2024年2月28日 · Our results show that the PP2A switch is induced by PKC-mediated phosphorylation of Ser24-PP2Ac and that this phosphorylation leads to apoptosis upon GqPCR induction of various cells. We propose that this mechanism may provide an unexpected way to treat some cancer types or problems in the endocrine machinery.

In the present study, we determined the cross talk between PI3K-AKT-GSK-3β and PP2A pathways and found that the former regulated the methylation of PP2Ac via GSK-3β. Upregulation of GSK-3β led to an increase in the methylation and activity of PP2Ac through suppression of protein phosphatase methylesterase-1 expression and phosphorylation of ...

Protein Phosphatase 2A (PP2A) is an important and ubiquitously expressed serine threonine phosphatase and regulates the function by dephosphorylating many critical cellular molecules like Akt, p53, c-Myc and β-catenin. It plays a critical role in ...

2018年8月1日 · The effects of AKT and SRC inhibitors on pancreatic cancer cell proliferation were investigated. Two human pancreatic cancer cell lines, MIA PaCa-2 and PANC-1, were treated with the AKT inhibitor 10-DEBC or SRC inhibitor PP2, and cell proliferation was measured after 72 h.

2003年1月24日 · PP2 abrogated 17β-estradiol-induced activation of PI3-kinase, indicating that the PP2-inhibitable kinase is upstream of PI3-kinase and Akt. A 17β-estradiol-induced estrogen receptor/c-Src association correlated with rapid c-Src phosphorylation.

In the present study, the pyrazolopyrimidine compound PP2 was used to inhibit Src family protein tyrosine kinases in A549 cells. It was demonstrated that PP2 was able to suppress cell viability, migration and invasion, and promote apoptosis via regulating the phosphoinositide 3-kinase/protein kinase B/B-cell lymphoma 2/caspase-3 signaling pathway.

2019年10月1日 · Our findings demonstrate that SNRK regulates insulin signaling through controlling PPP2R5D phosphorylation, which subsequently impacts PP2A activity and then AKT phosphorylation in both WAT and BAT. SNRK may represent a promising potential target for treating insulin resistance-related metabolic disorders. 1. Introduction.

One study identified sex-determining region Y box 2 as a novel target of epidermal growth factor receptor (EGFR)/Src/protein kinase B (Akt) signaling in NSCLC that modulates self-renewal and expansion of stem-like cells from NSCLC (10).

2021年11月23日 · Immunoblotting demonstrated PP2-sensitive phosphorylation of AKT and the MTORC1 target 4EBP1, suggesting PI3K/AKT activation as a key survival pathway downstream from transformation by FYN T alleles.

In the present study, the pyrazolopyrimidine compound PP2 was used to inhibit Src family protein tyrosine kinases in A549 cells. It was demonstrated that PP2 was able to suppress cell viability, migration and invasion, and promote apoptosis via regulating the phosphoinositide 3-kinase/protein kinase B/B-cell lymphoma 2/caspase-3 signaling pathway.

2020年12月4日 · Herein, we demonstrate that Aldob suppresses Akt activity and tumor growth through a protein complex containing Aldob, Akt, and protein phosphatase 2A (PP2A), leading to inhibition of cell viability, cell cycle progression, glucose uptake, and metabolism.

2022年11月10日 · Here, we show that MASTL/Greatwall, a cell cycle kinase that supports mitosis by phosphorylating the PP2A/B55 inhibitors ENSA/ARPP19, inhibits PI3K‐AKT activity by sustaining mTORC1‐ and S6K1‐dependent phosphorylation of IRS1 and GRB10. Genetic depletion of MASTL results in an inefficient feedback loop and AKT hyperactivity.

蛋白磷酸酶 2A （PP2A） 是一种必需的抑癌基因，其活性在癌细胞中经常受到 SE 易位 （SET） 等内源性 PP2A 抑制蛋白的阻碍。 SET/PP2A 轴在癌细胞的集落形成能力以及与此过程相关的 c-Myc 和 E2F1 蛋白的稳定中起关键作用。 然而，在骨肉瘤细胞系 HOS 中，SET 敲低 （KD） 抑制集落形成能力，而不影响 c-Myc 和 E2F1。 本研究旨在揭示 SET 增强 HOS 细胞集落形成能力的分子机制，并确定它是否泛化到其他癌细胞。 转录组分析显示 SET KD 抑制 mTORC1 信号传 …

2020年2月2日 · Rescue experiments done with either non-phosphorylatable mutant cofilin-1 (S3A) transfection or an activator of the AKT pathway significantly reversed the inhibition effects of PP2 on liver cancer cells. Taken together, we report a potential agent for liver cancer treatment and reveal its underlying mechanisms.

pp2a 在异种移植肿瘤模型中抑制肿瘤生长和 vm 形成。pi3k 抑制剂 benc-511 可以增强 pp2a 的激活，从而在体外和体内抑制 p-akt/zeb1 和 vm 的形成。该研究表明，pp2a 可以通过 pi3k/akt/zeb1 轴调节 nsclc 中 vm 的形成。

More specifically, in SCC1483 and YD15PP2 HNSCC cell lines, PP2 exposure downregulated Erk, Akt/Slug, and Snail but upregulated E-cadherin. These results suggest that PP2 inhibits cell growth and progression in HNSCC by regulating the epithelial–mesenchymal transition pathway.

2008年9月15日 · Our results suggest that the nature of the synergistic interaction between PP2 and 5-FU and the observed chemo-sensitizing effect is most likely associated with the inhibition of EGFR–AKT ...

Penfluridol treatment decreased phosphorylation at PP2A targets c-MYC, AKT and GSK3β and caused cell death in a PP2A dependent manner. Importantly, penfluridol and the structurally unrelated PP2A activator FTY720 both displayed synergy …

3 天之前 · Pulmonary hypertension (PH) is a progressive and life-threatening cardiopulmonary disease that is not uncommon. The modulation of the pulmonary artery (PA) involves various fatty acids, including omega-6 polyunsaturated fatty acids (ω-6 PUFAs) and ω-6 PUFAs-derived oxylipins. These lipid mediators are produced through cyclooxygenase (COX), lipoxygenase (LOX), cytochrome P450 (CYP450), and ...