- |||||||||| quercetin (LY294002) / Eli Lilly
Journal, IO biomarker: The protective effect of decoction of Rehmanniae via PI3K/Akt/mTOR pathway in MPP-induced Parkinson's disease model cells. (Pubmed Central) - Oct 6, 2021 To further determine the protective effect of DOR on acute injury via PI3K/Akt/mTOR pathway, cells were treated with LY294002 (LY), a PI3K/Akt/mTOR pathway inhibitor, with MMP + or DOR or not...DOR had a protective effect against MPP induced injury of Parkinson's disease model cell through activating the PI3K/Akt/mTOR pathway. It suggests that DOR should be further explored in Parkinson's disease.
- |||||||||| quercetin (LY294002) / Eli Lilly
Preclinical, Journal: Regulation mechanism of miR-494-3p on endometrial receptivity in mice via PI3K/AKT/mTOR pathway. (Pubmed Central) - Oct 5, 2021 Subsequently, human endometrial epithelial cells (hEECs) were transfected with miR-494-3p inhibitor and PI3K inhibitor (LY294002)...Overall, these results suggested that miR-494-3p is the key regulator of endometrial receptivity in mice, regulating this complex process through the PI3K/AKT/mTOR pathway. Understanding the role of miR-494-3p in endometrial receptivity is of great significance for exploring new targets for the diagnosis and treatment of early pregnancy failure, and improving the success rates of artificial reproduction.
- |||||||||| Erbitux (cetuximab) / Eli Lilly, EMD Serono, buparlisib (AN2025) / Novartis, Adlai Nortye
Biomarker, Trial completion, Combination therapy, Metastases: PI3K Inhibitor BKM120 and Cetuximab in Treating Patients With Recurrent or Metastatic Head and Neck Cancer (clinicaltrials.gov) - Oct 5, 2021 P1/2, N=12, Completed, Collectively, SLSP attenuated excessive autophagy and apoptosis in myocardial cells in heart tissue induced by SD, which might be acted through activating PI3K/Akt/mTOR signaling pathway. Active, not recruiting --> Completed
- |||||||||| Zyclara (imiquimod) / Mochida, Viatris, Bausch Health
Journal: Yangxue Jiedu Fang Ameliorates Psoriasis by Regulating Vascular Regression via Survivin/PI3K/Akt Pathway. (Pubmed Central) - Oct 3, 2021 In this study, we explored the effects of YXJD on angiogenesis and apoptosis of microvessels in PA, the underlying mechanisms in HUVEC cells transfected by Survivin overexpression plasmid and in a mouse model of imiquimod-induced psoriasis and the relationship between VEGF (vascular endothelial growth factor) and Survivin...YXJD inhibited the expression of Survivin via PI3K/Akt pathway to adjust apoptosis, autophagy, and angiogenesis of microvessels and thus improve the vascular sustainability in psoriasis. YXJD may represent a new direction of drug research and development for immunomodulatory therapy for psoriasis.
- |||||||||| Preclinical, Journal: Identification of Potential Kinase Inhibitors within the PI3K/AKT Pathway of Leishmania Species. (Pubmed Central) - Oct 3, 2021
In the case of Leishmania GSK3, an inhibitor of its human counterpart, prioritized by our method, was validated in vitro to test its anti-Leishmania activity and indirectly infer the presence of the enzyme in the parasite. The analysis contributes to improving the knowledge about the presence of similar signalling pathways in Leishmania, as well as the discovery of compounds acting against any of these kinases as potential molecular targets in the parasite.
- |||||||||| Journal: PPA1 Promotes Breast Cancer Proliferation and Metastasis Through PI3K/AKT/GSK3β Signaling Pathway. (Pubmed Central) - Oct 2, 2021
Moreover, PI3K inhibitors suppress the signaling pathways mediating the effects of PPA1 on breast cancer, resulting in tumor growth and metastasis suppression in vitro and in vivo. In summary, our results verify that PPA1 can act as an activator of PI3K/AKT/GSK3β/Slug-mediated breast cancer progression and that it is a potential therapeutic target for the inhibition of tumor progression.
- |||||||||| Journal: MiR155 modulates vascular calcification by regulating Akt-FOXO3a signalling and apoptosis in vascular smooth muscle cells. (Pubmed Central) - Oct 2, 2021
A PI3K inhibitor that suppresses Akt phosphorylation increased, whereas a pan-caspase inhibitor that suppresses apoptosis reduced VSMC calcification; and both inhibitors diminished the protective effects of miR155 deficiency on VSMC calcification. In conclusion, miR155 deficiency attenuates vascular calcification by increasing Akt phosphorylation and FOXO3a degradation, and thus reducing VSMC apoptosis induced by calcification medium.
- |||||||||| MK-2206 / Merck (MSD)
Journal, IO biomarker: Gastrodin prevents homocysteine-induced human umbilical vein endothelial cells injury via PI3K/Akt/eNOS and Nrf2/ARE pathway. (Pubmed Central) - Oct 2, 2021 Moreover, the protective effects of Gas on NO production and relaxation of thoracic aortic rings were blocked by L-NAME but enhanced by Cav-1 knockdown, and MK-2206 treatment abolished the effect of Gas on the ROS...Finally, gastrodin increased the expression of PI3K, p-Akt, and eNOS and decreased Cav-1 protein expression. In conclusion, our study suggested that gastrodin may protect HUVECs from homocysteine-induced injury, and the PI3K/Akt/eNOS and Nrf2/ARE pathways may be responsible for the efficacy of gastrodin.
- |||||||||| PIK3IP1/TrIP Immune Regulation on CD8+ T Cells Restricts Anti-Tumor Immunity (Poster Hall) - Oct 1, 2021 - Abstract #SITC2021SITC_509;
Our that CD8+ T cell-specific TrIP knockout mice are resistant to tumor challenge and show more robust tumor CD8+ T cell infiltrate. With these data, we are excited to propose TrIP as a potential future immunotherapeutic target worthy of continued investigation.
- |||||||||| Tagrisso (osimertinib) / AstraZeneca, Orpathys (savolitinib) / AstraZeneca, Hutchmed
Preclinical, Journal, Heterogeneity: Brief Report: Heterogeneity of Acquired Resistance Mechanisms to Osimertinib and Savolitinib. (Pubmed Central) - Oct 1, 2021 Patient 2 harbored an acquired PIK3CA p.H1047R mutation in which resistance could be overcome with combination of PI3K inhibitor and osimertinib in the patient-derived xenograft model. Our study reveals that acquired resistance to savolitinib plus osimertinib can occur from both MET-dependent and MET-independent mechanisms.
- |||||||||| quercetin (LY294002) / Eli Lilly
Journal: Extracellular vesicle-encapsulated microRNA-425-derived from drug-resistant cells promotes non-small-cell lung cancer progression through DAPK1-medicated PI3K/AKT pathway. (Pubmed Central) - Oct 1, 2021 Cell proliferation, invasion, migration and apoptosis after treatment of P-EVs, R-EVs, miR-425 inhibitor, miR-425 mimic, pcDNA-MED1, or phosphatidylinositol-3-kinase (PI3K)/AKT inhibitor LY294002 were detected...Moreover, miR-425 delivered by R-EVs promoted tumorigenesis in vivo. Taken together, the result suggested that EVs-delivered miR-425-derived from A549-R cells promoted the progression of NSCLC through regulating DAPK1-medicated PI3K/AKT signaling pathway.
- |||||||||| glibenclamide / Generic mfg., verapamil / Generic mfg.
Preclinical, Journal: Gentiopicroside Produces Endothelium-Independent Vasodilation by Deactivating the PI3K/Akt/Rho-Kinase Pathway in Isolated Rat Thoracic Aorta. (Pubmed Central) - Oct 1, 2021 Additionally, the vasorelaxation activity of GPS was attenuated upon pretreatment with LY294002 (PI3K/Akt inhibitor), Y27632 (Rho-kinase inhibitor), and verapamil (L-type Ca channel inhibitor). These findings demonstrate that GPS exhibits endothelium-independent vasorelaxant effects through inhibition of voltage-dependent, receptor-operated, and inositol triphosphate receptor (IPR)/ryanodine receptor- (RYR-) mediated Ca channels as well as the PI3K/Akt/Rho-kinase signaling pathway.
- |||||||||| Oncopore (ruxotemitide) / Verrica
Journal, PARP Biomarker, IO biomarker: Polypeptide LTX-315 reverses the cisplatin chemoresistance of ovarian cancer cells via regulating Beclin-1/PI3K/mTOR signaling pathway. (Pubmed Central) - Oct 1, 2021 These findings demonstrate that GPS exhibits endothelium-independent vasorelaxant effects through inhibition of voltage-dependent, receptor-operated, and inositol triphosphate receptor (IPR)/ryanodine receptor- (RYR-) mediated Ca channels as well as the PI3K/Akt/Rho-kinase signaling pathway. LTX-315 can inhibit the resistance of OC cells to DDP in vitro and plays a role by regulating Beclin-1/phosphatidylinositol-3-kinase/mTOR signaling pathway.
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