HS-173, a selective PI3K inhibitor, induces cell death in head and neck squamous cell carcinoma cell lines
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DOI: 10.1007/s00508-020-01729-3
Abstract: Background The selective PI3K (Phosphatidylinositol 3-kinase) inhibitor HS-173 has anticancer activity in non-small cell lung cancer and pancreatic cancer cells. Of all head and neck squamous cell carcinomas (HNSCC) 20% harbor specific mutations in the… read more here.
Keywords: inhibitor; selective pi3k; cell lines; effect ... See more keywords
Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.111718
Abstract: Phosphatidylinositol-3 kinase (PI3K) pathway is one of the most frequently activated pathogenic signaling cascades in human malignancies. PI3K is genetically mutated or overexpressed in a wide variety of cancers including ovarian, breast, prostate, gastric, colorectal,… read more here.
Keywords: pi3k; kinase pi3k; selective pi3k; phosphatidylinositol kinase ... See more keywords
Discovery of Potent and Selective PI3Kγ Inhibitors.
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DOI: 10.1021/acs.jmedchem.0c01203
Abstract: The selective inhibition of the lipid signaling enzyme PI3Kγ constitutes an opportunity to mediate immunosuppression and inflammation within the tumor microenvironment but is difficult to achieve due to the high sequence homology across the class… read more here.
Keywords: pi3k; potent selective; discovery potent; selective pi3k ... See more keywords
Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma.
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DOI: 10.1021/acs.jmedchem.1c01520
Abstract: PI3Kδ inhibitors have been developed for treatment of B-cell malignancies and inflammatory and autoimmune diseases. However, their therapeutic role in solid tumors like hepatocellular carcinoma (HCC) is rarely reported. Thus, the development of potent and… read more here.
Keywords: pi3k; hepatocellular carcinoma; pi3k inhibitors; selective pi3k ... See more keywords
Structural basis for tailor-made selective PI3K α/β inhibitors: a computational perspective
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DOI: 10.1039/d0nj04216a
Abstract: PI3K α and β are Class IA PI3K isoforms that share a highly homologous ATP binding site, differing only in a few residues around the binding site. They are ubiquitously expressed in various organs and… read more here.
Keywords: structural basis; pi3k; selective pi3k; basis tailor ... See more keywords