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 …

[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 …

Umbralisib, a dual PI3Kδ/CK1ε inhibitor in patients with relapsed or refractory indolent lymphoma

NH Fowler, F Samaniego, W Jurczak… - Journal of Clinical …, 2021 - ascopubs.org
PURPOSE Phosphatidylinositol-3-kinase (PI3K) inhibitors have shown activity in relapsed or
refractory (R/R) indolent non-Hodgkin lymphoma (iNHL). PI3K inhibitors have been …

Targeting the C481S ibrutinib-resistance mutation in Bruton's tyrosine kinase using PROTAC-mediated degradation

AD Buhimschi, HA Armstrong, M Toure… - Biochemistry, 2018 - ACS Publications
Inhibition of Bruton's tyrosine kinase (BTK) with the irreversible inhibitor ibrutinib has
emerged as a transformative treatment option for patients with chronic lymphocytic leukemia …

Signaling by the phosphoinositide 3-kinase family in immune cells

K Okkenhaug - Annual review of immunology, 2013 - annualreviews.org
Phosphoinositide 3-kinases (PI3Ks) control many important aspects of immune cell
development, differentiation, and function. Mammals have eight PI3K catalytic subunits that …

Class I PI3K in oncogenic cellular transformation

L Zhao, PK Vogt - Oncogene, 2008 - nature.com
Class I phosphoinositide 3-kinase (PI3K) is a dimeric enzyme, consisting of a catalytic and a
regulatory subunit. The catalytic subunit occurs in four isoforms designated as p110α …

The polycomb protein Ezh2 regulates differentiation and plasticity of CD4+ T helper type 1 and type 2 cells

DJ Tumes, A Onodera, A Suzuki, K Shinoda, Y Endo… - Immunity, 2013 - cell.com
After antigen encounter by CD4+ T cells, polarizing cytokines induce the expression of
master regulators that control differentiation. Inactivation of the histone methyltransferase …

Targeting phosphoinositide 3-kinase—moving towards therapy

R Marone, V Cmiljanovic, B Giese… - Biochimica et Biophysica …, 2008 - Elsevier
Phosphoinositide 3-kinases (PI3K) orchestrate cell responses including mitogenic signaling,
cell survival and growth, metabolic control, vesicular trafficking, degranulation, cytoskeletal …

The microRNA miR-181 is a critical cellular metabolic rheostat essential for NKT cell ontogenesis and lymphocyte development and homeostasis

J Henao-Mejia, A Williams, LA Goff, M Staron… - Immunity, 2013 - cell.com
Regulation of metabolic pathways in the immune system provides a mechanism to actively
control cellular function, growth, proliferation, and survival. Here, we report that miR-181 is a …

Mammalian phosphoinositide kinases and phosphatases

T Sasaki, S Takasuga, J Sasaki, S Kofuji… - Progress in lipid …, 2009 - Elsevier
Phosphoinositides are lipids that are present in the cytoplasmic leaflet of a cell's plasma and
internal membranes and play pivotal roles in the regulation of a wide variety of cellular …