- |||||||||| Venclexta (venetoclax) / Roche, AbbVie
[VIRTUAL] Managing Toxicities of Targeted Therapies in CLL - Live Q&A (Channel 2 (Virtual Meeting)) - Oct 11, 2020 - Abstract #ASH2020ASH_45; The last 5-10 years have been an incredible time for patients with CLL given the advent of novel agents such as venetoclax, BTK and PI3K inhibitors...Danielle Brander will discuss the identification and management of the early and late onset toxicities that can arise with the use of phosphoinositide-3-kinase (PI3K) inhibitors for treatment of patients with CLL. This will include a review of clinical trials investigating next generation PI3K inhibitors, combination therapy, and/or dosing schedules that may mitigate toxicity risk.
- |||||||||| Journal: Electrotaxis of Glioblastoma and Medulloblastoma Spheroidal Aggregates. (Pubmed Central) - Oct 11, 2020
Further, using selective pharmacological inhibition assays, focused on the PI3K/mTOR/AKT signaling axis, we validate whether there is a causal relationship to electrotaxis and these mechanisms of action. We find that U87 mg electrotaxis is abolished under pharmacological inhibition of PI3Kγ, mTOR, AKT and ErbB2 signaling, whereas DAOY cell electrotaxis was not attenuated by these or other pathways evaluated.
- |||||||||| Review, Journal: Modeling human disease in yeast: recreating the PI3K-PTEN-Akt signaling pathway in Saccharomyces cerevisiae. (Pubmed Central) - Oct 11, 2020
Here, we briefly review the use of S. cerevisiae as a tool to study human oncogenes and tumor suppressors, and we present an overview of the models applied to the study of the PI3K oncoproteins, the tumor suppressor PTEN, and the Akt protein kinase. We discuss the application of these models to study the basic functional properties of these signaling proteins, the functional assessment of their clinically relevant variants, and the design of feasible platforms for drug discovery.
- |||||||||| Journal: MiR-181d inhibits cell proliferation and metastasis through PI3K/AKT pathway in gastric cancer. (Pubmed Central) - Oct 10, 2020
MiR-181d functioned as a tumor suppressor by inhibiting the proliferation via PI3K/AKT pathway in vitro and in vivo and inhibiting invasion-mediated epithelial-mesenchymal transition (EMT) by targeting CYLD in gastric cancer. The newly identified miR-181d/CYLD axis provides novel insight into the pathogenesis of gastric cancer.
- |||||||||| ANXV / Annexin
Journal, IO Biomarker: Calcium relieves fluoride-induced bone damage through the PI3K/AKT pathway. (Pubmed Central) - Oct 10, 2020 On the other hand, CaCO3 supplementation reversed the histopathological injury along with the levels of ALP, StrACP and serum Ca, alleviating the gene expression levels of PI3K/AKT pathway-related markers. Altogether, we can conclude that CaCO3 supplementation mitigated F-induced bone damage via the PI3K/AKT signaling pathway.
- |||||||||| sirolimus / Generic mfg.
Journal: Human-origin Lactobacillus salivarius AR809 protects against immunosuppression in S. aureus-induced pharyngitis via Akt-mediated NF-κB and autophagy signaling pathways. (Pubmed Central) - Oct 10, 2020 AR809 also attenuated S. aureus-induced phosphorylations of protein kinase B (Akt) and rapamycin (mTOR), and elevated the autophagic protein (light chain 3 from II (LC3-II) and Beclin-1) level...Likewise, 740Y-P (a PI3K activator) decreased the anti-inflammatory effect of AR809 against S. aureus-induced inflammatory response, while AR809 treatments with wortmannin (a PI3K inhibitor) markedly reversed this inflammatory response. AR809 prevents S. aureus-induced pharyngeal inflammatory response, possibly by regulating TLR/PI3K/Akt/mTOR signalling pathway-related autophagy and TLR/PI3K/Akt/IκB/NF-κB pathway activity, and therefore has potential for use in preventing pharyngitis and other inflammatory diseases.
- |||||||||| Journal, IO Biomarker: p110δ PI3K as a therapeutic target of solid tumours. (Pubmed Central) - Oct 9, 2020
Furthermore, p110δ selective inhibitors are being studied as potential single agent treatments or as combination partners in attempt to improve cancer immunotherapy, with both strategies to shown great promise for the treatment of several solid tumours. In this review, we discuss the evidence implicating the p110δ PI3K in human solid tumours, their impact on the current state of the field and the potential of using p110δ-selective inhibitors as monotherapy or combined therapy in different cancer contexts.
- |||||||||| Review, Journal: Targeting the phosphoinositide-3-kinase/protein kinase B pathway in airway innate immunity. (Pubmed Central) - Oct 8, 2020
Moreover, Akt can increase the activity of the transcription factor nuclear factor erythroid 2 related factor-2 that protects cells from oxidative stress and may limit inflammation. In this review, we summarize the recent findings of non-cancerous functions of Akt signaling in airway innate host defense mechanisms, including an overview of several known downstream targets of Akt involved in innate immunity.
- |||||||||| quercetin (LY294002) / Eli Lilly
Preclinical, Journal: Inhibition of TRPA1 Promotes Cardiac Repair in Mice after Myocardial Infarction. (Pubmed Central) - Oct 8, 2020 However, treatment of HUVECs with a PI3K inhibitor, LY294002 before HC administration almost completely abolished HC-induced migration in HUVECs. In conclusion, we demonstrate that inhibition of TRPA1 promotes angiogenesis after MI thereby alleviating myocardial ischemia injury via mechanisms involving inhibition of PTEN expression, and subsequent activation of the PI3K/Akt signaling.
- |||||||||| Journal: Alantolactone suppresses human osteosarcoma through the PI3K/AKT signaling pathway. (Pubmed Central) - Oct 8, 2020
It was hypothesized that the antitumor functions of ALT are mediated through inhibition of the PI3K/AKT signaling pathway. In conclusion, the results of the present study confirmed the inhibition of ALT on osteosarcoma cells via downregulation of PI3K/AKT signaling pathways, suggesting ALT as a potential therapeutic candidate for osteosarcoma.
- |||||||||| benzesulfonate (PF-562271) / Pfizer, quercetin (LY294002) / Eli Lilly
Journal: Antiangiogenic effects of AG36, a triterpenoid saponin from Ardisia gigantifolia stapf. (Pubmed Central) - Oct 8, 2020 Molecular docking simulation indicated that AG36 formed hydrogen bonds and hydrophobic interactions within the ATP binding pocket of VEGFR2 kinase domain. The present study firstly revealed the high antiangiogenic potency and related underlying molecular of AG36, demonstrating that AG36 maybe a potential antiangiogenic cancer therapy agent or lead candidate.
- |||||||||| quercetin (LY294002) / Eli Lilly
[VIRTUAL] LY294002 Improves the Collagen-induced Arthritis by Inducing Neutrophil Apoptosis () - Oct 8, 2020 - Abstract #ACRARHP2020ACR_ARHP_1411; The present study firstly revealed the high antiangiogenic potency and related underlying molecular of AG36, demonstrating that AG36 maybe a potential antiangiogenic cancer therapy agent or lead candidate. This data suggested that delayed apoptosis of neutrophils played an important role in the development of RA, therefore, inhibition of PI3K pathway to facilitate neutrophil apoptosis are possible approaches to reduce inflammatory arthritis which might open new doors to future clinical treatment of RA.
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