolonged the seizure stages according to the Racine scale, significantly decreased the duration of general tonic-clonic seizure and reduced the number of myoclonic jerks (P?<?.05). In conclusion, we found that PI3K antagonist DUV significantly reduced PTZ-induced seizures, indicating that DUV exerts an anticonvulsant effect by inhibiting PI3K signaling pathway.
- | Preclinical, Journal: Meroterpenoids from Daphne genkwa shows promising in vitro antitumor activity via inhibiting PI3K/Akt/mTOR signaling pathway in A549 cells. (Pubmed Central) - Sep 18, 2023
Subsequent in vitro antitumor evaluation of 8a disclosed that it could inhibit the proliferation and metastasis, as well as induce significant apoptosis and cycle arrest, of A549 cells. Further mechanistic investigations revealed that 8a could exert its antitumor activity via inhibiting the PI3K/Akt/mTOR signaling pathway.
- | Journal: Design, synthesis, and biological evaluation of novel bivalent PI3K inhibitors for the potential treatment of cancer. (Pubmed Central) - Sep 18, 2023
Furthermore, compound 27 shows dose-dependent anticancer efficacies in a HGC-27 xenograft mice model. Overall, this work provides a possible strategy to discover novel PI3K inhibitors for the treatment of cancers.
- | Journal: Discovery of (S)-N-(thiazol-2-yl) pyrrolidine-1,2-dicarboxamide derivatives targeting PI3K?/HDAC6 for the treatment of cancer. (Pubmed Central) - Sep 18, 2023
Attributed to its favorable in vitro performance, 21j has the potential to alleviate the adverse effects resulted from pan-PI3K inhibition and pan-HDAC inhibition. It is valuable for further functional investigation as an anti-cancer agent.
- | Preclinical, Journal: Discovery of a Photosensitizing PI3K Inhibitor for Tumor Therapy: Design, Synthesis and in vitro Biological Evaluation. (Pubmed Central) - Sep 18, 2023
In biological assessment, FD2157 exhibited remarkably enhanced anticancer activity in inhibition of PI3K pathway against melanoma cell lines upon light irradiation (4 min). Hence, this photosensitive PI3K inhibitor FD2157 may represent a valuable tool compound for studying the PI3K pathway and further optimization toward light-triggered cancer treatment.
- | buparlisib (AN2025) / Novartis, Adlai Nortye, seliciclib (CYC202) - Cyclacel, Cedars / Sinai
Journal: Discovery and identification of a novel PI3K inhibitor with enhanced CDK2 inhibition for the treatment of triple negative breast cancer. (Pubmed Central) - Sep 18, 2023
Hence, this photosensitive PI3K inhibitor FD2157 may represent a valuable tool compound for studying the PI3K pathway and further optimization toward light-triggered cancer treatment. Moreover, FD2056 showed more efficacious anti-TNBC activity than the corresponding drugs BKM120 and CYC202 at an oral dose of 15
- | OP-11 / Ohara Pharma
Journal: Structure-based drug design, synthesis, and biological evaluation of novel 1,3,5-triazine or pyrimidine derivatives containing benzoyl hydrazine moiety as PI3K? selective inhibitors. (Pubmed Central) - Sep 18, 2023
Here, we described a series of PI3K? inhibitors with 1,3,5-triazine or pyrimidine skeleton containing benzoyl hydrazine based on the pan-PI3K inhibitor ZSTK474 relying on the strategies of structure-based drug discovery (SBDD) and computer-aided drug design (CADD)...Furthermore, compound F8 induced significant tumor regressions in a xenograft mouse model of U87-MG cell line with no clear evidence of toxicity following intraperitoneal injection of 40
- | LY294002 / Eli Lilly
Journal, PARP Biomarker, IO biomarker: Root extract of Hemsleya amabilis Diels suppresses renal cell carcinoma cell growth through inducing apoptosis and G/M phase arrest via PI3K/AKT signaling pathway activation. (Pubmed Central) - Sep 18, 2023
In addition, HRE inhibited proliferation through promoting apoptosis and P21-induced G/M phase arrest via PI3K/AKT signaling pathway. Overall, these results suggest that HRE may be a promising chemotherapy agent for RCC.
- | Calquence (acalabrutinib) / AstraZeneca, Imbruvica (ibrutinib) / AbbVie, J&J
Journal: BCR/integrin interaction in CLL: a physiological remnant with clinical relevance. (Pubmed Central) - Sep 18, 2023
Despite BTK inhibition, VLA-4 remains inside-out activated via BCR, an activation dampened by PI3K-inhibitors. Evaluation of CD49d expression in patients starting BTK-inhibitor therapy may improve their prognostic stratification.
- || Review, Journal: Phosphoinositide 3-kinase as a therapeutic target in angiogenic disease. (Pubmed Central) - Sep 16, 2023
Herein, we summarize the molecular mechanism of PI3K inhibitors in preventing the permeability of vessels and neovascularization. Additionally, we briefly illustrate how PI3K signaling modulates blood vessel growth and discuss the different roles that PI3K isoforms play in angiogenesis.
- | bile acid cholic acid (INT-777) / Intercept
Journal: G protein-coupled bile acid receptor 1 reduced hepatic immune response and inhibited NF?B, PI3K/AKT and PKC/P38 MAPK signaling pathway in hybrid grouper. (Pubmed Central) - Sep 16, 2023
INT-777 agonist significantly decreased the expression of phosphorylated phosphoinositide 3-kinase (p-PI3K) protein and the ratio of phosphorylated and non-phosphorylated serine/threonine-protein kinase (p-AKT/AKT). In conclusion, activation of hepatic TGR5 inhibited the PKC/P38 MAPK, PI3K/AKT, NF?B signaling pathway, and improved hepatic immune responses of hybrid grouper in vivo and in vitro.
- | Journal: Proanthocyanidin enhances the endogenous regeneration of alveolar bone by elevating the autophagy of PDLSCs. (Pubmed Central) - Sep 16, 2023
In conclusion, activation of hepatic TGR5 inhibited the PKC/P38 MAPK, PI3K/AKT, NF?B signaling pathway, and improved hepatic immune responses of hybrid grouper in vivo and in vitro. PA may activate autophagy by inhibiting PI3K/Akt/mTOR signaling pathway to promote the osteogenesis of PDLSCs and enhance endogenous alveolar bone regeneration.
- MEN1703 / Menarini
MEN1703/ SEL24, a potent PIM inhibitor, demonstrates promising anti-tumour activity in activated B cell like diffuse large B cell lymphoma, mantle cell lymphoma and marginal zone lymphoma cells. (LEVEL 2, EXHIBIT HALL D) - Sep 16, 2023 - Abstract #AACRNCIEORTC2023AACR_NCI_EORTC_632;
- Combinations of PI3K inhibitors with targeted oncology agents in multicellular spheroid models. (LEVEL 2, EXHIBIT HALL D) - Sep 16, 2023 - Abstract #AACRNCIEORTC2023AACR_NCI_EORTC_537;
- roginolisib (IOA-244) / iOnctura
A pharmacologic screen identifies drugs to be combined with the non-ATP competitive PI3K? inhibitor roginolisib (IOA-244) for an improved anti-tumor activity in lymphoma models. (LEVEL 2, EXHIBIT HALL D) - Sep 16, 2023 - Abstract #AACRNCIEORTC2023AACR_NCI_EORTC_483;
- KO-2806 / Kura Oncology
The next-generation farnesyltransferase inhibitor KO-2806 constrains compensatory signaling reactivation to deepen responses to KRASG12D inhibition. (LEVEL 2, EXHIBIT HALL D) - Sep 16, 2023 - Abstract #AACRNCIEORTC2023AACR_NCI_EORTC_349;
- Fyarro (nanoparticle albumin-bound rapamycin) / Aadi Biosci
Evaluation of nab-sirolimus in combination with PI3K pathway inhibitors to overcome PI3K/mTOR resistance in PI3K-mutant breast cancer cell lines. (LEVEL 2, EXHIBIT HALL D) - Sep 16, 2023 - Abstract #AACRNCIEORTC2023AACR_NCI_EORTC_271;
- batoprotafib (TNO155) / Novartis
RAS mutation status predicts activity of the SHP2 inhibitor TNO155 in RAS-pathway driven fusionnegative rhabdomyosarcoma. (LEVEL 2, EXHIBIT HALL D) - Sep 16, 2023 - Abstract #AACRNCIEORTC2023AACR_NCI_EORTC_251;
- iadademstat (ORY-1001) / Oryzon
The LSD1 inhibitor iadademstat shows preclinical efficacy in malignant peripheral nerve sheath tumor cells and synergistic effects in combination. (LEVEL 2, EXHIBIT HALL D) - Sep 16, 2023 - Abstract #AACRNCIEORTC2023AACR_NCI_EORTC_220;
- | Journal: Fat body-specific reduction of CTPS alleviates HFD-induced obesity. (Pubmed Central) - Sep 15, 2023
Furthermore, a dominant-negative form of CTPS also prevented adipocyte expansion and downregulated lipogenic genes. These findings not only establish a functional link between CTPS and lipid homeostasis but also highlight the potential role of CTPS manipulation in the treatment of HFD-induced obesity.
- | Journal: Thymocyte selection-associated high mobility box protein regulates T lymphocytes exhaustion in patients with myelodysplastic syndromes by inhibiting PI3K/AKT/mTOR pathway. (Pubmed Central) - Sep 15, 2023
Moreover, the knockdown of TOX using si-RNA in Jurkat cells improved cell proliferation activity, down-regulated IRs and activated PI3K/AKT/mTOR signaling pathway. TOX promotes the exhaustion of CD8 T lymphocytes by inhibiting PI3K/AKT/mTOR pathway, and targeted inhibition of TOX could partially restore the effector functions and activity of CD8 T lymphocytes.
- Joenja (leniolisib) / Pharming Group
Clinical History and Management of a Family with Activated Phosphoinositide-3-Kinase d (PI3Kd) Syndrome (Monitor 05) - Sep 14, 2023 - Abstract #ACAAI2023ACAAI_752;
Discussion This case emphasizes the significance of evaluating recurrent infections through genetic testing and the importance of considering testing family members. Genetic testing can provide valuable insights allowing for more effective management and targeted therapy.
- | Journal: Identification of galactosamine-(N-acetyl)-6-sulfatase (GALNS) as a novel therapeutic target in progression of nasopharyngeal carcinoma. (Pubmed Central) - Sep 14, 2023
Mechanistically, the anti-proliferative effect of GALNS silencing was the result of autophagy induction via the inhibition of PI3K-AKT-mTOR signaling pathway. Taken together, GALNS drives the progression of NPC via PI3K-AKT-mTOR signaling-mediated autophagy, and is therefore a promising therapeutic target.