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343 Trials |  |
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- |||| Precision Medicine Approaches Evolving With CDK4/6, PI3K Inhibitors in HR+ #BreastCancer #bcsm @stolaney1 @DanaFarber @harvardmed https://t.co/zFpqTQp5Gr (Twitter) - Feb 21, 2020
- PI3K inhibition + PD-1 inhibition (STARLIGHT BALLROOM) - Feb 21, 2020 - Abstract #IASLCLCTT2020IASLC_LCTT_307;
- S14 - mTOR/PI3K/CDK/DNA repair/CHK1/Wee1/PARP inhibition (STARLIGHT BALLROOM) - Feb 21, 2020 - Abstract #IASLCLCTT2020IASLC_LCTT_299;
- | lansoprazole / Generic mfg.
Journal, IO Biomarker: Protocatechuic acid-mediated DJ-1/PARK7 activation followed by PI3K/mTOR signaling pathway activation as a novel mechanism for protection against ketoprofen-induced oxidative damage in the gastrointestinal mucosa. (Pubmed Central) - Feb 20, 2020
The administration of lansoprazole, a type of proton pump inhibitor (PPI), strongly inhibited ketoprofen-induced GI mucosal injuries via up-regulation of DJ-1, indicating that DJ-1 is essential for the dietary antioxidant- and PPI drug-mediated mechanism of ulcer therapy. These results suggest that DJ-1 could be a novel target for protection against ketoprofen-induced GI ulcers due to its antioxidant and anti-apoptosis characteristics.
- || buparlisib (BKM120) / Novartis, Adlai Nortye
Clinical, P2 data, Journal: Buparlisib in Patients With Recurrent Glioblastoma Harboring Phosphatidylinositol 3-Kinase Pathway Activation: An Open-Label, Multicenter, Multi-Arm, Phase II Trial. (Pubmed Central) - Feb 20, 2020
Although buparlisib achieved significant brain penetration, the lack of clinical efficacy was explained by incomplete blockade of the PI3K pathway in tumor tissue. Integrative results suggest that additional study of PI3K inhibitors that achieve more-complete pathway inhibition may still be warranted.
- ||||| Mekinist (trametinib) / Novartis, uprosertib (UPB795) / Laekna, trametinib
Clinical, Combination therapy: Phase I dose-escalation trial of the oral AKT inhibitor uprosertib in combination with the oral MEK1/MEK2 inhibitor trametinib in patients with solid tumors | co inhibiting PI3k and AKT pathway is again toxic https://t.co/odxQ90Q98O (Twitter) - Feb 20, 2020
- | Preclinical, Journal: Elabela protects against podocyte injury in mice with streptozocin-induced diabetes by associating with the PI3K/Akt/mTOR pathway. (Pubmed Central) - Feb 20, 2020
Furthermore, Elabela acts through the phosphoinositide 3-kinase /Akt/mammalian target of rapamycin signaling pathway and decreases podocyte apoptosis, thereby exhibiting a nephroprotective effect against diabetic nephropathy. Our findings provide the first evidence that Elabela has a potential renoprotective effect in patients of diabetes.
- | sirolimus / Generic mfg.
Journal: Carnosine inhibits glioblastoma growth independent from PI3K/Akt/mTOR signaling. (Pubmed Central) - Feb 20, 2020
Therefore, glioblastoma cells from the lines U87 and T98G were exposed to carnosine, to the mTOR inhibitor rapamycin and to the PI3K inhibitor Ly-294,002...We conclude that carnosine's anti-neoplastic effect is independent from PI3K/Akt/mTOR signaling. As the dipeptide reduced viability in tumor cells that do not respond to PI3K or mTOR inhibitors, it appears to be worth to further investigate the mechanisms by which carnosine exerts its anti-tumor effect and to consider it for therapy, especially as it is a naturally occurring compound that has already been used for the treatment of other diseases without indication of side-effects.
- | voxtalisib (SAR245409) / Sanofi
Journal: Anticancer compound XL765 as PI3K/mTOR dual inhibitor: A structural insight into the inhibitory mechanism using computational approaches. (Pubmed Central) - Feb 20, 2020
The virtual screening of the generated compound library led to identification of six novel promising compounds proposed as PI3K/mTOR dual inhibitors. Thus, the present work will through light on the drug inhibitory mechanism of XL765 for PI3K and mTOR, and will also assist in designing novel efficacious drug candidates.
- [VIRTUAL] Weighted burden analysis of exome-sequenced late onset Alzheimer's cases and controls provides further evidence for involvement of PSEN1 and demonstrates role for PI3K/Akt/GSK-3β signalling pathway (Station 02) - Feb 20, 2020 - Abstract #EPA2020EPA_3432;
The results provide further evidence that disruption of the PI3K/Akt/GSK-3β signalling pathway can increase risk of LOAD while enhancement of signalling through reduction of tyrosine phosphatase inhibition can reduce risk. Variants in C1R might increase risk via a direct effect of complement activity in the brain or indirectly mediated through encouraging periodontitis and P. gingivalis infection.
- [VIRTUAL] 'Research Domain Criteria' in context: PI3K/PDK1/PKB signaling pathway, fear, anxiety and cognitive deficits (Station 11) - Feb 20, 2020 - Abstract #EPA2020EPA_656;
Variants in C1R might increase risk via a direct effect of complement activity in the brain or indirectly mediated through encouraging periodontitis and P. gingivalis infection. The present results contribute to the in vivo characterization of the behavioral impact of PKB/Akt signal pathway dysfunction and support the conceptualization of qualitative and quantitative variations of neural circuit disruptions underpinning phenotypic differences that are relevant to several mental disorders.
- | cordycepin (OVI-123) / OncoVista
Journal: Cordycepin induces apoptosis in human bladder cancer T24 cells through ROS-dependent inhibition of the PI3K/Akt signaling pathway. (Pubmed Central) - Feb 20, 2020
Furthermore, the presence of NAC significantly attenuated the enhanced apoptotic cell death and reduction of cell viability by treatment with cordycepin and LY294002. Collectively, the data indicate that cordycepin induces apoptosis through the activation of extrinsic and intrinsic apoptosis pathways and the ROS-dependent inactivation of PI3K/Akt signaling in human bladder cancer T24 cells.
- | Journal: Lupiwighteone induces caspase-dependent and -independent apoptosis on human breast cancer cells via inhibiting PI3K/Akt/mTOR pathway. (Pubmed Central) - Feb 20, 2020
We also showed that treatment with lupiwighteone induced caspase-dependent apoptosis (up-regulation of caspase-3, -7, -8, -9, PARP, and Bax or down-regulation of Bid, Bcl-2), induction of caspase-independent apoptosis (up-regulation of AIF and Endo G on cytosol), and inhibition of the PI3K/Akt/mTOR signaling pathway (down-regulation of PI3K, p-Akt, and p-mTOR) in both MCF-7 and MDA-MB-231 cells. These results suggest that lupiwighteone induces caspase-dependent and -independent apoptosis in both breast cancer cell lines via inhibiting PI3K/Akt/mTOR pathway.
- || Piqray (alpelisib) / Novartis, Erbitux (cetuximab) / Eli Lilly, EMD Serono
P1 data, Journal: A Phase Ib Study of Cetuximab and BYL719 (Alpelisib) Concurrent with Intensity-Modulated Radiation Therapy in Stage III-IVB Head and Neck Squamous Cell Carcinoma. (Pubmed Central) - Feb 20, 2020
The recommended phase II dose of BYL719 is 250 mg/day in combination with cetuximab and IMRT in patients with locally advanced HNSCC. Further evaluation of the addition of BYL719 to the platinum-sparing regimen of cetuximab and IMRT in the treatment of locally advanced HNSCC is warranted.
- | Journal: Insulin-Like Growth Factor-1 Down-Regulates the Phosphorylation of FXYD1 and Rescues Behavioral Deficits in a Mouse Model of Rett Syndrome. (Pubmed Central) - Feb 19, 2020
Interestingly, blocking the PI3K/AKT pathway by PI3K inhibitor could abolish the effect of IGF-1 on p-FXYD1 level, in addition to the effect of IGF-1 on the phosphorylation of other components in the PI3K/AKT pathway. Thus, our study has provided new insights into the mechanism of IGF-1 treatment for RTT, which appears to involve FXYD1.
- | quercetin (LY294002) / Eli Lilly
Journal: HMGB1 Protects the Heart Against Ischemia-Reperfusion Injury via PI3K/AkT Pathway-Mediated Upregulation of VEGF Expression. (Pubmed Central) - Feb 19, 2020
However, these effects of HMGB1 were abolished by LY294002. The obtained results demonstrate that the cardioprotective effects of intravenous administration of HMGB1 prior to I/R may be mediated by upregulation of myocardial expression of VEGF, which may activate the PI3K/Akt signaling pathway.
- | quercetin (LY294002) / Eli Lilly
Preclinical, Journal, IO Biomarker: Exercise Preconditioning Plays a Protective Role in Exhaustive Rats by Activating the PI3K-Akt Signaling Pathway. (Pubmed Central) - Feb 19, 2020
However, the cardioprotective effects of EP were attenuated when pretreated with the LY294002. EP protected the heart from EE-induced injury, and it may improve the cardiac function and reduce the cardiomyocyte apoptosis by activating the PI3K-Akt signaling pathway.
- | Journal: The aberrant expression of ADAR1 promotes resistance to BET inhibitors in pancreatic cancer by stabilizing c-Myc. (Pubmed Central) - Feb 19, 2020
Moreover, we reveal that EZH2 regulates ADAR1 expression, and EZH2 and BET inhibitors show synergistic inhibition in pancreatic cancer. Collectively, these findings suggest that ADAR1 could serve as a new diagnostic and prognostic marker for the treatment of pancreatic cancer.
- | doxorubicin hydrochloride / Generic mfg.
Journal: Econazole nitrate reversed the resistance of breast cancer cells to Adriamycin through inhibiting the PI3K/AKT signaling pathway. (Pubmed Central) - Feb 19, 2020
The combination of econazole and Adriamycin exerted synergistic inhibitory effects in breast cancer cells in vitro and in vivo. Taken together, the PI3K inhibitor econazole could effectively overcome Adriamycin resistance and showed synergistic effects with chemotherapy on breast cancer.
- Piqray (alpelisib) / Novartis
Treatment Considerations for Patients With Advanced Breast Cancer Who Receive Alpelisib After CDK4/6 Inhibitor-Based Therapy (Henry B. Gonzalez Convention Center - Tower View Registration) - Feb 17, 2020 - Abstract #ONS2020ONS_239;
P2
There were no safety signals such as mood disorders or other off-target effects associated with pan-PI3K inhibitor treatment. Due to the rapid onset of hyperglycemia, frequent glucose monitoring (once/week for the first 2 weeks then at least once/month) is recommended upon alpelisib initiation.
- | Journal: Correction: Hypoxic Tumor-Derived Exosomal miR-301a Mediates M2 Macrophage Polarization via PTEN/PI3Kγ to Promote Pancreatic Cancer Metastasis. (Pubmed Central) - Feb 17, 2020
Due to the rapid onset of hyperglycemia, frequent glucose monitoring (once/week for the first 2 weeks then at least once/month) is recommended upon alpelisib initiation. No abstract available
- | gedatolisib (PF-05212384) / Celcuity
Trial completion date, Trial primary completion date, Metastases: An Initial Safety Study of Gedatolisib Plus PTK7-ADC for Metastatic Triple-negative Breast Cancer (clinicaltrials.gov) - Feb 17, 2020
P1, N=18, Recruiting, Sponsor: Kathy Miller
No abstract available Trial completion date: Jun 2020 --> Jun 2021 | Trial primary completion date: Jan 2020 --> Jan 2021
- | paclitaxel / Generic mfg.
Journal: PI3K inhibitor provides durable response in metastatic metaplastic carcinoma of the breast: A hidden gem in the BELLE-4 study. (Pubmed Central) - Feb 16, 2020
P2/3
Buparlisib plus weekly paclitaxel might be a new treatment option for patients with metastatic MCB harboring a PIK3CA mutation. Additional prospective studies for investigating the efficacy of the proposed combination are warranted.
- | Journal: Insight into the Selective Mechanism of PI3Kγ with Benzothiazole and Thiazolopiperidine γ-specific Inhibitors by in Silico Approaches. (Pubmed Central) - Feb 16, 2020
Finally, through the MM/GBSA binding free energy decomposition, residue-inhibitor interactions spectra were obtained and several key residues contributing to favorable binding were highlighted, which provides valuable information for rational PI3K? inhibitor design and modification.
- | quercetin (LY294002) / Eli Lilly
Journal: PI3K/Akt Signaling Pathway may be involved in MCP-1-induced P2X4R Expression in cultured microglia and Cancer-induced Bone Pain Rats. (Pubmed Central) - Feb 16, 2020
Besides, PI3K inhibitor LY 294002 could attenuate MCP-1-induced P2X4R expression in cultured microglia...Moreover, RS-504393 also reduced the increase of p-Akt induced by CIBP. Inhibition of PI3K/Akt pathway may partly reduce MCP-1/CCR2-induced expression of P2X4R and mechanical allodynia in CIBP rats.
- | MK-2206 / Merck (MSD), quercetin (LY294002) / Eli Lilly, dactolisib (RTB101) / Novartis, PureTech
Journal: Deoxyshikonin isolated from Arnebia euchroma inhibits colorectal cancer by down-regulating the PI3K/Akt/mTOR pathway. (Pubmed Central) - Feb 16, 2020
In vivo study, the weight of tumour tissues at deoxyshikonin groups was significantly reduced compared with the control group, and PI3K, p-PI3K, Akt, p-Akt308 and mTOR expression was decreased. Discussion and We can conclude that deoxyshikonin isolated from Arnebia euchroma inhibited CRC through the PI3K/Akt/mTOR pathway.
- | Journal, IO Biomarker: Diacetyl Hexamethylene Diamine (CAHB) Exerts Pro-Apoptotic and Anti-Proliferative Function in Leukemic T Lymphocytes via Downregulating PI3K/Akt Signaling. (Pubmed Central) - Feb 15, 2020
RESULTS CAHB inhibited the proliferation and promoted the apoptosis of Jurkat cells in a time- and dose-dependent manner by decreasing activation of Akt, reducing the mitochondrial membrane potential, and downregulating the Bcl-2/Bax ratio. CONCLUSIONS Our data suggest that CAHB might be regarded as a novel treatment agent for T-ALL since it can induce apoptosis and inhibit proliferation of the T-ALL cell line at a relatively low level.
- | quercetin (LY294002) / Eli Lilly
Journal: Apigenin Protects Against Renal Tubular Epithelial Cell Injury and Oxidative Stress by High Glucose via Regulation of NF-E2-Related Factor 2 (Nrf2) Pathway. (Pubmed Central) - Feb 15, 2020
LY294002 also attenuated the increase in Nrf2 protein by apigenin in high glucose-treated HK-2 cells. CONCLUSIONS Apigenin protects renal tubular epithelial cells against high glucose-induced injury through suppression of oxidative stress and inflammation via activation of the Nrf2 pathway.
- | gefitinib / Generic mfg.
Journal: An effective drug sensitizing agent increases gefitinib treatment by down regulating PI3K/Akt/mTOR pathway and up regulating autophagy in non-small cell lung cancer. (Pubmed Central) - Feb 15, 2020
Our results indicated that when associating with gefitinib in a dose-dependent fashion, CKI demonstrated the ability to inhibit the proliferation and to increase the sensitivity to gefitinib treatment in gefitinib less sensitive cell lines. This could be the results of down regulation of the PI3K/Akt/mTOR pathway and up regulation of autophagy, which were identified as the potential primary targets of CKI to increase gefitinib treatment effect.
- | Preclinical, Journal, IO Biomarker: Parthenolide Inhibits the Proliferation of MDA-T32 Papillary Thyroid Carcinoma Cells in Vitro and in Mouse Tumor Xenografts and Activates Autophagy and Apoptosis by Downregulation of the Mammalian Target of Rapamycin (mTOR)/PI3K/AKT Signaling Pathway. (Pubmed Central) - Feb 15, 2020
Parthenolide induced increased expression of the autophagocytic proteins, LC3-II and beclin-1, had a dose-dependent inhibitory effect on the mTOR/PI3K/AKT cascade in MDA-T32 cells and inhibited the growth of the mouse xenograft tumors in vivo. CONCLUSIONS Parthenolide inhibited the growth and migration of MDA-T32 human papillary thyroid carcinoma cells in vitro and mouse tumor xenografts and activated autophagy and apoptosis by downregulation of the mTOR/PI3K/AKT signaling pathway.
- | Journal, IO Biomarker: LaSota Strain Expressing The Rabies Virus Glycoprotein (rL-RVG) Suppresses Gastric Cancer by Inhibiting the Alpha 7 Nicotinic Acetylcholine Receptor (α7 nAChR)/Phosphoinositide 3-Kinase (PI3K)/AKT Pathway. (Pubmed Central) - Feb 15, 2020
Compared with the NDV group, the results of light microscopy, FCM, and TUNEL assay showed that alpha7-nAChR antagonist significantly affected the apoptosis of gastric cancer cells in the rL-RVG group. CONCLUSIONS rL-RVG leads to much greater apoptosis through the alpha7-nAChR/PI3K/AKT pathway.
- | tacrolimus / Generic mfg.
Preclinical, Journal: The PI3Kδ selective inhibitor AS2541019 suppresses donor-specific antibody production in rat cardiac and non-human primate renal allotransplant models. (Pubmed Central) - Feb 15, 2020
In cynomolgus monkey renal allotransplant model, concomitant administration of AS2541019 with tacrolimus and MMF significantly inhibited de novo DSA production. Together, our findings indicate that the PI3Kδ selective inhibitor AS2541019 is a potential candidate for preventing AMR development by inhibiting DSA production.
- | quercetin (LY294002) / Eli Lilly, PD98059 / Wayne State University, SP600125 / BMS
Journal: Naringenin-induced HO-1 ameliorates high glucose or free fatty acids-associated apoptosis via PI3K and JNK/Nrf2 pathways in human umbilical vein endothelial cells. (Pubmed Central) - Feb 15, 2020
Finally, pretreatment of HUVECs with NG remarkably reduced HG- or FFA-induced cell apoptosis, and this effect was greatly abrogated in the presence of SnPP (an HO-1 inhibitor). Above all, our data show that NG increased HO-1 expression and reduced HG- or FFA-induced cell apoptosis in HUVECs by upregulating PI3K, JNK, and Nrf2 pathways, which may confer an adaptive survival response in diabetes-induced vascular injury.
- | Journal: Naringin mitigates myocardial strain and the inflammatory response in sepsis-induced myocardial dysfunction through regulation of PI3K/AKT/NF-κB pathway. (Pubmed Central) - Feb 15, 2020
Finally, Nar also inhibited NF-κB nuclear translocation and the activity of iNOS in H9c2 cardiomyocytes by activating PI3K/AKT signaling pathway. These results suggest that naringin may possess novel therapeutic potential for protection against LPS-induced myocardial dysfunction.
- | Journal: DMBT1 suppresses progression of gallbladder carcinoma through PI3K/AKT signaling pathway by targeting PTEN. (Pubmed Central) - Feb 15, 2020
Further study of underlying mechanisms demonstrated that DMBT1 combined with PTEN which could stabilize PTEN protein, resulting in inhibiting the activation of PI3K/AKT signaling pathway. Our study revealed a new sight of DMBT1 as a tumor-suppressor gene on the PI3K/AKT pathway in GBC, which may be a potential therapeutic target for improving treatment.
- | Journal: Ginkgolide K supports remyelination via induction of astrocytic IGF/PI3K/Nrf2 axis. (Pubmed Central) - Feb 15, 2020
Further findings suggest that IGF/PI3K, but not BDNF, was induced in the corpus callosum after GK treatment, revealing that Nrf2 activation inhibited caspase-3 and apoptosis in O4+ oligodendrocytes possibly through IGF/PI3K signaling molecules. Since the current immunomodulatory therapies for MS have failed to prevent patients from entering the progressive phase of the disease, thus targeting Nrf2 in astrocytes with GK would be an ideal strategy for myelin protection and regeneration.
- | rocilinostat (ACY-1215) / Regenacy, BMS
Journal: Ricolinostat (ACY-1215) inhibits VEGF expression via PI3K/AKT pathway and promotes apoptosis in osteoarthritic osteoblasts. (Pubmed Central) - Feb 15, 2020
These data of immunohistochemistry and micro-CT from OA model mice also demonstrated the weak staining of MMPs in cartilage and prevention of aberrant subchondral bone formation after ACY-1215 injection. Therefore, high expression of HDAC6 in osteoblasts also contributed to the OA progression, and our study provided a new evidence that HDAC6 inhibitor may be a potential therapeutic drug for OA.
- | Preclinical, Journal: Comparing the Protection Imparted by Different Fraction Extracts of Garlic (Allium sativum L.) against Der p-Induced Allergic Airway Inflammation in Mice. (Pubmed Central) - Feb 15, 2020
The water fraction also inhibited the PI3K/Akt/NF-κB signal pathways in A549 cells. These findings suggest that water fraction extracts of garlic have a clear anti-inflammatory effect on Der p-induced allergic asthma.
- | Journal: Genistein potentiates Centchroman induced antineoplasticity in breast cancer via PI3K/Akt deactivation and ROS dependent induction of apoptosis. (Pubmed Central) - Feb 15, 2020
These findings suggest that water fraction extracts of garlic have a clear anti-inflammatory effect on Der p-induced allergic asthma. Together, these studies suggest that GN represents a potential adjunct molecule whose role in CC induced apoptosis deserves attention.
- | progesterone / Generic mfg.
Journal: miR-431 regulates granulosa cell function through the IRS2/PI3K/AKT signaling pathway. (Pubmed Central) - Feb 15, 2020
Further, luciferase reporter assay demonstrated that IRS2 was a direct target of miR-431. In conclusion, this study demonstrated that miR-431 regulates granulosa cell function through the IRS2/PI3K/AKT signaling pathway.
- | Journal: MicroRNA-21 and microRNA-155 promote the progression of Burkitt's lymphoma by the PI3K/AKT signaling pathway. (Pubmed Central) - Feb 15, 2020
miR-21 and miR-155 promote the progression of Burkitt's lymphoma through PI3K/AKT signaling by targeting C1RL and TCAP. Our findings will provide a novel biomarker and therapeutic strategies for Burkitt's lymphoma.
- | quercetin (LY294002) / Eli Lilly
Preclinical, Journal, IO Biomarker: Echinocystic acid provides a neuroprotective effect via the PI3K/AKT pathway in intracerebral haemorrhage mice. (Pubmed Central) - Feb 15, 2020
EA may provide neuroprotection via activation of the PI3K/AKT pathway. Given the safety of EA has been proven, further studies are required to investigate whether EA is a potential agent for the treatment of ICH.
- Xalkori (crizotinib) / Pfizer
Exosome-Transmitted lncARSR Promotes Crizotinib Resistance in Lung Carcinoma by regulating PI3K/Akt/mTOR signaling pathway (Hall 1) - Feb 15, 2020 - Abstract #ELCC2020ELCC_271;
- | Journal: A high-avidity biosensor reveals plasma membrane PI(3,4)P is predominantly a class I PI3K signaling product. (Pubmed Central) - Feb 14, 2020
We show that despite clear evidence for class II PI3K in PI(3,4)P-driven function, the overwhelming majority of the lipid accumulates through degradation of class I PI3K-produced PIP However, we show that PI(3,4)P is also subject to hydrolysis by the tumor suppressor lipid phosphatase PTEN. Collectively, our results show that PI(3,4)P is potentially an important driver of class I PI3K-driven signaling and provides powerful new tools to begin to resolve the biological functions of this lipid downstream of class I and II PI3K.
- | Journal: TCF21 inhibits tumor-associated angiogenesis and suppresses the growth of cholangiocarcinoma by targeting PI3K/Akt and ERK signaling. (Pubmed Central) - Feb 14, 2020
Collectively, our results show that PI(3,4)P is potentially an important driver of class I PI3K-driven signaling and provides powerful new tools to begin to resolve the biological functions of this lipid downstream of class I and II PI3K. TCF21 presents anti-angiogenic activities and thus, elevating TCF21 expression may provide therapeutic benefits for CCA.
- | Alinia (nitazoxanide) / Lupin, Romark Lab
Preclinical, Journal: Nitazoxanide, an anti-parasitic drug, efficiently ameliorates learning and memory impairments in AD model mice. (Pubmed Central) - Feb 14, 2020
Furthermore, NTZ administration decreased Aβ level and senile plaque formation in the hippocampus and cerebral cortex of APP/PS1 transgenic mice, and improved learning and memory impairments in Morris water maze assay. In conclusion, our results highlight the potential of NTZ in the treatment of AD.
- | Preclinical, Journal: 3-Deoxyglucosone interferes with insulin signaling and attenuates insulin action on glucose-induced GLP-1 secretion in the enteroendocrine L cell line STC-1. (Pubmed Central) - Feb 14, 2020
3DG-mediated reduction in GLUT2 expression contributes to the attenuation of insulin-induced GLP-1 secretion under high-glucose conditions in part through the insulin-PI3K/Akt/GLUT2 pathway in STC-1 cells. We conclude that 3DG interferes with insulin signaling and attenuates insulin action on glucose-induced GLP-1 secretion in STC-1 cells.
- | selegiline / Generic mfg.
Preclinical, Journal: Possible involvement of PI3K/AKT/mTOR signaling pathway in the protective effect of selegiline (deprenyl) against memory impairment following ischemia reperfusion in rat. (Pubmed Central) - Feb 14, 2020
Findings showed that selegiline increased the level and expression of PI3K, AKT and mTOR as well as decreased the proportion of dark neurons in the CA1 area of the pyramidal layer of the hippocampus. We concluded that selegiline, partially at least, through increases the expression of PI3K, AKT and mTOR as well as decreases the percent of dark neurons in the hippocampus could improve the memory impairment following the ischemia in rats.
- | dactolisib (RTB101) / Novartis, PureTech
Journal: Targeting the phosphoinositide 3-kinase/AKT pathways by small molecules and natural compounds as a therapeutic approach for breast cancer cells. (Pubmed Central) - Feb 14, 2020
In addition, TWIST-1 mRNA expression was down regulated in samples treated with both NVP-BEZ235 and CAPE. These altogether signified that NVP-BEZ235 in combination with CAPE showed improved therapeutic efficacy in breast cancer cells by decreasing apoptotic resistance and reduction of CXCR4 and TWIST-1 expression at mRNA level could be one of mechanism of action.
- || Avastin (bevacizumab) / Roche, buparlisib (BKM120) / Novartis, Adlai Nortye
Clinical, P1/2 data, P2 data, Journal: Phase I/II study of bevacizumab with BKM120, an oral PI3K inhibitor, in patients with refractory solid tumors (phase I) and relapsed/refractory glioblastoma (phase II). (Pubmed Central) - Feb 14, 2020
This regimen was poorly tolerated, despite the low daily dose of BKM120. Further development of this combination for the treatment of glioblastoma is not recommended.