PI3K inhibitors are finally coming of age

B Vanhaesebroeck, MWD Perry, JR Brown… - Nature reviews Drug …, 2021 - nature.com
Abstract Overactive phosphoinositide 3-kinase (PI3K) in cancer and immune dysregulation
has spurred extensive efforts to develop therapeutic PI3K inhibitors. Although progress has …

Role of PI3K/AKT pathway in cancer: the framework of malignant behavior

N Jiang, Q Dai, X Su, J Fu, X Feng, J Peng - Molecular biology reports, 2020 - Springer
Given that the PI3K/AKT pathway has manifested its compelling influence on multiple
cellular process, we further review the roles of hyperactivation of PI3K/AKT pathway in …

Proliferation, survival and metabolism: the role of PI3K/AKT/mTOR signalling in pluripotency and cell fate determination

JSL Yu, W Cui - Development, 2016 - journals.biologists.com
Phosphatidylinositide 3 kinases (PI3Ks) and their downstream mediators AKT and
mammalian target of rapamycin (mTOR) constitute the core components of the …

PI3K in cancer: divergent roles of isoforms, modes of activation and therapeutic targeting

LM Thorpe, H Yuzugullu, JJ Zhao - Nature Reviews Cancer, 2015 - nature.com
Abstract Phosphatidylinositol 3-kinases (PI3Ks) are crucial coordinators of intracellular
signalling in response to extracellular stimuli. Hyperactivation of PI3K signalling cascades is …

[HTML][HTML] PI3K signalling in inflammation

PT Hawkins, LR Stephens - … et Biophysica Acta (BBA)-Molecular and Cell …, 2015 - Elsevier
PI3Ks regulate several key events in the inflammatory response to damage and infection.
There are four Class I PI3K isoforms (PI3Kα, β, γ, δ), three Class II PI3K isoforms (PI3KC2α …

Activity of the PI3K-δ, γ inhibitor duvelisib in a phase 1 trial and preclinical models of T-cell lymphoma

SM Horwitz, R Koch, P Porcu, Y Oki… - Blood, The Journal …, 2018 - ashpublications.org
Abstract Duvelisib (IPI-145) is an oral inhibitor of phosphatidylinositol 3-kinase (PI3K)–δ/γ
isoforms currently in clinical development. PI3K-δ/γ inhibition may directly inhibit malignant T …

PI3K signalling: the path to discovery and understanding

B Vanhaesebroeck, L Stephens… - Nature reviews Molecular …, 2012 - nature.com
Over the past two decades, our understanding of phospoinositide 3-kinases (PI3Ks) has
progressed from the identification of an enzymatic activity associated with growth factors …

PI3Kδ and primary immunodeficiencies

CL Lucas, A Chandra, S Nejentsev… - Nature Reviews …, 2016 - nature.com
Primary immunodeficiencies are inherited disorders of the immune system, often caused by
the mutation of genes required for lymphocyte development and activation. Recently …

Phosphoinositides: tiny lipids with giant impact on cell regulation

T Balla - Physiological reviews, 2013 - journals.physiology.org
Phosphoinositides (PIs) make up only a small fraction of cellular phospholipids, yet they
control almost all aspects of a cell's life and death. These lipids gained tremendous research …

Duvelisib, a novel oral dual inhibitor of PI3K-δ, γ, is clinically active in advanced hematologic malignancies

IW Flinn, S O'Brien, B Kahl, M Patel… - Blood, The Journal …, 2018 - ashpublications.org
Duvelisib is an oral dual inhibitor of phosphoinositide 3-kinase-δ (PI3K-δ) and PI3K-γ in late-
stage clinical development for hematologic malignancy treatment. This phase 1 study …