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 …

Targeting PI3 kinase in cancer

TM Bauer, MR Patel, JR Infante - Pharmacology & therapeutics, 2015 - Elsevier
Abstract The PI3K/Akt/mTOR pathway is the most frequently known activated aberrant
pathway in human cancers. Pathologic activation can occur at multiple levels along the …

Targeting the phosphoinositide 3-kinase pathway in cancer

P Liu, H Cheng, TM Roberts, JJ Zhao - Nature reviews Drug discovery, 2009 - nature.com
Abstract The phosphoinositide 3-kinase (PI3K) pathway is a key signal transduction system
that links oncogenes and multiple receptor classes to many essential cellular functions, and …

Inhibition of PI3K signaling spurs new therapeutic opportunities in inflammatory/autoimmune diseases and hematological malignancies

JG Foster, MD Blunt, E Carter, SG Ward - Pharmacological reviews, 2012 - ASPET
The phosphoinositide 3-kinase/mammalian target of rapamycin/protein kinase B
(PI3K/mTOR/Akt) signaling pathway is central to a plethora of cellular mechanisms in a wide …

The present and future of PI3K inhibitors for cancer therapy

P Castel, E Toska, JA Engelman, M Scaltriti - Nature cancer, 2021 - nature.com
Abstract Phosphoinositide 3-kinase (PI3K) signaling regulates cellular proliferation, survival
and metabolism, and its aberrant activation is one of the most frequent oncogenic events …

PI3Kδ inhibitors in cancer: rationale and serendipity merge in the clinic

DA Fruman, C Rommel - Cancer discovery, 2011 - AACR
Abstract Several phosphoinositide 3-kinase (PI3K) inhibitors are in the clinic and many more
are in preclinical development. CAL-101, a selective inhibitor of the PI3Kδ isoform, has …

[HTML][HTML] Drugging PI3K in cancer: refining targets and therapeutic strategies

TA Yap, L Bjerke, PA Clarke, P Workman - Current opinion in pharmacology, 2015 - Elsevier
Highlights•PI3K is an important target for innovative anticancer drug development and
precision medicine.•Over 30 small molecule PI3K inhibitors are currently in clinical trial …

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] Targeting PI3K in cancer: mechanisms and advances in clinical trials

J Yang, J Nie, X Ma, Y Wei, Y Peng, X Wei - Molecular cancer, 2019 - Springer
Abstract Phosphatidylinositol-3-kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR)
signaling is one of the most important intracellular pathways, which can be considered as a …

[HTML][HTML] The PI3K pathway in human disease

DA Fruman, H Chiu, BD Hopkins, S Bagrodia… - Cell, 2017 - cell.com
Phosphoinositide 3-kinase (PI3K) activity is stimulated by diverse oncogenes and growth
factor receptors, and elevated PI3K signaling is considered a hallmark of cancer. Many PI3K …