(Q33852403)

29 July 2017

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title

Discovery of novel anticancer therapeutics targeting the PI3K/Akt/mTOR pathway (English)

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29 July 2017

Sauveur-Michel Maira

1

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PubMed ID

21426073

29 July 2017

Pascal Furet

series ordinal

2

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PubMed ID

21426073

29 July 2017

Frédéric Stauffer

series ordinal

3

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29 July 2017

1 April 2009

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Future Medicinal Chemistry

29 July 2017

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29 July 2017

1

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29 July 2017

137-155

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29 July 2017

1

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Inositol derivatives: evolution and functions

29 July 2017

1 reference

PI3K pathway alterations in cancer: variations on a theme

21 January 2018

1 reference

The role of PTEN signaling perturbations in cancer and in targeted therapy

21 January 2018

1 reference

The evolution of phosphatidylinositol 3-kinases as regulators of growth and metabolism

21 January 2018

1 reference

Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers

21 January 2018

1 reference

mTOR inhibition reverses Akt-dependent prostate intraepithelial neoplasia through regulation of apoptotic and HIF-1-dependent pathways

21 January 2018

1 reference

Phosphorylation and regulation of Akt/PKB by the rictor-mTOR complex

21 January 2018

1 reference

The TSC1-TSC2 complex: a molecular switchboard controlling cell growth

21 January 2018

1 reference

Chemical modification of rapamycin: the discovery of SDZ RAD.

21 January 2018

1 reference

Mechanisms of Disease: survival benefit of temsirolimus validates a role for mTOR in the management of advanced RCC.

21 January 2018

1 reference

Efficacy of everolimus in advanced renal cell carcinoma: a double-blind, randomised, placebo-controlled phase III trial

21 January 2018

1 reference

Prolonged rapamycin treatment inhibits mTORC2 assembly and Akt/PKB

21 January 2018

1 reference

Isoform-specific phosphoinositide 3-kinase inhibitors from an arylmorpholine scaffold

21 January 2018

1 reference

Structural Determinants of Phosphoinositide 3-Kinase Inhibition by Wortmannin, LY294002, Quercetin, Myricetin, and Staurosporine

21 January 2018

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Wortmannin inactivates phosphoinositide 3-kinase by covalent modification of Lys-802, a residue involved in the phosphate transfer reaction

21 January 2018

1 reference

Wortmannin is a potent phosphatidylinositol 3-kinase inhibitor: the role of phosphatidylinositol 3,4,5-trisphosphate in neutrophil responses.

21 January 2018

1 reference

PWT-458, a novel pegylated-17-hydroxywortmannin, inhibits phosphatidylinositol 3-kinase signaling and suppresses growth of solid tumors

21 January 2018

1 reference

A vascular targeted pan phosphoinositide 3-kinase inhibitor prodrug, SF1126, with antitumor and antiangiogenic activity

21 January 2018

1 reference

Adaptation of the Folts and electrolytic methods of arterial thrombosis for the study of anti-thrombotic molecules in small animals

21 January 2018

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PI 3-kinase p110beta: a new target for antithrombotic therapy

21 January 2018

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Ligand efficiency: a useful metric for lead selection

21 January 2018

1 reference

Antitumor activity of ZSTK474, a new phosphatidylinositol 3-kinase inhibitor

21 January 2018

1 reference

Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity

21 January 2018

1 reference

A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma

21 January 2018

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Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases.

21 January 2018

1 reference

The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer

21 January 2018

1 reference

Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors

21 January 2018

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Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases

21 January 2018

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Molecular cloning, expression and characterization of the human serine/threonine kinase Akt-3

21 January 2018

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Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors

21 January 2018

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Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity

21 January 2018

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Design and crystal structures of protein kinase B-selective inhibitors in complex with protein kinase A and mutants

21 January 2018

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A structural comparison of inhibitor binding to PKB, PKA and PKA-PKB chimera

21 January 2018

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Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase B/Akt inhibitors with reduced hypotension

21 January 2018

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Akt inhibitor A-443654 induces rapid Akt Ser-473 phosphorylation independent of mTORC1 inhibition

21 January 2018

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PDK1, the master regulator of AGC kinase signal transduction

21 January 2018

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Allosteric activation of the protein kinase PDK1 with low molecular weight compounds

21 January 2018

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High-resolution structure of the pleckstrin homology domain of protein kinase b/akt bound to phosphatidylinositol (3,4,5)-trisphosphate

21 January 2018

1 reference

Anticancer alkylphospholipids: mechanisms of action, cellular sensitivity and resistance, and clinical prospects

21 January 2018

1 reference

Signalling specificity of Ser/Thr protein kinases through docking-site-mediated interactions

21 January 2018

1 reference

From the cyclooxygenase-2 inhibitor celecoxib to a novel class of 3-phosphoinositide-dependent protein kinase-1 inhibitors

21 January 2018

1 reference

2-amino-N-{4-[5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]-phenyl} acetamide (OSU-03012), a celecoxib derivative, directly targets p21-activated kinase

21 January 2018

1 reference

Potentiation of antileukemic therapies by the dual PI3K/PDK-1 inhibitor, BAG956: effects on BCR-ABL- and mutant FLT3-expressing cells

21 January 2018

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A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling

21 January 2018

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The structure of a human p110alpha/p85alpha complex elucidates the effects of oncogenic PI3Kalpha mutations

21 January 2018

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Structural comparisons of class I phosphoinositide 3-kinases

21 January 2018

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Proliferative defect and embryonic lethality in mice homozygous for a deletion in the p110alpha subunit of phosphoinositide 3-kinase

21 January 2018

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Critical role for the p110alpha phosphoinositide-3-OH kinase in growth and metabolic regulation

21 January 2018

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The p110alpha isoform of PI3K is essential for proper growth factor signaling and oncogenic transformation

21 January 2018

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Phosphoinositide 3-kinase p110beta activity: key role in metabolism and mammary gland cancer but not development

21 January 2018

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The p110beta isoform of phosphoinositide 3-kinase signals downstream of G protein-coupled receptors and is functionally redundant with p110gamma.

21 January 2018

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PTEN-deficient cancers depend on PIK3CB.

21 January 2018

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Validating cancer drug targets

21 January 2018

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Breast tumor cells with PI3K mutation or HER2 amplification are selectively addicted to Akt signaling

21 January 2018

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Insulin growth factor-binding protein 2 is a candidate biomarker for PTEN status and PI3K/Akt pathway activation in glioblastoma and prostate cancer

21 January 2018

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Poor prognosis in carcinoma is associated with a gene expression signature of aberrant PTEN tumor suppressor pathway activity.

21 January 2018

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Circulating tumour cell detection on its way to routine diagnostic implementation?

21 January 2018

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Detection of mutated K-ras DNA in urine, plasma, and serum of patients with colorectal carcinoma or adenomatous polyps.

21 January 2018

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Dose- and schedule-dependent inhibition of the mammalian target of rapamycin pathway with everolimus: a phase I tumor pharmacodynamic study in patients with advanced solid tumors.

21 January 2018

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Identifying optimal biologic doses of everolimus (RAD001) in patients with cancer based on the modeling of preclinical and clinical pharmacokinetic and pharmacodynamic data

21 January 2018

1 reference

The skin and hair as surrogate tissues for measuring the target effect of inhibitors of phosphoinositide-3-kinase signaling

21 January 2018

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Class 1A PI3K regulates vessel integrity during development and tumorigenesis

21 January 2018

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Angiogenesis selectively requires the p110alpha isoform of PI3K to control endothelial cell migration.

21 January 2018

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Effects of the dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235 on the tumor vasculature: implications for clinical imaging

21 January 2018

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SOS phosphorylation and disassociation of the Grb2-SOS complex by the ERK and JNK signaling pathways

21 January 2018

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The PTEN-PI3K pathway: of feedbacks and cross-talks

21 January 2018

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mTOR inhibition induces upstream receptor tyrosine kinase signaling and activates Akt

21 January 2018

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The BAD protein integrates survival signaling by EGFR/MAPK and PI3K/Akt kinase pathways in PTEN-deficient tumor cells

21 January 2018

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The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP

21 January 2018

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Allelic dilution obscures detection of a biologically significant resistance mutation in EGFR-amplified lung cancer

21 January 2018

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ErbB-3 mediates phosphoinositide 3-kinase activity in gefitinib-sensitive non-small cell lung cancer cell lines

21 January 2018

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Escape from HER-family tyrosine kinase inhibitor therapy by the kinase-inactive HER3

21 January 2018

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MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling

21 January 2018

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A functional genetic approach identifies the PI3K pathway as a major determinant of trastuzumab resistance in breast cancer

21 January 2018

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Transforming growth factor beta engages TACE and ErbB3 to activate phosphatidylinositol-3 kinase/Akt in ErbB2-overexpressing breast cancer and desensitizes cells to trastuzumab

21 January 2018

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Acquired resistance to small molecule ErbB2 tyrosine kinase inhibitors

21 January 2018

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NVP-BEZ235, a dual PI3K/mTOR inhibitor, prevents PI3K signaling and inhibits the growth of cancer cells with activating PI3K mutations.

21 January 2018

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Phosphatidylinositol 3-kinase hyperactivation results in lapatinib resistance that is reversed by the mTOR/phosphatidylinositol 3-kinase inhibitor NVP-BEZ235.

21 January 2018

1 reference

Mechanisms of disease: the PI3K-Akt-PTEN signaling node--an intercept point for the control of angiogenesis in brain tumors

21 January 2018

1 reference

Rapamune® (RAPA, rapamycin, sirolimus): mechanism of action immunosuppressive effect results from blockade of signal transduction and inhibition of cell cycle progression

21 January 2018

1 reference

Structural insights into phosphoinositide 3-kinase catalysis and signalling

21 January 2018

1 reference

Rapamycin (AY-22,989), a new antifungal antibiotic. II. Fermentation, isolation and characterization.

21 January 2018

1 reference

12 April 2024

https://opencitations.net/index/api/v1/citations/10.7164/ANTIBIOTICS.28.727

UCN-01, a selective inhibitor of protein kinase C from Streptomyces.

1 reference

12 April 2024

https://opencitations.net/index/api/v1/citations/10.7164/ANTIBIOTICS.40.1782

Identifiers

DOI

10.4155/FMC.09.5

1 reference

29 July 2017

1 reference

PubMed ID

21426073