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


«12...4849505152535455565758...229230»
  • ||||||||||  Piqray (alpelisib) / Novartis, Zydelig (idelalisib) / Gilead
    Journal:  Combined Treatment with PI3K Inhibitors BYL-719 and CAL-101 Is a Promising Antiproliferative Strategy in Human Rhabdomyosarcoma Cells. (Pubmed Central) -  May 21, 2022   
    When combined with CAL-101, BYL-719 decreased cell viability and induced apoptosis in a synergistic manner, equaling or surpassing results achieved with AZD8835. In conclusion, our findings indicate that BYL-719, either alone or in combination with the p110δ inhibitor, CAL-101, could represent an efficient treatment for human rhabdomyosarcoma presenting with aberrant upregulation of the PI3K signaling pathway.
  • ||||||||||  Preclinical, Journal, Tumor Mutational Burden:  Cell line models for drug discovery in PIK3CA-mutated colorectal cancers. (Pubmed Central) -  May 21, 2022   
    In concordance with patient samples, colorectal cancer cell lines with PIK3CA mutations display more commonly MSI and tend to be more sensitive to PI3K inhibitors. Variability in sensitivity of PIK3CA-mutated cell lines suggests that additional molecular abnormalities contribute to sensitivity.
  • ||||||||||  LY294002 / Eli Lilly
    Preclinical, Journal:  Asthma susceptibility in prenatal nicotine-exposed mice attributed to β-catenin increase during CD4 T cell development. (Pubmed Central) -  May 20, 2022   
    Moreover, inhibiting PI3K-AKT by LY294002 abrogated nicotine-mediated β-catenin level increase and thymopoiesis abnormalities, and an α7 nAChR antagonist (α-btx) also reversed nicotine-induced PI3K-AKT activation. Our findings provide strong evidence that PNE is a risk factor for T cell deviation and postnatal asthma, and revealed that nicotine-induced β-catenin level increase induces thymopoiesis abnormalities.
  • ||||||||||  Dual Therapy with Esculin and Erythropoietin Attenuates Renal Ischemia-Reperfusion Injury via P2x7 Receptor and Nlrp3 Inflammasome Inhibition, and Pi3k/akt Activation (Hynes Halls C & D: Board No. A074) -  May 20, 2022 - Abstract #ATC2022ATC_3205;    
    Our study suggests that mitofilin regulates pyroptosis through the PI3K/AKT signaling pathway in cardiomyocytes to ameliorate AMI, which may serve as a therapeutic strategy for the management of AMI. ESC, for the first time, demonstrated effective protection against RI/R-injury and its combination with EPO exerted maximal renoprotection when compared to each monotherapy, thereby representing an effective therapeutic approach via inhibiting oxidative stress, inflammation, renal tubular and endothelial injury, apoptosis, and P2X7 receptors, and activating PI3K/Akt pathway.
  • ||||||||||  roginolisib (IOA-244) / iOnctura
    Enrollment change, Trial completion date, Trial primary completion date, Combination therapy, Metastases:  DIONE-01: A Study to Assess a PI3K? Inhibitor (IOA-244) in Patients With Metastatic Cancers (clinicaltrials.gov) -  May 20, 2022   
    P1,  N=210, Recruiting, 
    ESC, for the first time, demonstrated effective protection against RI/R-injury and its combination with EPO exerted maximal renoprotection when compared to each monotherapy, thereby representing an effective therapeutic approach via inhibiting oxidative stress, inflammation, renal tubular and endothelial injury, apoptosis, and P2X7 receptors, and activating PI3K/Akt pathway. N=60 --> 210 | Trial completion date: Apr 2023 --> Apr 2024 | Trial primary completion date: Sep 2022 --> Sep 2023
  • ||||||||||  LY294002 / Eli Lilly
    Biomarker, Journal:  TEAD4 functions as a prognostic biomarker and triggers EMT via PI3K/AKT pathway in bladder cancer. (Pubmed Central) -  May 19, 2022   
    This study firstly provides a novel selective Grp94 inhibitor as a NPC candidate. TEAD4 is closely correlated with poor prognosis in BLCA and mediates its metastasis through regulating EMT via PI3K/AKT pathway, proving that TEAD4 is not only an effective biomarker for predicting the prognosis but also a great potential target for treatment of metastatic BLCA.
  • ||||||||||  Journal:  Expert consensus to optimize the treatment of elderly patients with luminal metastatic breast cancer. (Pubmed Central) -  May 19, 2022   
    It was concluded that the chronological age of the patient alone should not guide therapeutic decisions and that a Comprehensive Geriatric Assessment (CGA) should be performed whenever possible before establishing treatment. Treatment selection for the elderly population should consider the patient's baseline status, the expected benefit and toxicity of each treatment, and the impact of treatment toxicity on the patient's quality of life and functionality.
  • ||||||||||  cisplatin / Generic mfg.
    Journal:  Mubritinib enhanced the inhibiting function of cisplatin in lung cancer by interfering with mitochondrial function. (Pubmed Central) -  May 18, 2022   
    HIF-1α and/or Glut-1 knockout facilitated radiosensitivity in laryngeal carcinoma Tu212 cells by regulation of the PI3K/Akt/mTOR pathway. Mubritinib can upregulate intracellular ROS concentration and cell apoptosis, inhibit the PI3K signaling pathway and interfere with the function of mitochondria, thus reducing cell proliferation and increasing ROS induced apoptosis by reducing the activation of Nrf2 by PI3K.
  • ||||||||||  hydroxychloroquine / Generic mfg.
    Journal:  Hydroxychloroquine alleviates renal interstitial fibrosis by inhibiting the PI3K/Akt signaling pathway. (Pubmed Central) -  May 18, 2022   
    Mechanistically, HCQ treatment suppressed the activation of the PI3K/Akt and NF-kB pathways. This study demonstrated that HCQ ameliorated renal fibrosis by inhibiting the PI3K/AKT and NF-κB signaling pathways to attenuate inflammatory factors and the apoptotic function of renal tubular epithelial cells, thus providing renewed theoretical evidence for HCQ treatment of renal fibrosis.
  • ||||||||||  Review, Journal:  PI3K Inhibitors in Advanced Breast Cancer: The Past, The Present, New Challenges and Future Perspectives. (Pubmed Central) -  May 15, 2022   
    Nevertheless, the PI3K/AKT/mTOR cascade includes a complex network of biological events, needing more sophisticated approaches for their use in cancer treatment. In this review, we described the rationale for targeting the PI3K pathway, the development of PI3K inhibitors and the future treatment directions of different breast cancer subtypes in the metastatic setting.
  • ||||||||||  Journal:  PI 3-Kinase signaling: A journey in three AKTs. (Pubmed Central) -  May 14, 2022   
    I will also present recent efforts aimed at targeting AKT with novel therapies, including degrader technologies and how these have illuminated novel aspects of AKT biology. I will conclude with some personal thoughts and future perspectives as to where the field is going, gaps in knowledge and what studying AKT for 30 years has taught me.
  • ||||||||||  LY294002 / Eli Lilly, PTC-209 / PTC Therap
    Journal:  The ErbB3 Receptor Restricts Bmi1 to Regulate Paneth Cells. (Pubmed Central) -  May 14, 2022   
    Furthermore, BMI1 activity promotes LYZ1 expression. Together, these results support our hypothesis that ErbB3 regulates secretory cell differentiation through BMI1 in the intestinal epithelium.
  • ||||||||||  Piqray (alpelisib) / Novartis
    Journal:  Alkaline intracellular pH (pHi) increases mTORC1 and mTORC2 signaling through PI3K to promote protein synthesis and cell survival. (Pubmed Central) -  May 14, 2022   
    Indeed, alkaline pHi increased PI-3',4',5'-P3 levels in a manner sensitive to the PI3K inhibitor BYL-719...Taken together, these findings reveal alkaline pHi as a previously unrecognized activator of PI3K-mTORC1/2 signaling that promotes protein synthesis and cell survival. As elevated pHi represents an under-appreciated hallmark of cancer cells, these findings suggest that by alkaline pHi sensing by the PI3K-mTOR axis and AMPK-mTORC2 axes may contribute to tumorigenesis.
  • ||||||||||  Journal, IO biomarker:  5HTR1E receptor interacts with Neurotrophic factor-α1 and serotonin to activate two distinct signaling pathways. (Pubmed Central) -  May 14, 2022   
    Using LDH cytotoxicity assay we demonstrated that NF-α1/CPE was able to protect HEK-293-5HTR1E expressing cells against H O -induced cytotoxicity, via increasing pro-survival protein BCL2 expression; however, this protective effect of NFα1/CPE was diminished in the β-arrestin KO cells. Our study identified two ligands for HTR1E: NFα1/CPE which interacts with HTR1E to activate β-arrestin/ERK/BCL2 signaling pathway for protecting cells against oxidative stress; and serotonin which activated a Gi-cAMP-dependent pathway, the physiological role is under investigation.
  • ||||||||||  methotrexate IV / Generic mfg., methotrexate / Generic mfg.
    Biomarker, Review, Journal, IO biomarker:  Novel insights into the biomarkers and therapies for primary central nervous system lymphoma. (Pubmed Central) -  May 14, 2022   
    After the introduction and widespread use of high-dose-methotrexate (HD-MTX)-based polychemotherapy, treatment responses of PCNSL have been improved...In addition, the diagnostic efficiency of novel markers and the antitumor efficacy of novel therapies are needed to be assessed further in larger clinical trials. This review provides an overview of recent research on novel diagnostic markers and therapeutic strategies for PCNSL.
  • ||||||||||  B-CELL MALIGNANCIES TREATED WITH TARGETED DRUGS AND SARS-COV-2 INFECTION. A EUROPEAN HEMATOLOGY ASSOCIATION SURVEY (EPICOVIDEHA) (Hall Strauss 1-2) -  May 13, 2022 - Abstract #EHA2022EHA_2722;    
    Aims The aim of this study is to describe and analyse the outcome of COVID-19 patients with underlying LPD treated with targeted drugs such as monoclonal antibodies (obinutuzumab, ofatumumab, brentuximab, nivolumab or pembrolizumab), BTK inhibitors (ibrutinib, acalabrutinib), PI3K inhibitors (idelalisib), BCL2 inhibitors (venetoclax) and IMIDs, (lenalidomide)...Most used targeted drugs were ITKs (51.1%), anti-CD20 other than rituximab (16%), BCL2 inhibitors (7.3%) and lenalidomide (7.9%)...- COVID-19 vaccination was a protective factor for mortality, even in this population with humoral immunity impairment. - The learning curve in the management of the infection throughout the pandemic and the development of COVID-19 treatments showed benefit in this particularly vulnerable population.
  • ||||||||||  Zydelig (idelalisib) / Gilead
    FUNCTIONAL SCREENING OF PI3K INHIBITORS STRATIFIES RESPONDERS TO IDELALISIB AND INDICATES DRUG CLASS ACTIVITY IN IDELALISIB-REFRACTORY CLL () -  May 13, 2022 - Abstract #EHA2022EHA_1186;    
    Aims To characterize functional responses to 10 PI3Ki in CLL To study PI3Ki drug class activity in idelalisib-refractory CLL To investigate whether ex vivo drug sensitivity can predict in vivo treatment responses Methods CLL cells from patients that were treatment naïve (n=7), idelalisib refractory (n=9), or on idelalisib treatment (longitudinal samples from n=6 patients) were screened against 10 PI3Ki (buparlisib, compound 7n, copanlisib, duvelisib, idelalisib, nemiralisib, pictilisib, pilaralisib, umbralisib, ZSTK474), both alone and in combination with the B-cell lymphoma 2 (Bcl-2) antagonist venetoclax...Ex vivo drug testing on CLL cells from a patient who presented with relapsed disease after sequential treatment with FCR, ibrutinib, idelalisib and venetoclax revealed sensitivity to PI3Ki+venetoclax treatment...Conclusion Our findings indicate PI3Ki drug class activity in idelalisib-refractory CLL, and suggest that ex vivo drug sensitivity may guide precision medicine and predict treatment responses. These results warrant further testing in larger cohorts and in clinical trials.
  • ||||||||||  Mechanism of hepatocyte growth factor-induced decreased expression of protein C inhibitor in HepG2 cells (Exhibition) -  May 13, 2022 - Abstract #ISTH2022ISTH_2072;    
    PCI expression in HepG2 cells was decreased by HGF treatment, and this HGF-induced decreased expression of PCI in HepG2 cells was recovered by c-Met inhibitor, MEK inhibitor and PI3K inhibitor treatments, but JUN kinase inhibitor and ERK inhibitor had no effect on it. Conclusion(s): Our results indicated that HGF decreases PCI expression in hepatocytes via c-Met, MEK and PI3K.