PI3K inhib 
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  • ||||||||||  Journal:  Methyl vinyl ketone and its analogs covalently modify PI3K and alter physiological functions by inhibiting PI3K signaling. (Pubmed Central) -  Apr 3, 2024   
    Furthermore, we analyzed the effects of the 23 RCS compounds with structures similar to MVK and showed that their analogs also suppressed PI3K-Akt signaling in a manner that correlated with their similarities to MVK. Our study demonstrates the mechanism of MVK and its analogs in suppressing PI3K-Akt signaling and modulating physiological functions, providing a model for future studies analyzing environmental reactive species.
  • ||||||||||  Review, Journal:  Regulation of ferroptosis by PI3K/Akt signaling pathway: a promising therapeutic axis in cancer. (Pubmed Central) -  Apr 2, 2024   
    Evidence suggests that inhibiting the PI3K/Akt pathway may sensitize cancer cells to ferroptosis induction, offering a promising strategy to overcome drug resistance. This review aims to provide a comprehensive exploration of this interplay, shedding light on the potential for disrupting the PI3K/Akt pathway to enhance ferroptosis as an alternative route for inducing cell death and improving cancer treatment outcomes.
  • ||||||||||  Cilcane (cilengitide) / Iceni Pharma, LY294002 / Eli Lilly, Ex-Rad (recilisib) / Onconova
    Journal:  FNDC5 inhibits malignant growth of human cervical cancer cells via restraining PI3K/AKT pathway. (Pubmed Central) -  Apr 1, 2024   
    The effects of FNDC5 were prevented by inhibiting integrin with cilengitide, activating PI3K with recilisib or activating Akt with SC79...PI3K inhibitor LY294002 showed similar effects to FNDC5 in HeLa and SiHa cells...These results indicate that FNDC5 inhibits the malignant phenotype of CxCa cells through restraining PI3K/Akt signaling. Upregulation of FNDC5 may play a beneficial role in retarding the tumor growth of CxCa.
  • ||||||||||  Mekinist (trametinib) / Novartis, BeiGene, Estybon (rigosertib) / Onconova, SymBio Pharma, Knight Therap
    Targeting RAS/RAF/PI3K pathway for CD40 induction in melanoma cells to overcome resistance to anti-PD1 immunotherapies (Exhibit Hall F1; Poster Board Number: B137) -  Mar 29, 2024 - Abstract #IMMUNOLOGY2024IMMUNOLOGY_718;    
    We showed that rigosertib (RGS), a RAS-pathway inhibitor, promotes CD40 upregulation on melanoma cells and synergizes with ICB in preclinical melanoma models...Our present study explores the efficacy of RGS plus trametinib (T), a MEK1/2 inhibitor, to overcome ICB resistance...CRISPR/dCas9-based overexpression of CD40 (CD40-OE) in 1014 melanoma cells reduced in vivo tumor growth and successfully turned the ICB-resistant tumors into responders to ?PD1 (p=0.025), which further regressed with aCD40+?PD1 (p<0.001). Our preclinical data support the therapeutic use of RAS/RAF/PI3K inhibition plus CD40 agonism for metastatic melanoma patients who do not respond to ICB.
  • ||||||||||  metformin / Generic mfg.
    Journal:  Anti-ENO1 antibody combined with metformin against tumor resistance: a novel antibody-based platform. (Pubmed Central) -  Mar 26, 2024   
    The study preliminarily revealed anti-ENO1 antibody combined with metformin could overcome drug resistance against CSCs by inhibiting the Wnt//?-catenin pathway and might serve as a potential precursor platform for screening ADC. More importantly, it is reasonably believed that antibody-based drug combination therapy might function as an encouraging tool for oncotherapy.
  • ||||||||||  Preclinical, Journal:  Isoalantolactone exerts anti-melanoma effects via inhibiting PI3K/AKT/mTOR and STAT3 signaling in cell and mouse models. (Pubmed Central) -  Mar 25, 2024   
    Moreover, IATL inhibited STAT3 activation both in melanoma cells and allograft tumors not only by binding to the SH2 domain of STAT3 but also by suppressing the activity of its upstream kinase Src. These findings demonstrate that IATL exerts anti-melanoma effects via inhibiting the STAT3 and PI3K/AKT/mTOR signaling pathways, and provides a pharmacological basis for developing IATL as a novel phytotherapeutic agent for treating melanoma clinically.
  • ||||||||||  Preclinical, Journal:  Emodin ameliorates myocardial fibrosis in mice by inactivating the ROS/PI3K/Akt/mTOR axis. (Pubmed Central) -  Mar 24, 2024   
    Emodin could regulate the activity of PI3K to increase the expression of collagen II and downregulate ?-SMA expression in part through the PI3K/AKT/mTOR pathway, and emodin significantly improved cardiac structure and function in mice. This study revealed that emodin targeted the PI3K/AKT/mTOR pathway to inhibit the development of myocardial fibrosis and may be an antifibrotic agent for the treatment of cardiac fibrosis.
  • ||||||||||  propylthiouracil / Generic mfg.
    Journal:  Ginseng extracts improve circadian clock gene expression and reduce inflammation directly and indirectly through gut microbiota and PI3K signaling pathway. (Pubmed Central) -  Mar 24, 2024   
    This paper illustrates that intermittent supplementation with ginseng extracts improved body temperature rhythm and suppressed inflammatory responses in peripheral metabolic organs of propylthiouracil (PTU)-induced hypothermic rats...Furthermore, administration of PI3K inhibitor blocked ginseng or microbiota-induced gene expression related with circadian clock and inflammation in vitro. These findings demonstrate that the hot property of ginseng may be mediated by improving circadian clock and suppressing inflammation directly or indirectly through the gut microbiota and PI3K-AKT signaling pathways.
  • ||||||||||  parsaclisib (INCB50465) / Incyte, gedatolisib (PF-05212384) / Celcuity, buparlisib (AN2025) / Novartis, Adlai Nortye
    Journal:  A Long Way to Go: A Scenario for Clinical Trials of PI3K Inhibitors in Treating Cancer. (Pubmed Central) -  Mar 22, 2024   
    sh-Ambra1 increased IRS-1/PI3K/Akt protein phosphorylation levels to reduce autophagy in gestational diabetes. The establishment of development indicators based on clinical trials for cancer treatment was useful to highlight the clinical investment in 3 new PI3K drugs and the advantages of combine therapy using FDA-approved drugs.
  • ||||||||||  risovalisib (CYH33) / HaiHe Biopharma
    Enrollment change, Trial termination, Combination therapy, Metastases:  Study of CYH33 in Combination With Olaparib an Oral PARP Inhibitor in Patients With Advanced Solid Tumors. (clinicaltrials.gov) -  Mar 21, 2024   
    P1,  N=24, Terminated, 
    The establishment of development indicators based on clinical trials for cancer treatment was useful to highlight the clinical investment in 3 new PI3K drugs and the advantages of combine therapy using FDA-approved drugs. N=350 --> 24 | Recruiting --> Terminated; Business decision
  • ||||||||||  Zelboraf (vemurafenib) / Roche
    Journal, IO biomarker:  Mechanisms of vemurafenib-induced anti-tumor effects in ATC FRO cells. (Pubmed Central) -  Mar 21, 2024   
    N=350 --> 24 | Recruiting --> Terminated; Business decision The protein expression levels of Bax and E-cadherin were up-regulated significantly, and the expression levels of BRAF, CyclinD1, Bcl-2, p-PI3K, p-AKT, and p-mTOR were markedly down-regulated with increasing concentrations of vemurafenib (P
  • ||||||||||  Journal:  Identification of Novel PI3K? Inhibitor Against Gastric Cancer: QSAR-, Molecular Docking-, and Molecular Dynamics Simulation-Based Analysis. (Pubmed Central) -  Mar 20, 2024   
    Furthermore, compound 1-(3-(2,4-dimethylthiazol-5-YL)-4-oxo-2,4-dihydroindeno[1,2-C]pyrazol-5-YL)-3-(4-methylpiperazin-1-YL) urea was selected as a potential hit in the final screening by analyzing a number of parameters, including the Rg, RMSD, RMSF, H bonding, and SASA profile. Therefore, we conclude that compound 1-(3-(2, 4-dimethylthiazol-5-YL)-4-oxo-2,4-dihydroindeno[1,2-C]pyrazol-5-YL)-3-(4-methylpiperazin-1-YL) urea has efficient inhibitory potential against PI3Kalpha protein and could be utilized for the development of effective drugs against GC.
  • ||||||||||  Journal:  Cancer cells hijack physiological metabolic signals to seed liver metastasis. (Pubmed Central) -  Mar 19, 2024   
    Rogava and colleagues identified Pip4kc as a driver of liver metastasis, acting by sensitizing cancer cells to insulin-dependent PI3K/AKT signaling, which could be reversed by dual pharmacological inhibition of PI3K and SGLT2 or a ketogenic diet. The study highlights the importance of tumor: microenvironment communication in the context of systemic physiology and points towards potential combination therapies.
  • ||||||||||  Review, Journal:  PI3K and tankyrase inhibitors as therapeutic targets in colorectal cancer. (Pubmed Central) -  Mar 18, 2024   
    The design of potent inhibitors is crucial to effectively block these protein signaling pathways. Moreover, it is essential to explore the potential of dual target inhibition of other signaling pathways in conjunction with PI3K and tankyrase.
  • ||||||||||  Kinenza (enzastaurin) / Denovo, Aytu BioPharma, paxalisib (GDC-0084) / Kazia
    Journal:  PI3K/mTOR is a therapeutically targetable genetic dependency in diffuse intrinsic pontine glioma. (Pubmed Central) -  Mar 18, 2024   
    Therapeutic adaptation was assessed using spatial transcriptomics and ATAC-sequencing, identifying changes in myelination and tumor immune microenvironment crosstalk. Together, we have identified a clinically relevant DIPG therapeutic combinatorial approach.
  • ||||||||||  Massive Endocytosis Mechanisms are Involved in CD169-Mediated Uptake of HIV-1 by Dendritic Cells. (Poster hall) -  Mar 16, 2024 - Abstract #CROI2024CROI_1155;    
    This work provides new insights into the interaction of HIV-1 with myeloid cells revealing new therapeutical targets to hinder virus dissemination. Blocking VCC formation offers potential cross-protection against enveloped viral infections that use CD169 receptor, such as Ebolaviruses and other hemorrhagic fever viruses.