Identification of a Potent Phosphoinositide 3‐Kinase Pan Inhibitor Displaying a Strategic Carboxylic Acid Group and Development of Its Prodrugs
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DOI: 10.1002/cmdc.201700340
Abstract: Activation of the phosphoinositide 3‐kinase (PI3K) pathway is a key signaling event in cancer, inflammation, and other proliferative diseases. PI3K inhibitors are already approved for some specific clinical indications, but their systemic on‐target toxicity limits… read more here.
Keywords: inhibitor; kinase; phosphoinositide kinase; pan ... See more keywords
Targeting phosphoinositide‐3‐kinase pathway in biliary tract cancers: A remedial route?
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Cellular Physiology"
DOI: 10.1002/jcp.27673
Abstract: Biliary tract cancers (BTC) are aggressive tumours with a low survival rate. At the advent of the genomic era, various genetic mutations in cell signalling pathways have been incriminated in carcinogenesis. Genomic analysis studies have… read more here.
Keywords: biliary tract; phosphoinositide kinase; pathway btcs; tract cancers ... See more keywords
Upstream regulators of phosphoinositide 3‐kinase and their role in diseases
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DOI: 10.1002/jcp.28215
Abstract: Phosphoinositide 3‐kinase (PI3K), a crucial signaling molecule, is regulated by various upstream regulators. Traditionally, receptor tyrosine kinases and G protein‐coupled receptor are regarded as its principle upstream regulators; however, recent reports have indicated that spleen… read more here.
Keywords: kinase role; regulators phosphoinositide; upstream regulators; role diseases ... See more keywords
The lipid products of phosphoinositide 3-kinase isoforms in cancer and thrombosis
Sign Up to like & getrecommendations! Published in 2018 at "Cancer and Metastasis Reviews"
DOI: 10.1007/s10555-018-9735-z
Abstract: Our knowledge on the role of the different lipid messengers produced by phosphoinositide 3-kinases (PI3Ks) in normal and cancer cells as well as in platelets during arterial thrombosis has greatly expanded these last 15 years. PI3Ks… read more here.
Keywords: products phosphoinositide; lipid products; cancer thrombosis; phosphoinositide kinase ... See more keywords
Phosphoinositide 3-kinase pathways and autophagy require phosphatidylinositol phosphate kinases.
Sign Up to like & getrecommendations! Published in 2018 at "Advances in biological regulation"
DOI: 10.1016/j.jbior.2018.02.003
Abstract: Phosphatidylinositol phosphate kinases (PIPKs) generate a lipid messenger phosphatidylinositol 4,5-bisphosphate (PI4,5P2) that controls essentially all aspects of cellular functions. PI4,5P2 rapidly diffuses in the membrane of the lipid bilayer and does not greatly change in… read more here.
Keywords: phosphoinositide kinase; pi4 5p2; phosphatidylinositol phosphate; phosphate kinases ... See more keywords
In vitro and in vivo anti-malignant melanoma activity of Alocasia cucullata via modulation of the phosphatase and tensin homolog/phosphoinositide 3-kinase/AKT pathway.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of ethnopharmacology"
DOI: 10.1016/j.jep.2017.11.025
Abstract: Alocasia cucullata, a Chinese herb, has been used as an anticancer treatment in southern China. Phosphatase and tensin (PTEN), is a tumor suppressor gene and the loss of PTEN expression may activate the phosphoinositide-3-kinase (PI3K)/AKT… read more here.
Keywords: melanoma; phosphatase tensin; alocasia cucullata; vitro vivo ... See more keywords
Deficiency of γδT cells protects against abdominal aortic aneurysms by regulating phosphoinositide 3-kinase/AKT signaling.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of vascular surgery"
DOI: 10.1016/j.jvs.2016.03.474
Abstract: OBJECTIVE It is known that T lymphocytes are activated in human abdominal aortic aneurysms (AAAs). γδT cells, as a subset of T cells, play a role in many inflammation-related diseases. However, whether γδT cells participate in… read more here.
Keywords: akt signaling; aortic aneurysms; phosphoinositide kinase; kinase akt ... See more keywords
Discovery of Novel Phosphoinositide-3-Kinase α Inhibitors with High Selectivity, Excellent Bioavailability, and Long-Acting Efficacy for Gastric Cancer.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00549
Abstract: Phosphoinositide-3-kinase (PI3K) overexpressed in many tumors is a promising target for cancer therapy. However, due to toxicity from the ubiquitous expression of PI3K in many tissues, the development of PI3K inhibitors with high selectivity and… read more here.
Keywords: pi3k; inhibitors high; high selectivity; cancer ... See more keywords
C-SH2 point mutation converts p85β regulatory subunit of phosphoinositide 3-kinase to an anti-aging gene
Sign Up to like & getrecommendations! Published in 2019 at "Scientific Reports"
DOI: 10.1038/s41598-019-48157-6
Abstract: Insulin interacts with the insulin receptor, and the activated receptor promotes activity of the phosphoinositide-3 kinase (PI3K) enzyme. A decrease in insulin or insulin-like growth factor 1 (IGF-1) signaling increases the lifespan in mammalian species.… read more here.
Keywords: point mutation; p85 regulatory; phosphoinositide kinase; gene ... See more keywords
Phosphoinositide 3-kinase δ (PI3Kδ) in respiratory disease.
Sign Up to like & getrecommendations! Published in 2018 at "Biochemical Society transactions"
DOI: 10.1042/bst20170467
Abstract: Defining features of chronic airway diseases include abnormal and persistent inflammatory processes, impaired airway epithelial integrity and function, and increased susceptibility to recurrent respiratory infections. Phosphoinositide 3-kinases (PI3K) are lipid kinases, which contribute to multiple… read more here.
Keywords: pi3k; kinase pi3k; respiratory disease; pi3k respiratory ... See more keywords
Introduction of pyrrolidineoxy or piperidineamino group at the 4-position of quinazoline leading to novel quinazoline-based phosphoinositide 3-kinase delta (PI3Kδ) inhibitors
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2018.1444608
Abstract: Abstract Phosphoinositide 3-kinase Delta (PI3Kδ) plays a key role in B-cell signal transduction and inhibition of PI3Kδ was confirmed to have clinical benefit in certain types of activation of B-cell malignancies. Herein, we reported a… read more here.
Keywords: quinazoline; kinase delta; pi3k; pyrrolidineoxy piperidineamino ... See more keywords