Phosphatidylinositol 3-kinase PI3K inhibitors as cancer therapeuticsReport as inadecuate

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Journal of Hematology and Oncology

, 6:88

Novel agents for cancer therapy


Phosphatidylinositol 3-kinases PI3Ks are lipid kinases that regulate diverse cellular processes including proliferation, adhesion, survival, and motility. Dysregulated PI3K pathway signaling occurs in one-third of human tumors. Aberrantly activated PI3K signaling also confers sensitivity and resistance to conventional therapies. PI3K has been recognized as an attractive molecular target for novel anti-cancer molecules. In the last few years, several classes of potent and selective small molecule PI3K inhibitors have been developed, and at least fifteen compounds have progressed into clinical trials as new anticancer drugs. Among these, idelalisib has advanced to phase III trials in patients with advanced indolent non-Hodgkin’s lymphoma and mantle cell lymphoma. In this review, we summarized the major molecules of PI3K signaling pathway, and discussed the preclinical models and clinical trials of potent small-molecule PI3K inhibitors.

AbbreviationsAMPK5′ adenosine monophosphate-activated protein kinase

BADBcl-2-associated death promoter

FAKFocal adhesion kinase

FOXOForkhead box protein O

GPCRG protein coupled receptors

GSK3Glycogen synthase kinase 3

JNKc-Jun N-terminal kinases

LKB1Liver kinase B1

MDM2Mouse double minute 2 homolog

mTOR C1Mammalian target of rapamycin complex 1

NF-κBNuclear factor kappa-light-chain-enhancer of activated B cells

PDK1Pyruvate dehydrogenase lipoamide kinase isozyme 1

PI3KPhosphatidylinositide 3-kinases

PIP3Phosphatidylinositol 3,4,5-triphosphate

PTENPhosphatase and tensin homolog

RHEBRas homolog enriched in brain

RTKReceptor tyrosine kinase

SHIPSH2-containing inositol phosphatase

TCS1-2Two-component signal transduction protein 1-2.

Electronic supplementary materialThe online version of this article doi:10.1186-1756-8722-6-88 contains supplementary material, which is available to authorized users.

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Author: Akintunde Akinleye - Parthu Avvaru - Muhammad Furqan - Yongping Song - Delong Liu



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