- |||||||||| Journal: Solid lipid nanoparticle of hesperidine exerts diethylnitrosamine/phenobarbital-induced hepatocellular carcinoma via alteration of PI3K/Akt pathway. (Pubmed Central) - Jul 8, 2021
HP-SLN significantly (p < 0.001) modulated the hepatic parameter viz., AFP (78.3%), AST (61.3%), ALP (60.3%), ALT (55.8%), CEA (58.3%), GGT (63.2%); non-hepatic parameter viz., albumin (52.5%), total protein (63.4%), BUN (54.6%), bilirubin (67.3%), direct bilirubin (52.3%); antioxidant. In conclusion, HP-SLN regulated the Akt and PI3K pathways involved in suppression of hepatic cancer growth and proliferation and suggest the chemoprotective effect.
- |||||||||| 5-fluorouracil / Generic mfg.
Journal: Ginsenoside Rg3 enhances the anticancer effect of 5‑FU in colon cancer cells via the PI3K/AKT pathway. (Pubmed Central) - Jul 8, 2021 Chemotherapy is one of the most commonly used treatments for patients with advanced colon cancer, yet the toxicity of chemotherapy agents, such as 5‑fluorouracil (5‑FU), limits the effectiveness of chemotherapy...Similarly, combined treatment of Rg3 and 5‑FU altered the expression of colon cancer protein in vivo and in vitro. Collectively, the present study demonstrated that ginsenoside Rg3 enhances the anticancer effect of 5‑FU in colon cancer cells via the PI3K/AKT pathway.
- |||||||||| fimepinostat (CUDC-907) / Curis, Lynparza (olaparib) / Merck (MSD), AstraZeneca
Journal: The dual HDAC-PI3K inhibitor CUDC-907 displays single-agent activity and synergizes with PARP inhibitor olaparib in small cell lung cancer. (Pubmed Central) - Jul 8, 2021 The results of the present study suggest that SPAG6 may play a key role in the progression of BL and may be of value as a predictive prognostic biomarker in patients with BL. Our study uncovers that dual PI3K and HDAC inhibition by CUDC-907 exerts significant single-agent activity and strong synergistic effects with PARP inhibitor olaparib in SCLC, which thus provides a rational combination treatment strategy for SCLC clinical investigation.
- |||||||||| pictilisib (GDC-0941) / Roche
Preclinical, Journal: Fenhexamid induces cancer growth and survival via estrogen receptor-dependent and PI3K-dependent pathways in breast cancer models. (Pubmed Central) - Jul 8, 2021 The WST assay, live cell monitoring, cell cycle analysis, colony formation assay, apoptotic analysis by JC-1 dyeing, and Western blot analysis were applied in ER positive MCF-7 and ER negative MDA-MB-231 breast cancer cells, after exposure to 17β-estradiol (E2), Fen, ICI 182,780 (ICI; an ER antagonist) and/or Pictilisib (Pic; a PI3K inhibitor)...Taken together, these results indicate that Fen promotes the growth of breast cancer cells via the ER and/or PI3K pathways, similar to the E2 mechanism. Although a relatively safe pesticide, Fen possibly exerts its influence as an endocrine disrupting chemical in ER-positive breast cancer cells via the ER and PI3K pathways.
- |||||||||| quercetin (LY294002) / Eli Lilly
Journal, Epigenetic controller: The histone demethylase KDM2B activates FAK and PI3K that control tumor cell motility. (Pubmed Central) - Jul 7, 2021 In line with this, the p85-PI3 K-subunit was downregulated upon knockdown of KDM2B in DU-145 cells, while the opposite effect became evident in KDM2B-overexpressing cells. These results revealed a novel functional role of KDM2B in regulating the activation of the FAK/PI3 K signaling in prostate cancer cells that participates in the control of cell motility.
- |||||||||| Livalo (pitavastatin) / Kowa, Eli Lilly
Journal, PARP Biomarker: Pitavastatin and metformin synergistically activate apoptosis and autophagy in pancreatic cancer cells. (Pubmed Central) - Jul 7, 2021 These findings clearly indicated that metformin plus pitavastatin had a synergistic anticancer effect on pancreatic cancer cells, potentially caused due to the activation of AMPK and inhibition of PI3K/mTOR signaling. Altogether, our results provide that use of metformin plus pitavastatin maybe serve as a chemotherapeutic agent for human pancreatic cancer in future.
- |||||||||| Journal: Targeting DNAJC19 overcomes tumor growth and lung metastasis in NSCLC by regulating PI3K/AKT signaling. (Pubmed Central) - Jul 6, 2021
Taken together, our results showed that Se-Y has an added value to antagonize Cd-induced necroptosis in chicken kidney by regulating the miR-26a-5p/PTEN/PI3K/AKT signaling pathway and HSPs, indicating that Se-Y could serve as an effective antagonist on Cd-induced renal necroptosis in chickens. DNAJC19 greatly promotes NSCLC cell growth and lung metastasis by regulating PI3K/AKT signaling, providing a novel therapeutic target for treating NSCLC patients.
- |||||||||| Epidaza (chidamide) / Chipscreen, Meiji Seika, Eisai, HUYA Bioscience
Journal, IO biomarker: Chidamide Inhibits Cell Proliferation via the PI3K/AKT Pathway in K562 Cells Based on Network Pharmacology and Experimental Validation. (Pubmed Central) - Jul 6, 2021 DNAJC19 greatly promotes NSCLC cell growth and lung metastasis by regulating PI3K/AKT signaling, providing a novel therapeutic target for treating NSCLC patients. The study demonstrated that Chidamide may inhibit the proliferation of K562 cells by promoting cell cycle arrest and apoptosis via suppressing the PI3K/AKT pathway, suggesting that Chidamide could be a promising approach to the treatment of CML.
- |||||||||| torkinib (PP242) / Takeda, UCSF Medical Center
Journal: Connectivity Map Analysis Indicates PI3K/Akt/mTOR Inhibitors as Potential Anti-Hypoxia Drugs in Neuroblastoma. (Pubmed Central) - Jul 4, 2021 A heat map representation of hypoxia-modulated genes in the Mohlin dataset and the gene set enrichment analysis (GSEA) showed an opposite regulation of these genes in the set of NB cells treated with the mTORC inhibitor PP242. In conclusion, our analysis identified inhibitors of the PI3K/Akt/mTOR signaling pathway as novel candidate compounds to treat NB patients with hypoxic tumors and a poor prognosis.
- |||||||||| Previfenon (epigallocatechin gallate) / MELISA Institute
Preclinical, Journal: Green Tea Polyphenol Catechins Inhibit Coronavirus Replication and Potentiate the Adaptive Immunity and Autophagy-Dependent Protective Mechanism to Improve Acute Lung Injury in Mice. (Pubmed Central) - Jul 4, 2021 We found that catechins containing 32.8% epigallocatechin gallate, 15.2% epicatechin gallate, 13.2 epicatechin, 10.8% epigallocatechin, 10.4% gallocatechin, and 4.4% catechin directly inhibited SARS-CoV replication at sub-micromolecular concentrations...Pretreatment of autophagy inhibitor 3-Methyladenine reversed the inhibiting effects of catechins on the cytokines and oxidative stress levels and ALI. In conclusion, our data indicated that catechins directly inhibited SARS-CoV replication, potentiated the CD25/CD69/CD94/CD8 T lymphocytes-mediated adaptive immunity and attenuated lipopolysaccharide-induced ALI and cytokine storm by PI3K/AKT/mTOR-signaling-mediated autophagy, which may be applied to prevent and/or treat SARS-CoV infection.
- |||||||||| Review, Journal, IO biomarker: Challenges with Approved Targeted Therapies against Recurrent Mutations in CLL: A Place for New Actionable Targets. (Pubmed Central) - Jul 4, 2021
The effect of these new targeted therapies has been widely analyzed in TP53-mutated cases, but few data exist about the response of patients carrying other recurrent mutations. In this review, we describe the biological pathways recurrently altered in CLL that might have an impact on the response to these new therapies together with the possibility to use new actionable targets to optimize treatment responses.
- |||||||||| dactolisib (RTB101) / Adicet Bio
Clinical, P1 data, Journal: A phase I study of a dual PI3-kinase/mTOR inhibitor BEZ235 in adult patients with relapsed or refractory acute leukemia. (Pubmed Central) - Jul 4, 2021 P1 In this review, we describe the biological pathways recurrently altered in CLL that might have an impact on the response to these new therapies together with the possibility to use new actionable targets to optimize treatment responses. Combined inhibition of PI3K and mTOR inhibits a clinically meaningful driver pathway in a small subset of patients with ALL, with no benefit in patients with AML.
- |||||||||| Journal: Fibronectin 1 inhibits the apoptosis of human trophoblasts by activating the PI3K/Akt signaling pathway. (Pubmed Central) - Jul 4, 2021
Consistently, the apoptosis‑inhibiting effect of FN1 overexpression was reversed by a PI3K/Akt signaling pathway inhibitor, and the apoptosis‑promoting effect of FN1 silencing was reversed by a PI3K/Akt signaling pathway activator. On the whole, the findings of the present study demonstrate that the inhibition of FN1 induces the apoptosis of JEG‑3 and BeWo cells, and the overexpression of FN1 inhibits cell apoptosis by activating the PI3K/Akt signaling pathway.
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