- |||||||||| Review, Journal: Class II PI3K Functions in Cell Biology and Disease. (Pubmed Central) - Feb 25, 2020
Increasing evidence suggests that the three class II PI3Ks isoforms (PI3K-C2α, PI3K-C2β, and PI3K-C2γ) have distinct and non-overlapping cellular roles. Here, we focus on the cellular functions of class II PI3Ks in different cell systems and underline the emerging importance of these enzymes in various physiological and pathological contexts.
- |||||||||| zoledronic acid / Generic mfg., Asahi Kasei
Journal: The Antitumor Effect of Lipophilic Bisphosphonate BPH1222 in Melanoma Models: The Role of the PI3K/Akt Pathway and the Small G Protein Rheb. (Pubmed Central) - Feb 25, 2020 Earlier, the prenylation inhibitor hydrophilic bisphosphonate zoledronic acid (ZA) was found to inhibit melanoma growth in vitro, but only a weaker effect was observed in vivo due to its hydrophilic properties...In vitro, only M24met cells were more sensitive to ZA than to BPH; however, in vivo growth of M24met was inhibited more strongly by BPH. Here, we present that lipophilic BPH is more effective on melanoma cells than ZA and identify the PI3K pathway, particularly Rheb as an important mediator of growth inhibition.
- |||||||||| Journal: YARS as an oncogenic protein that promotes gastric cancer progression through activating PI3K-Akt signaling. (Pubmed Central) - Feb 25, 2020
An improved mechanistic understanding of fusion genes will support the future identification of innovative therapeutic approaches for these challenging diseases. By revealing the existence of a YARS-PI3K-Akt signaling axis in gastric cancer, we discovered that tRNA synthetase YARS is a novel tumorigenic factor, characterized by its upregulation in tumor-derived specimens, as well as its functions in promoting gastric cancer progression.
- |||||||||| quercetin (LY294002) / Eli Lilly
Journal: Akirin1 promotes myoblast differentiation by modulating multiple myoblast differentiation factors. (Pubmed Central) - Feb 24, 2020 Similarly, we found that enhanced MEF2B expression by Akirin1 can be abrogated by treatment with LY294002, a PI3K inhibitor. Together, our results indicate that Akirin1 promotes myoblast differentiation by acting on the p38 and PI3K pathways and subsequently inducing the expression of myoblast differentiation factors.
- |||||||||| Visudyne (verteporfin) / Novartis
Preclinical, Journal: PI3K-Yap activity drives cortical gyrification and hydrocephalus in mice. (Pubmed Central) - Feb 24, 2020 Our data defines apical cell-adhesion as the earliest known substrate for cortical gyrification. In addition, our preclinical results support the testing of Yap-related small-molecule therapeutics for developmental hydrocephalus.
- |||||||||| doxorubicin hydrochloride / Generic mfg.
Journal, PARP Biomarker, IO Biomarker: Irisin Enhances Doxorubicin-Induced Cell Apoptosis in Pancreatic Cancer by Inhibiting the PI3K/AKT/NF-κB Pathway. (Pubmed Central) - Feb 24, 2020 Irisin attenuated serine/threonine kinase AKT (protein kinase B/PKB) phosphorylation and inhibited the activation of nuclear factor kappaB (NF-kappaB) signaling in PC cells. CONCLUSIONS Irisin can potentiate the cytotoxicity of doxorubicin in PC cells without increasing cardiotoxicity, possibly through inactivating the PI3K/AKT/NF-kappaB signaling pathway.
- |||||||||| Tevimbra (tislelizumab-jsgr) / BeiGene, Brukinsa (zanubrutinib) / BeiGene, BGB-10188 / BeiGene
New P1/2 trial, Combination therapy, Monotherapy: BGB-A317-3111-10188-101: Study of BGB-10188 as Monotherapy, and in Combination With Zanubrutinib, and Tislelizumab (clinicaltrials.gov) - Feb 24, 2020 P1/2, N=150, Not yet recruiting,
- |||||||||| Journal, IO Biomarker: Effect of MiRNA-145 on Apoptosis of Leukemia HuT 78 Cells and Its Mechanism (Pubmed Central) - Feb 23, 2020
Since this drug is currently used with relative low side effects, its repurposing may represent a new therapeutic opportunity for leukemia treatment. Upregulation of miRNA-145 may inhibit the proliferation of leukemia cells and promote the apoptosis, which may be related with the inhibition of PI3K/AKT signaling pathway.
- |||||||||| decitabine / Generic mfg., Nexavar (sorafenib) / Bayer, Amgen
Journal, PARP Biomarker, IO Biomarker: Mechanism of Sorafenib and Decitabine Inducing Apoptosis of Diffuse Large B-Cell Lymphoma Cells (Pubmed Central) - Feb 23, 2020 Upregulation of miRNA-145 may inhibit the proliferation of leukemia cells and promote the apoptosis, which may be related with the inhibition of PI3K/AKT signaling pathway. Sorafenib combined with decitabine induces the apoptosis of diffuse large B-cell lymphoma cell line OCI-LY1 by inhibiting PI3K-AKT pathway and activating P53.
- |||||||||| Preclinical, Journal, IO Biomarker: Panax ginseng C.A. Meyer (Rg3) Ameliorates Gastric Precancerous Lesions in Atp4a Mice via Inhibition of Glycolysis through PI3K/AKT/miRNA-21 Pathway. (Pubmed Central) - Feb 23, 2020
In conclusion, the findings of this study imply that abnormal glycolysis in GPL mice was relieved by Rg3 via regulation of the expressions of PI3K, AKT, mTOR, HIF-1α, LDHA, HK-II, and miRNA-21. Rg3 is an effective supplement for GPL treatment and can be harnessed to inhibit proliferation and induce apoptosis of GPL cells.
- |||||||||| Decadron (dexamethasone) / Merck (MSD), cyclophosphamide intravenous / Generic mfg.
Journal: Exon-4 Mutations in KRAS Affect MEK/ERK and PI3K/AKT Signaling in Human Multiple Myeloma Cell Lines. (Pubmed Central) - Feb 23, 2020 Specifically, KRAS, KRAS, KRAS, and KRAS were overexpressed in HEK293 cells and the KRAS MM cell lines JJN3 and OPM2 using lentiviral transduction and the Sleeping Beauty vector system. Even though KRAS-mutations were not correlated with survival, all KRAS-mutants were found capable of potentially activating MEK/ERK- and sustaining PI3K/AKT-signaling in MM cells.
- |||||||||| taselisib (GDC-0032) / Roche, paclitaxel / Generic mfg., docetaxel / Generic mfg.
Clinical, Journal, Combination therapy: A phase Ib, open-label, dose-escalation study of the safety and pharmacology of taselisib (GDC-0032) in combination with either docetaxel or paclitaxel in patients with HER2-negative, locally advanced, or metastatic breast cancer. (Pubmed Central) - Feb 21, 2020 P1 Despite evidence of antitumor activity, the benefit-risk profile was deemed not advantageous. Further development is not planned.
- |||||||||| quercetin (LY294002) / Eli Lilly
Journal: COX‑2 promotes epithelial‑mesenchymal transition and migration in osteosarcoma MG‑63 cells via PI3K/AKT/NF‑κB signaling. (Pubmed Central) - Feb 21, 2020 A Transwell chamber migration assay was performed to quantify the migration of the COX‑2‑transduced cells, and of cells treated with a COX‑2 inhibitor (NS398) or a PI3K inhibitor (LY294002)...The total protein levels of PI3K, AKT and IKK were not changed among the treatment groups. In summary, COX‑2 overexpression decreased the expression levels of the epithelial protein E‑cadherin and increased the expression levels of the mesenchymal proteins vimentin, MMP‑2 and MMP‑9, as well as promoted cell migration, by activating the PI3K/AKT/NF‑κB signaling pathway.
|