Journal of Enzyme Inhibition and Medicinal Chemistry, 2023 Phosphoinositide 3-kinases (PI3K) and phosphoinositide 3-kinase-related protein kinases (PIKK) are two structurally related families of kinases that play vital roles in cell growth and DNA damage repair.
Xueqin Huang +11 more
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Phosphoinositide 3-kinase inhibitors induce DNA damage through nucleoside depletion [PDF]
Proceedings of the National Academy of Sciences of the United States of America, 2016 Significance Mutations in the PI3K pathway are highly prevalent in cancers, and isoform-specific and pan-PI3K inhibitors have entered clinical trials in both solid and hematologic malignancies. The PI3K δ-specific inhibitor idelalisib (in combination with rituximab) was recently approved for the treatment of chronic lymphocytic leukemia ...
Ashish Juvekar +2 more
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Phosphoinositide 3-kinase inhibitors in lymphoma. [PDF]
Curr Opin Oncol, 2014 Purpose of review The phosphoinositide 3-kinase (PI3K) pathway, with downstream targets including Akt and mammalian target of rapamycin, has been implicated in numerous human cancers, including hematologic malignancies and lymphomas.
Curran E, Smith SM.
europepmc +5 more sources
Development of Phosphoinositide-3 Kinase Pathway Inhibitors for Advanced Cancer [PDF]
Current Oncology Reports, 2010 The phosphoinositide-3 kinase (PI3K) pathway plays a critical role in cancer cell growth and survival. PI3K is activated in human cancers by elevated receptor tyrosine kinase activity, RAS mutation, as well as by mutation, amplification, and deletion of ...
James M Cleary +2 more
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Analysis of phosphoinositide 3-kinase inhibitors by bottom-up electron-transfer dissociation hydrogen/deuterium exchange mass spectrometry. [PDF]
Biochem J, 2017 Until recently, one of the major limitations of hydrogen/deuterium exchange mass spectrometry (HDX-MS) was the peptide-level resolution afforded by proteolytic digestion.
Masson GR, Maslen SL, Williams RL.
europepmc +2 more sources
Therapeutic potential of phosphoinositide 3-kinase inhibitors. [PDF]
Chemistry & Biology, 2003 At least one Holy Grail for many academic researchers and pharmaceutical research divisions alike has been to identify therapeutically useful selective PI3K inhibitors. There are several different but closely related PI3Ks which are thought to have distinct biological roles.
S. Ward +4 more
semanticscholar +3 more sources
Phosphoinositide 3-Kinase Inhibitor-Induced Hyperglycemia
Journal of the Endocrine Society, 2021 Background: Phosphoinositide 3-kinase inhibitors (PI3Ki) are a new class of medications used to treat HR positive, HER2 negative, PIK3CA mutated advanced or metastatic breast cancer.
S. Shey +3 more
semanticscholar +2 more sources
Selective phosphoinositide 3-kinase inhibitors and implication in diabetic retinopathy as pharmacological tools [PDF]
Frontiers in PharmacologyPhosphoinositide 3-kinases (PI3Ks) are ubiquitous enzymes, that regulate different cellular functions, most involved in pathogenesis and progression of several oncological diseases.
Carmela Bonaccorso +10 more
doaj +2 more sources
Identification of Novel Thiazolo[5,4-b]Pyridine Derivatives as Potent Phosphoinositide 3-Kinase Inhibitors [PDF]
Molecules, 2020 A series of novel 2-pyridyl, 4-morpholinyl substituted thiazolo[5,4-b]pyridine analogues have been designed and synthesized in this paper. These thiazolo[5,4-b]pyridines were efficiently prepared in seven steps from commercially available substances in ...
Liang Xia +7 more
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Phosphoinositide 3-kinase (PI3K) pathway inhibitors in solid tumors: From laboratory to patients
Cancer Treatment Reviews, 2017 The phosphoinositide 3-kinase (PI3K) pathway is an intracellular signaling pathway that has regulatory roles in cell survival, proliferation, and differentiation, and a critical role in tumorigenesis.
Filip Janku
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