GSK1059615

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Company:

GSK

Drug class:

PI3K inhibitor

Related drugs:

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almost4years

Cotargeting CHK1 and PI3K Synergistically Suppresses Tumor Growth of Oral Cavity Squamous Cell Carcinoma in Patient-Derived Xenografts. (PubMed, Cancers (Basel))

The antitumor efficacy of CHK1 inhibitors (PF477736, AZD7762, LY2606368) and PI3K inhibitors (BYL719, GDC0941, GSK1059615) was investigated in OSCC cell lines and PDX models. Furthermore, compared with monotherapy, cotreatment with CHK1 and PI3K inhibitors exerted synergistic anticancer effects by suppressing CHK1, AKT, and 4E-BP1 phosphorylation. In summary, our study identified CHK1 and PI3K as promising targets, especially in a dual treatment strategy combining a CHK1 inhibitor with cisplatin or a PI3K inhibitor as a novel therapeutic approach for OSCC patients with aberrant cell cycle regulation and PI3K signaling activation.

almost 4 years ago

Clinical • Journal • PARP Biomarker

PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PIK3CD (Phosphatidylinositol-4 5-Bisphosphate 3-Kinase Catalytic Subunit Delta) • EIF4EBP1 (Eukaryotic translation initiation factor 4E binding protein 1)

cisplatin • Piqray (alpelisib) • prexasertib (ACR-368) • pictilisib (GDC-0941) • GSK1059615

almost4years

Glucose restriction reverses the Warburg effect and modulates PKM2 and mTOR expression in breast cancer cell lines. (PubMed, Cell Mol Biol (Noisy-le-grand))

GSK1059615 does not significantly modulate lactate secretion and glucose uptake in both cell lines. Glucose restriction contribute to the reduction of the Warburg effect through mTOR inhibition and regulation of PKM2 kinases.

almost 4 years ago

Journal

mTOR (Mechanistic target of rapamycin kinase)

GSK1059615