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
doaj +4 more sources
Phosphoinositide 3-kinase inhibitors in lymphoma. [PDF]
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. The development and refinement of PI3K inhibitors directed toward this pathway show promising clinical efficacy.
Curran E, Smith SM.
europepmc +5 more sources
Phosphoinositide 3-kinase inhibitors induce DNA damage through nucleoside depletion. [PDF]
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 ...
Juvekar A +15 more
europepmc +5 more sources
Analysis of phosphoinositide 3-kinase inhibitors by bottom-up electron-transfer dissociation hydrogen/deuterium exchange mass spectrometry. [PDF]
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]
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
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
Isoform-specific phosphoinositide 3-kinase inhibitors exert distinct effects in solid tumors. [PDF]
Abstract Therapeutic inhibitors are being developed against the phosphoinositide 3-kinase (PI3K) pathway, the deregulation of which drives tumor growth and survival in many cancers. There are eight PI3Ks in mammals divided into three classes.
K. Edgar +7 more
semanticscholar +3 more sources
Identification of Novel Thiazolo[5,4-b]Pyridine Derivatives as Potent Phosphoinositide 3-Kinase Inhibitors [PDF]
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
doaj +2 more sources
Effects of novel isoform-selective phosphoinositide 3-kinase inhibitors on natural killer cell function. [PDF]
Phosphoinositide 3-kinases (PI3Ks) are promising targets for therapeutic development in cancer. The class I PI3K isoform p110α has received considerable attention in oncology because the gene encoding p110α (PIK3CA) is frequently mutated in human cancer.
Sung Su Yea +6 more
doaj +2 more sources
Magic power of phosphoinositide 3-kinase inhibitors
Phosphoinositide 3-kinases (PI3K) play critical roles in the maintenance of cell biological functions and are suggested as a therapeutic target for drug discovery and development.
Xiangdong Wang
semanticscholar +2 more sources

