PI3K inhib 
Welcome,         Profile    Billing    Logout  
 67 Companies  59 Products   59 Products   344 Diseases   342 Trials   12240 News 


«12...3334353637383940414243...229230»
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  Overexpression of fibroblast growth factor 13 ameliorates amyloid-β-induced neuronal damage. (Pubmed Central) -  Dec 2, 2022   
    The changes were reversed by the phosphatidylinositol-3-kinase inhibitor LY294002. These findings suggest that overexpression of fibroblast growth factor 13 improved neuronal damage in a rat model of Alzheimer's disease through activation of the phosphatidylinositol-3-kinase/AKT/glycogen synthase kinase 3β signaling pathway.
  • ||||||||||  Journal:  Cardiac PI3K p110α attenuation delays aging and extends lifespan. (Pubmed Central) -  Dec 1, 2022   
    In humans, explanted failing hearts showed in-creased PI3K signaling, as indicated by increased phos-phorylation of the serine/threonine-protein kinase AKT. Hence, late-life cardiac-specific targeting of PI3K might have a therapeutic potential in cardiac aging and related diseases.
  • ||||||||||  Perjeta (pertuzumab) / Roche, inavolisib (GDC-0077) / Roche
    GeparPiPPa- A randomized, open-label, phase II trial comparing neoadjuvant trastuzumab, pertuzumab and endocrine therapy +/- the PI3K inhibitor inavolisib in patients (pts) with HER2+/HR+, PIK3CA mutant early breast cancer (BC) (Room A2) -  Nov 30, 2022 - Abstract #DKK2022DKK_1856;    
    The phase III Solar-1 study demonstrated a sig- nificant improvement in progression-free survival with the addition of alpelisib to fulvestrant in PIK3CA mutant metastatic BC (André F 2019)...170 pts with cT1c – cT3 early BC, centrally confirmed HER2+ and HR+-status as well as a PIK3CA tumor mutation (by NGS) will be randomized 1:1 to receive 6 cycles of tamoxifen or an aromatase inhibitor (1x1/d orally, day 1-21 q3w) +/- gonadotropin-releasing hor- mone analogue plus pertuzumab/trastuzumab (subcutaneous formula- tion [1200 (600) mg/600 mg on d1, q3w]) without or with inavolisib (9mg 1x1/d orally, day 1-21 q3w)...Secondary endpoints include com- parison of other pCR definitions, invasive disease-free survival, overall survival, and safety. Further (neo)adjuvant systemic treatment and radio- therapy will be administered at the discretion of the investigator accord- ing to standard of care.
  • ||||||||||  Zydelig (idelalisib) / Gilead
    Potential Drivers of Acquired Resistance to Idelalisib in CLL Patients () -  Nov 29, 2022 - Abstract #ASH2022ASH_7605;    
    We checked the phosphorylation/activation level of AKT and ERK1/2 at the responding and progression time points in the three original CLL patients with acquired resistance and observed that pERK levels are inhibited by idelalisib at baseline, but not at progression, in 2 patients (patient 1 and 2). In conclusion, we have identified potential drivers of acquired resistance to idelalisib in CLL patients, including MAPK pathway activation as in our prior study, and we continue with ongoing work evaluating the potential role of PI3K pathway mutations, BIRC3, AICDA and LTK in treatment resistance, since insights from these studies will help us guide therapy for CLL patients with refractory disease.
  • ||||||||||  Polivy (polatuzumab vedotin-piiq) / Roche
    A Phase 1b Open-Label Study of Loncastuximab Tesirine in Combination with Other Anticancer Agents in Patients with Relapsed or Refractory (R/R) B-Cell Non-Hodgkin Lymphoma (LOTIS-7) () -  Nov 29, 2022 - Abstract #ASH2022ASH_7453;    
    P1b
    Key inclusion criteria are patients age ≥18 years with a pathologic diagnosis of R/R B-NHL (2016 WHO classification) and the following: those who failed/are intolerant to any approved Tx, received ≥2 systemic Tx regimens, need systemic Tx, have an ECOG performance status of 0-2, and have measurable disease (2014 Lugano Classification). Patients who previously received any study drugs; received a stem-cell transplant within 60 days prior to the start of study drugs; have lymphoma with active CNS involvement, serious skin-related disease, ascites, edema, or effusion; and have significant medical comorbidities are excluded.Result s : The study opened in December 2021, and the first patient was dosed in the Lonca + Pola arm in June 2022.
  • ||||||||||  Brukinsa (zanubrutinib) / BeiGene, Calquence (acalabrutinib) / AstraZeneca
    Utilization of Pharmacogenomics in Assessment of Tolerability and Efficacy of BTK Inhibitors () -  Nov 29, 2022 - Abstract #ASH2022ASH_7183;    
    We identified patient with pharmacogenomics polymorphisms that can affect plasma drug levels and are evaluating concurrent use of medication with can affect BTKi metabolism, as well as their effect on time to therapy discontinuation and adverse events. These results will inform the personalized selection of BTKi therapy for patients with B cell malignancies.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  Reversion of glucocorticoid-induced senescence and collagen synthesis decrease by LY294002 is mediated through p38 in skin. (Pubmed Central) -  Nov 29, 2022   
    Interestingly, the protective effect of LY was dose-dependently reversed by treatment with a p38 inhibitor and reached 2.9 ± 0.15 fold at dose 20 µM. Taken together, our results demonstrate that LY reduced CP-induced upregulation of the atrophy marker FKBP51, GR phosphorylation, and GR nuclear translocation via the activation of p38, whilst maintaining the anti-inflammatory effect of glucocorticoids.
  • ||||||||||  methotrexate / Generic mfg.
    Journal, IO biomarker:  Wenhua Juanbi Recipe Attenuates Rheumatoid Arthritis via Inhibiting miRNA-146a-Mediated Autophagy. (Pubmed Central) -  Nov 29, 2022   
    The model rats were administered WJR or methotrexate (MTX) to assess the therapeutic effect of the drugs...WJR could, therefore, regulate autophagy by influencing the miRNA-146a-mediated PI3K/AKT/mTOR pathway, which induces apoptosis and proliferation of FLS. WJR can inhibit autophagy, apoptosis, and proliferation in a CIA rat model by inhibiting the miRNA-146a-mediated PI3K/AKT/mTOR pathway.
  • ||||||||||  gefitinib / Generic mfg.
    Journal:  STE029 Overcomes EGFR-TKI Resistance in Human Lung Adenocarcinoma (Pubmed Central) -  Nov 25, 2022   
    STE029 could sensitize Gefitinib by inhibiting EGFR/PI3K/Akt pathway, blocking the tumor cell cycle and proliferation and inducing apoptosis through caspase-8 and caspase-9 dependent pathway. STE029 deserves further investigations in overcoming EGFR-TKI resistance in lung cancer.
  • ||||||||||  Journal:  GLP-1 rescued gestational diabetes mellitus-induced suppression of fetal thalamus development. (Pubmed Central) -  Nov 25, 2022   
    In vitro study observed enhanced axonal elongation after supplements of GLP-1 analog, GLP-1 analog PI3K-dependently active ROCK1 activity, IP injection of GLP-1 analog could partly reverse GDM-induced suppression of fetal thalamocortical axon development and improve tactile sensory behavior of GDM offspring. Our study provided a novel mechanism of GDM induced-neurological diseases and predicted GLP-1 as possible prevention supplement during gestation.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  EphA4/ephrinA3 reverse signaling mediated downregulation of glutamate transporter GLAST in Müller cells in an experimental glaucoma model. (Pubmed Central) -  Nov 24, 2022   
    In Müller cells with ephrinA3 knockdown, the PI3K inhibitor LY294002 still decreased the protein levels of NF-κB p65 in the presence of EphA4-Fc, and the mRNA levels of GLAST were reduced by LY294002 and the NF-κB inhibitor SN50, respectively...Western blot and TUNEL staining showed that transfecting of Si-EFNA3 reduced Müller cell gliosis and RGC apoptosis in COH retinas. Our results suggest that activated EphA4/ephrinA3 reverse signaling induces GLAST downregulation in Müller cells via inhibiting PI3K/Akt/NF-κB pathways, thus contributing to RGC damage in glaucoma.
  • ||||||||||  Journal:  Loss of NF1 in melanoma confers sensitivity to SYK kinase inhibition. (Pubmed Central) -  Nov 22, 2022   
    Furthermore, combinations of inhibitors targeting either MEK or PI3K/mTOR with an independent SYK kinase inhibitor or SYK knockdown reduced the growth of NF1-LoF melanoma cells. These studies provide a path to exploit SYK dependency to selectively target NF1-LoF melanoma cells.
  • ||||||||||  LY294002 / Eli Lilly
    Preclinical, Journal:  Knockdown of CCR3 gene inhibits Proliferation, migration and degranulation of eosinophils in mice by downregulating the PI3K/Akt pathway. (Pubmed Central) -  Nov 22, 2022   
    Bone marrow cells from wild-type mice (WT) were harvested for primary culture and differentiated into mature EOS, which were then randomly divided into the control, 740Y-P, and LY294002 group...Mechanistically, CCR3 inhibited EOS's proliferation, migration, and degranulation by downregulating PI3K/Akt pathway. This data suggests that the knockout of the CCR3 gene in bone marrow cells may inhibit the function of EOS by downregulating the PI3K/Akt pathway, thereby affecting AR; thus, the CCR3 gene may be a target gene for AR therapy.
  • ||||||||||  Visanne (dienogest) / Mochida, Bayer
    Journal:  Melatonin inhibits endometriosis development by disrupting mitochondrial function and regulating tiRNAs. (Pubmed Central) -  Nov 20, 2022   
    The results of this study demonstrated that melatonin and dienogest administration effectively reduced surgically induced endometriotic lesions in a mouse model...Furthermore, we demonstrated that tiRNA and tiRNA were associated with the proliferation of endometriosis and that melatonin suppressed the expression of these tiRNAs in primary endometriotic stromal cells and lesions in a mouse model. Thus, melatonin can be used as a novel therapeutic agent to manage endometriosis.
  • ||||||||||  lenalidomide / Generic mfg.
    Journal, IO biomarker:  Molecular and clinical diversity in primary central nervous system lymphoma. (Pubmed Central) -  Nov 20, 2022   
    Thus, melatonin can be used as a novel therapeutic agent to manage endometriosis. The integration of genome-wide data from multi-omics data revealed four molecular patterns in PCNSL with a distinctive prognostic impact that provides a basis for future clinical stratification and subtype-based targeted interventions.
  • ||||||||||  Brukinsa (zanubrutinib) / BeiGene, Lunsumio (mosunetuzumab) / Roche, Biogen, Rituxan (rituximab) / Biogen, Zenyaku Kogyo, Roche
    Journal:  Top advances in lymphoma for 2021. (Pubmed Central) -  Nov 19, 2022   
    On the basis of these trends, PI3K inhibitors are being displaced in favor of safer and more durable constructs. In addition, within the past year, the approval and implementation of zanubrutinib for marginal zone lymphoma have filled a need for later line therapy, especially for less fit and elderly patients.
  • ||||||||||  doxorubicin hydrochloride / Generic mfg.
    Journal:  Inhibition of colorectal cancer tumorigenesis by ursolic acid and doxorubicin is mediated by targeting the Akt signaling pathway and activating the Hippo signaling pathway. (Pubmed Central) -  Nov 18, 2022   
    The efficacy of combined treatment with natural product‑derived and chemotherapy agents including curcumin combined with 5‑fluorouracil, resveratrol combined with cisplatin and epigallocatechin‑3‑gallate (EGCG) combined with cisplatin in preventing cancer progression and killing cancer cells has emerged...Furthermore, The PI3K inhibitor LY294002 further suppressed Akt activity and enhance the function of Hippo pathway‑associated proteins in DOX + UA treated cells; this effect led to subsequent oncogenic Yap and CTGF inhibition following combined treatment, whereas Akt activator SC79 exerted an opposite effect in CTGF expression...In conclusion, these findings suggested that combination therapy with UA and DOX may be more effective than DOX alone. UA may be a novel anticancer strategy and could be considered for investigation as a complementary chemotherapy agent in the future.
  • ||||||||||  Review, Journal:  PI3K signalling at the intersection of cardio-oncology networks: cardiac safety in the era of AI. (Pubmed Central) -  Nov 18, 2022   
    This was followed by an intersection scheme of the networks that can be functionalised with machine learning for safety and risk prediction, diagnoses, and defining new novel encouraging leads and targets for clinical translation. This will hopefully overcome the challenges of the one-signalling-one-health-outcome alliance, and expand our knowledge of the totality of PI3K signalling in cardio-oncology.
  • ||||||||||  Erbitux (cetuximab) / Eli Lilly, EMD Serono
    Journal:  Platycodin D sensitizes KRAS-mutant colorectal cancer cells to cetuximab by inhibiting the PI3K/Akt signaling pathway. (Pubmed Central) -  Nov 18, 2022   
    Our results confirmed that platycodin-D increased the cytotoxic effects of cetuximab, including inhibition of growth, migration, and invasion, via downregulation of PI3K and Akt phosphorylation in HCT116 and LoVo cells both in vitro and in vivo. Given these data, platycodin-D may sensitize KRAS-mutant colorectal cancer cells to cetuximab via inhibition of the PI3K/Akt signaling pathway.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  The prognostic value and mechanisms of centromere protein M in patients with lung adenocarcinoma. (Pubmed Central) -  Nov 18, 2022   
    In vitro studies, LUAD cell lines were treated with CENPM-short hairpin RNA (shRNA) (shCENPM), or transfected with CENPM overexpression plasmids with or without LY294002 (PI3K inhibitor) treatment...CENPM was upregulated in LUAD patients, and it correlated with higher pathological stages and poor survival rates. CENPM could affect cell proliferation, cell cycle, cell migration and invasion capacity, and apoptosis in LUAD cell lines via regulation of AKT1/mTOR signaling pathway.
  • ||||||||||  Journal:  Hydroxytyrosol Ameliorates Intervertebral Disc Degeneration and Neuropathic Pain by Reducing Oxidative Stress and Inflammation. (Pubmed Central) -  Nov 18, 2022   
    Moreover, HT inhibited the secretion of COX-2, tumor necrosis factor-α (TNF-α), interleukin (IL)-6, IL-1β, and iNOS and activation of the NLRP3 inflammasome in microglia by inhibiting the phosphatidylinositol 3-kinase (PI3K)/protein kinase B (AKT) and extracellular regulated protein kinase (ERK) signaling pathways. In conclusion, HT plays a protective role against IVDD and secondary neuropathic pain by inhibiting the NF-κB, PI3K/AKT, and ERK signaling pathways.