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 …

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 …

Structural basis for activation and inhibition of class I phosphoinositide 3-kinases

O Vadas, JE Burke, X Zhang, A Berndt, RL Williams - Science signaling, 2011 - science.org
Phosphoinositide 3-kinases (PI3Ks) are implicated in a broad spectrum of cellular activities,
such as growth, proliferation, differentiation, migration, and metabolism. Activation of class I …

Synergy in activating class I PI3Ks

JE Burke, RL Williams - Trends in biochemical sciences, 2015 - cell.com
The class I phosphoinositide 3-kinases (PI3Ks) are lipid kinases that transduce a host of
cellular signals and regulate a broad range of essential functions including growth …

Class I phosphoinositide 3-kinase (PI3K) regulatory subunits and their roles in signaling and disease

MK Rathinaswamy, JE Burke - Advances in Biological Regulation, 2020 - Elsevier
The Class I phosphoinositide 3-kinases (PI3Ks) are a group of heterodimeric lipid kinases
that regulate crucial cellular processes including proliferation, survival, growth, and …

Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent

J Ni, Q Liu, S Xie, C Carlson, T Von, K Vogel, S Riddle… - Cancer discovery, 2012 - AACR
Genetic approaches have shown that the p110β isoform of class Ia phosphatidylinositol-3-
kinase (PI3K) is essential for the growth of PTEN-null tumors. Thus, it is desirable to develop …

[HTML][HTML] Structure of lipid kinase p110β/p85β elucidates an unusual SH2-domain-mediated inhibitory mechanism

X Zhang, O Vadas, O Perisic, KE Anderson, J Clark… - Molecular cell, 2011 - cell.com
Summary Phosphoinositide 3-kinases (PI3Ks) are essential for cell growth, migration, and
survival. The structure of a p110β/p85β complex identifies an inhibitory function for the C …

G protein–coupled receptor–mediated activation of p110β by Gβγ is required for cellular transformation and invasiveness

HA Dbouk, O Vadas, A Shymanets, JE Burke… - Science …, 2012 - science.org
Synergistic activation by heterotrimeric guanine nucleotide–binding protein (G protein)–
coupled receptors (GPCRs) and receptor tyrosine kinases distinguishes p110β from other …

The p110α and p110β isoforms of PI3K play divergent roles in mammary gland development and tumorigenesis

T Utermark, T Rao, H Cheng, Q Wang… - Genes & …, 2012 - genesdev.cshlp.org
Class Ia phosphatidylinositol 3 kinase (PI3K) is required for oncogenic receptor-mediated
transformation; however, the individual roles of the two commonly expressed class Ia PI3K …

Structural determinants of isoform selectivity in PI3K inhibitors

MS Miller, PE Thompson, SB Gabelli - Biomolecules, 2019 - mdpi.com
Phosphatidylinositol 3-kinases (PI3Ks) are important therapeutic targets for the treatment of
cancer, thrombosis, and inflammatory and immune diseases. The four highly homologous …