Phase 1/1b dose escalation and expansion study of BEZ235, a dual PI3K/mTOR inhibitor, in patients with advanced solid tumors including patients with advanced breast cancer
Sign Up to like & getrecommendations! Published in 2018 at "Cancer Chemotherapy and Pharmacology"
DOI: 10.1007/s00280-018-3610-z
Abstract: PurposeTo determine the maximum tolerated dose (MTD) of BEZ235, an oral inhibitor of class I PI3K and mTOR complexes 1 and 2.MethodsWe performed a phase I/Ib, multicenter, open-label study of oral BEZ235 administered in a… read more here.
Keywords: pi3k mtor; dose escalation; bez235; study ... See more keywords
The dual specificity PI3K/mTOR inhibitor PKI-587 displays efficacy against T-cell acute lymphoblastic leukemia (T-ALL).
Sign Up to like & getrecommendations! Published in 2017 at "Cancer letters"
DOI: 10.1016/j.canlet.2017.01.035
Abstract: Although significant improvements have been made in the treatment of acute lymphoblastic leukemia (ALL), there is a substantial subset of high-risk T-cell ALL (T-ALL) patients with relatively poor prognosis. Like in other leukemia types, alterations… read more here.
Keywords: mtor pathway; pi3k mtor; inhibitor; pki 587 ... See more keywords
Leflunomide-induced liver injury in mice: Involvement of TLR4 mediated activation of PI3K/mTOR/NFκB pathway.
Sign Up to like & getrecommendations! Published in 2019 at "Life sciences"
DOI: 10.1016/j.lfs.2019.116824
Abstract: AIMS Leflunomide is a disease modifying anti-rheumatic drug (DMARD) beneficial in refractory cases of rheumatoid arthritis. Since leflunomide approval, hepatotoxicity and instructions of liver function monitoring have been recommended. The current work aimed to explore… read more here.
Keywords: tlr4; pi3k mtor; leflunomide induced; mice ... See more keywords
Stearic Acid Activates the PI3K-mTOR-4EBP1/S6K and mTOR-SREBP-1 Signaling Axes through FATP4-CDK1 To Promote Milk Synthesis in Primary Bovine Mammary Epithelial Cells.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of agricultural and food chemistry"
DOI: 10.1021/acs.jafc.2c00208
Abstract: Stearic acid (SA), an 18-carbon long-chain saturated fatty acid, has great potential for promoting lactation. Therefore, this study investigates the effects and mechanism of SA on milk synthesis in primary bovine mammary epithelial cells (BMECs).… read more here.
Keywords: mtor 4ebp1; mtor; milk synthesis; pi3k mtor ... See more keywords
Discovery of 2-Methyl-2-(4-(2-methyl-8-(1H-pyrrolo[2,3-b]pyridin-6-yl)-1H-naphtho[1,2-d]imidazol-1-yl)phenyl)propanenitrile as a Novel PI3K/mTOR Inhibitor with Enhanced Antitumor Efficacy In Vitro and In Vivo.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00572
Abstract: PI3K/Akt/mTOR signaling pathway is a validated drug target for cancer treatment that plays a critical role in controlling tumor growth, proliferation, and apoptosis. However, no FDA-approved PI3K/mTOR dual inhibitor exists. Thus, a candidate with a… read more here.
Keywords: inhibitor; pi3k mtor; antitumor efficacy; mtor ... See more keywords
Regulatory role of hippocampal PI3K and mTOR signaling pathway in NMDA-induced infant spasm rats
Sign Up to like & getrecommendations! Published in 2019 at "Neurological Research"
DOI: 10.1080/01616412.2019.1672412
Abstract: ABSTRACT Objectives: To explore the role of mTOR signaling pathway in modulating epileptogenesis in an N-methyl-D-aspartic acid (NMDA)-induced infant spasm (IS) rat model. Methods: After inducing IS successfully, the phosphorylation status of PI3K, Akt, mTOR… read more here.
Keywords: pi3k; pi3k mtor; nmda induced; mtor signaling ... See more keywords
Epithelial cells expressed IL-33 to promote degranulation of mast cells through inhibition on ST2/PI3K/mTOR-mediated autophagy in allergic rhinitis
Sign Up to like & getrecommendations! Published in 2020 at "Cell Cycle"
DOI: 10.1080/15384101.2020.1749402
Abstract: ABSTRACT Nasal epithelial cells are the first barrier against allergen infiltration in allergic rhinitis (AR), and the relationship between nasal epithelial cells and mast cell-mediated hypersensitivity remains unclear. This study aimed to investigate the possible… read more here.
Keywords: mast cells; degranulation; epithelial cells; pi3k mtor ... See more keywords
ACTR-51. PHASE 2 STUDY TO EVALUATE THE SAFETY, PHARMACOKINETICS AND CLINICAL ACTIVITY OF PI3K/MTOR INHIBITOR GDC-0084 GIVEN TO GLIOBLASTOMA (GBM) PATIENTS WITH UNMETHYLATED O6-METHYLGUANINE-METHYLTRANSFERASE PROMOTER STATUS
Sign Up to like & getrecommendations! Published in 2018 at "Neuro-Oncology"
DOI: 10.1093/neuonc/noy148.083
Abstract: BACKGROUND GDC-0084 is a potent, oral, selective small molecule inhibitor of class I phosphoinositide 3-kinase and mammalian target of rapamycin (PI3K/mTOR) efficacious in GBM models driven by activation of the PI3K pathway. GDC-0084 crosses the… read more here.
Keywords: pi3k mtor; pi3k; inhibitor; phase study ... See more keywords
ACTR-64. PHASE 2 STUDY TO EVALUATE THE SAFETY, PHARMACOKINETICS AND CLINICAL ACTIVITY OF PI3K/mTOR INHIBITOR GDC-0084 IN GBM PATIENTS WITH UNMETHYLATED O6-METHYLGUANINE-METHYLTRANSFERASE (MGMT) PROMOTER STATUS
Sign Up to like & getrecommendations! Published in 2019 at "Neuro-Oncology"
DOI: 10.1093/neuonc/noz175.106
Abstract: GDC-0084 is a potent, oral, selective small molecule inhibitor of class I phosphoinositide 3-kinase and mammalian target of rapamycin (PI3K/mTOR). GDC-0084 crosses the blood-brain barrier and achieves a brain / plasma ratio of approximately 1.0.… read more here.
Keywords: pi3k mtor; phase; inhibitor; part ... See more keywords
A proteomics approach to identifying novel protein targets involved in erinacine A–mediated inhibition of colorectal cancer cells’ aggressiveness
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Cellular and Molecular Medicine"
DOI: 10.1111/jcmm.13004
Abstract: Erinacine A, a major active component of a diterpenoid derivative isolated from Hericium erinaceus mycelium, has been demonstrated to exert anticancer effects. Herein, we present an investigation of the molecular mechanism of erinacine A induction… read more here.
Keywords: pi3k mtor; novel protein; erinacine; cancer cells ... See more keywords
A First-in-Human Phase 1 Study of LY3023414, an Oral PI3K/mTOR Dual Inhibitor, in Patients with Advanced Cancer
Sign Up to like & getrecommendations! Published in 2018 at "Clinical Cancer Research"
DOI: 10.1158/1078-0432.ccr-17-3421
Abstract: Purpose: The PI3K/mTOR pathway is frequently aberrated in cancer. LY3023414 is a potent and selective ATP-competitive inhibitor of class I PI3K isoforms, mTOR, and DNA-PK. Here we report the dose-escalation results of the first-in-human phase… read more here.
Keywords: pi3k mtor; phase; inhibitor; twice daily ... See more keywords