PI3K inhibitors are finally coming of age
Abstract Overactive phosphoinositide 3-kinase (PI3K) in cancer and immune dysregulation
has spurred extensive efforts to develop therapeutic PI3K inhibitors. Although progress has …
has spurred extensive efforts to develop therapeutic PI3K inhibitors. Although progress has …
FDA-approved small-molecule kinase inhibitors
P Wu, TE Nielsen, MH Clausen - Trends in pharmacological sciences, 2015 - cell.com
Kinases have emerged as one of the most intensively pursued targets in current
pharmacological research, especially for cancer, due to their critical roles in cellular …
pharmacological research, especially for cancer, due to their critical roles in cellular …
Atropisomerism in drug discovery: a medicinal chemistry perspective inspired by atropisomeric class I PI3K inhibitors
S Perreault, J Chandrasekhar… - Accounts of Chemical …, 2022 - ACS Publications
Conspectus Atropisomerism is a type of axial chirality resulting from hindered rotation about
a σ bond that gives rise to nonsuperimposable stereoisomers (termed “atropisomers”). The …
a σ bond that gives rise to nonsuperimposable stereoisomers (termed “atropisomers”). The …
PI3K and cancer: lessons, challenges and opportunities
DA Fruman, C Rommel - Nature reviews Drug discovery, 2014 - nature.com
The central role of phosphoinositide 3-kinase (PI3K) activation in tumour cell biology has
prompted a sizeable effort to target PI3K and/or downstream kinases such as AKT and …
prompted a sizeable effort to target PI3K and/or downstream kinases such as AKT and …
Dominant-activating germline mutations in the gene encoding the PI (3) K catalytic subunit p110δ result in T cell senescence and human immunodeficiency
The p110δ subunit of phosphatidylinositol-3-OH kinase (PI (3) K) is selectively expressed in
leukocytes and is critical for lymphocyte biology. Here we report fourteen patients from …
leukocytes and is critical for lymphocyte biology. Here we report fourteen patients from …
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 …
progressed from the identification of an enzymatic activity associated with growth factors …
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 …
control almost all aspects of a cell's life and death. These lipids gained tremendous research …
Structural basis for regulation of phosphoinositide kinases and their involvement in human disease
JE Burke - Molecular cell, 2018 - cell.com
Lipid phosphoinositides play fundamental roles in virtually all pathways that control a cell's
decision to grow, move, divide, and die. Because of this, kinases that phosphorylate …
decision to grow, move, divide, and die. Because of this, kinases that phosphorylate …
A highly potent and selective Vps34 inhibitor alters vesicle trafficking and autophagy
B Ronan, O Flamand, L Vescovi, C Dureuil… - Nature chemical …, 2014 - nature.com
Vps34 is a phosphoinositide 3-kinase (PI3K) class III isoform that has attracted major
attention over the recent years because of its role in autophagy. Herein we describe the …
attention over the recent years because of its role in autophagy. Herein we describe the …
Phosphoinositide 3-kinase δ gene mutation predisposes to respiratory infection and airway damage
Genetic mutations cause primary immunodeficiencies (PIDs) that predispose to infections.
Here, we describe activated PI3K-δ syndrome (APDS), a PID associated with a dominant …
Here, we describe activated PI3K-δ syndrome (APDS), a PID associated with a dominant …