AKT3 inhib 
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  • ||||||||||  SOX2 Deregulated Squamous Carcinomas Are Vulnerable to AKT3 Inhibition (Exhibit Hall) -  Jul 25, 2023 - Abstract #IASLCWCLC2023IASLC_WCLC_1212;    
    Therefore, targeting miR-29a-3p may provide a new therapeutic strategy for silica-induced pulmonary fibrosis. Taken together, our work suggests that SOX2-amplified squamous cancers may be vulnerable to isoform-specific inhibition of AKT3.
  • ||||||||||  GSK690693 / GSK
    Journal:  PCBP1-mediated regulation of WNT signaling is critical for breast tumorigenesis. (Pubmed Central) -  Jun 4, 2022   
    Using a xenograft orthotopic model of breast tumorigenesis (4T1-Pcbp1), we show here that PCBP1 knockdown-induced tumorigenesis is inhibited by activation of the WNT signaling via treating with the glycogen synthase kinase 3 beta inhibitor TWS119, but not the Akt2/Akt3 inhibitor GSK690693...Using cytotoxic T cells isolated from healthy donors, we show that TWS119-induced WNT signaling-mediated inhibition of cytotoxic T cell expansion is reliant on expression of PCBP1. In conclusion, decreased PCBP1 expression favors breast tumorigenesis by potentiating skewing of tumor infiltrating T cells towards Tregs, thereby effectively suppressing anti-tumor immunity.
  • ||||||||||  AUTOANTIBODIES SPECIFIC FOR FIBROSIS-RELATED PROTEINS AS CANDIDATE BIOMARKERS IN SYSTEMIC SCLEROSIS (MC2 HALL) -  May 25, 2022 - Abstract #AUTO2022AUTO_110;    
    Furthermore, two of these autoantibodies, against Phosphatidylinositol-5-phosphate 4-kinase type 2 beta (PIP42K2B) and AKT Serine/Threonine Kinase 3 (AKT3), might serve as new candidate biomarkers for fibrosis in SSc patients in the future. Conclusions Further studies in larger cohorts are needed to validate our preliminary results.
  • ||||||||||  dasatinib / Generic mfg.
    Journal:  E-Cadherin-Deficient Cells Are Sensitive to the Multikinase Inhibitor Dasatinib. (Pubmed Central) -  Apr 13, 2022   
    Treatment with combinations of dasatinib and an inhibitor of AKT, MK2206, enhanced the effect of dasatinib in breast MCF10A cells. In conclusion, targeting the DDR2-SRC-AKT3 axis with dasatinib represents a promising approach for the chemoprevention and chemotherapy of gastric and breast cancers lacking E-cadherin.
  • ||||||||||  Biomarker, Journal:  Expression of Selected Genes and Circulating microRNAs in Patients with Celiac Disease. (Pubmed Central) -  Mar 5, 2022   
    The DIANA and miRNet databases identified significant functional activity for miR-449a and miR-192-5p and an interconnection of miR-194-5p and miR-449a with CCND1. In conclusion, genes and circulating miRNAs require further studies as they could represent important biomarkers in clinical practice.
  • ||||||||||  Journal:  PPAR-gamma induced AKT3 expression increases levels of mitochondrial biogenesis driving prostate cancer. (Pubmed Central) -  Oct 22, 2021   
    Collectively our results demonstrate how PPARG over-expression drives an increase in AKT3 levels, which in turn has the downstream effect of increasing PGC1α localisation within the nucleus, driving mitochondrial biogenesis. Furthermore, this increase in mitochondrial mass provides higher energetic output in the form of elevated ATP levels which may fuel the progression of the tumour cell through epithelial to mesenchymal transition (EMT) and ultimately metastasis.
  • ||||||||||  Journal:  MicroRNA‑16‑5p regulates cell survival, cell cycle and apoptosis by targeting AKT3 in prostate cancer cells. (Pubmed Central) -  May 22, 2021   
    Moreover, luciferase reporter assay and western blot analysis showed that miR‑16‑5p directly targets AKT3 (AKT serine/threonine kinase 3), which is associated with PCa carcinogenesis, and the effects of the downregulation of AKT3 were similar to the effects of upregulation of miR‑16‑5p in PC‑3 cells. In conclusion, our data clarify that miR‑16‑5p has anticancer functions in PCa cells, and our findings provide experimental evidence to highlight the potential value of miR‑targeting treatment strategies for PCa.
  • ||||||||||  Journal, IO biomarker:  Transcriptome sequencing identifies genes associated with invasion of ovarian cancer. (Pubmed Central) -  May 15, 2021   
    In conclusion, our data clarify that miR‑16‑5p has anticancer functions in PCa cells, and our findings provide experimental evidence to highlight the potential value of miR‑targeting treatment strategies for PCa. Candidate genes enriched in cell adhesion, extracellular matrix-receptor interaction and PI3K-Akt signalling pathways were identified that may be closely associated with ovarian cancer invasion and potential targets for ovarian cancer treatment.
  • ||||||||||  sildenafil / Generic mfg.
    Journal:  PDE5 inhibition rescues mitochondrial dysfunction and angiogenic responses induced by Akt3 inhibition by promotion of PRC expression. (Pubmed Central) -  Mar 26, 2021   
    We found that, sildenafil, a phosphodiesterase 5 inhibitor, induced mitochondrial biogenesis as measured by increased uncoupled oxygen consumption, mitochondrial DNA content, and voltage-dependent anion channel protein expression...Thus, PRC can functionally substitute during Akt3 depletion for absent PGC-1α activity to restore mitochondrial homeostasis and promote angiogenesis. These findings show that mitochondrial homeostasis as controlled by the PGC family of transcriptional activators is required for angiogenic responses.
  • ||||||||||  Journal:  Adaptive Molecular Evolution of AKT3 Gene for Positive Diversifying Selection in Mammals. (Pubmed Central) -  Mar 23, 2021   
    From 39 mammalian species studied, there was a signal of positive diversifying selection with Hominidae at 13Q, 16G, 23R, 24P, 121P, 294K, 327V, 376L, 397K, 445T, and 471F among other codon sites of the AKT3 gene. These sites were codes for amino acids such as arginine, proline, lysine, and leucine indicating major roles for the function of immunological proteins, and in particular, the study highlighted the importance of changes in gene expression of AKT3 on immunity.
  • ||||||||||  Journal:  PDE5 inhibition rescues mitochondrial dysfunction and angiogenic responses induced by Akt3 inhibition by promotion of PRC expression. (Pubmed Central) -  Jan 20, 2021   
    We found that, sildenafil, a phosphodiesterase 5 inhibitor, induced mitochondrial biogenesis as measured by increased uncoupled oxygen consumption, mitochondrial DNA content, and voltage-dependent anion channel protein expression...Thus, PRC can functionally substitute during Akt3 depletion for absent PGC-1α activity to restore mitochondrial homeostasis and promote angiogenesis. These findings show that mitochondrial homeostasis as controlled by the PGC family of transcriptional activators is required for angiogenic responses.
  • ||||||||||  Journal:  The histone demethylase JMJD2B regulates endothelial-to-mesenchymal transition. (Pubmed Central) -  Jul 19, 2020   
    Silencing of JMJD2B prevented the EndMT-induced reduction of H3K9me3 marks at these promotors and further repressed these EndMT-related genes. Our study reveals that endothelial identity and function is critically controlled by the histone demethylase JMJD2B, which is induced by EndMT-promoting, proinflammatory, and hypoxic conditions, and supports the acquirement of a mesenchymal phenotype.