Phosphoinositide 3-kinase in Health and Disease
Volume 2
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Article
PI3K and cancer: lessons, challenges and opportunities
Mutations that activate the phosphoinositide 3-kinase (PI3K) signalling network are nearly ubiquitous in human cancer.
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Article
Investigational drug MLN0128, a novel TORC1/2 inhibitor, demonstrates potent oral antitumor activity in human breast cancer xenograft models
Aberrant activation of the mammalian target of rapamycin (mTOR) signaling plays an important role in breast cancer progression and represents a potential therapeutic target for breast cancer. In this study, we...
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The translational landscape of mTOR signalling steers cancer initiation and metastasis
The mammalian target of rapamycin (mTOR) kinase is a master regulator of protein synthesis that couples nutrient sensing to cell growth and cancer. However, the downstream translationally regulated nodes of ge...
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Next-generation flow cytometry
Mass cytometry dramatically enhances the dimensionality of fluorescence-based flow cytometry for phenotypic analysis of heterogeneous cell populations.
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Book
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Book
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Chapter
PI3K: From the Bench to the Clinic and Back
From humble beginnings over 25 years ago as a lipid kinase activity associated with certain oncoproteins, PI3K (phosphoinositide 3-kinase) has been catapulted to the forefront of drug development in cancer, im...
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Chapter
Taking PI3Kδ and PI3Kγ One Step Ahead: Dual Active PI3Kδ/γ Inhibitors for the Treatment of Immune-Mediated Inflammatory Diseases
The multiple roles of PI3Kδ (p110δ) and PI3Kγ (p110γ) in various immune cells have encouraged the development of small-molecule inhibitors of both PI3K isoforms, alone or in combination, for the treatment of i...
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Article
Correction: Corrigendum: The p110δ structure: mechanisms for selectivity and potency of new PI(3)K inhibitors
Nat. Chem. Biol. 6, 117–124 (2010); published online 10 January 2010; corrected after print 12 February 2010 and 2 March 2010 In the version of this article initially published, the structure of p110δ in compl...
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Article
Correction: Corrigendum: The p110δ structure: mechanisms for selectivity and potency of new PI(3)K inhibitors
Nat. Chem. Biol. 6, 117–124 (2010); published online 10 January 2010; corrected after print 12 February 2010 In the version of this article initially published, **da Ren was inadvertently left off the author...
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Article
Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor
The protein kinase mTOR is known to contribute to cancer development. However, existing drugs targeting mTOR, such as rapamycin, have not been very effective at inhibiting cancer cell survival and also have th...
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Article
The p110δ structure: mechanisms for selectivity and potency of new PI(3)K inhibitors
Upregulation of PI(3)K signaling pathways is implicated in many diseases, and a number of inhibitors are currently in clinical development. The structure of a PI(3)Kδ kinase domain, along with co-complexes wit...
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Article
Targeting dual-specificity phosphatases: manipulating MAP kinase signalling and immune responses
Dual-specificity phosphatases (DUSPs) are a subclass of protein tyrosine phosphatases (PTPs) that specifically interact with and regulate mitogen-activated pro...
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PI3Kδ and PI3Kγ: partners in crime in inflammation in rheumatoid arthritis and beyond?
Phosphoinositide 3-kinases (PI3Ks) generate lipid-based second messengers that control an array of intracellular signalling pathways that are responsible for m...
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Article
PI(3)Kγ has an important context-dependent role in neutrophil chemokinesis
The directional movement of cells in a gradient of external stimulus is termed chemotaxis and is important in many aspects of development and differentiated cell function. Phophoinositide 3-kinases (PI(3)Ks) a...
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Article
PI3Kγ inhibition: towards an 'aspirin of the 21st century'?
Phosphatidylinositol 3-kinases (PI3Ks) are lipid and protein kinases that are involved in numerous signalling pathways in various cellular contexts. The class ...
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Article
Decompartmentalizing target validation—thinking outside the pipeline boxes
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Article
Positive regulation of immune cell function and inflammatory responses by phosphatase PAC-1
Mitogen-activated protein kinases facilitate many cellular processes and are essential for immune cell function. Their activity is controlled by kinases and dual-specificity phosphatases. A comprehensive micro...
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Article
PI3Kγ inhibition blocks glomerulonephritis and extends lifespan in a mouse model of systemic lupus
Systemic lupus erythematosus (SLE) is a chronic inflammatory disease generated by deregulation of T cell–mediated B-cell activation, which results in glomerulonephritis and renal failure. Disease is treated wi...
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Article
Blockade of PI3Kγ suppresses joint inflammation and damage in mouse models of rheumatoid arthritis
Phosphoinositide 3-kinases (PI3K) have long been considered promising drug targets for the treatment of inflammatory and autoimmune disorders as well as cancer and cardiovascular diseases. But the lack of spec...
