Drug discovery approaches targeting the PI3K/Akt pathway in cancer (Q37270455)

19 August 2017

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title

Drug discovery approaches targeting the PI3K/Akt pathway in cancer (English)

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19 August 2017

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C Garcia-Echeverria

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19 August 2017

W R Sellers

series ordinal

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19 August 2017

language of work or name

English

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publication date

1 September 2008

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19 August 2017

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19 August 2017

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19 August 2017

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19 August 2017

page(s)

5511-5526

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Expression, purification, characterization and homology modeling of active Akt/PKB, a key enzyme involved in cell survival signaling

19 August 2017

cites work

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

HSP90 and the chaperoning of cancer

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

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21 January 2018

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Mechanism of activation of protein kinase B by insulin and IGF-1

31 March 2020

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Characterization of a 3-phosphoinositide-dependent protein kinase which phosphorylates and activates protein kinase Balpha

31 March 2020

1 reference

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Celecoxib induces apoptosis by inhibiting 3-phosphoinositide-dependent protein kinase-1 activity in the human colon cancer HT-29 cell line

31 March 2020

1 reference

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

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Akt forms an intracellular complex with heat shock protein 90 (Hsp90) and Cdc37 and is destabilized by inhibitors of Hsp90 function

31 March 2020

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https://api.crossref.org/works/10.1038%2FONC.2008.246

Akt activation by growth factors is a multiple-step process: the role of the PH domain

31 March 2020

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Identification of a pocket in the PDK1 kinase domain that interacts with PIF and the C-terminal residues of PKA

31 March 2020

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https://api.crossref.org/works/10.1038%2FONC.2008.246

PKBalpha/Akt1 acts downstream of DNA-PK in the DNA double-strand break response and promotes survival

31 March 2020

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

31 March 2020

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Structure-based optimization of novel azepane derivatives as PKB inhibitors

31 March 2020

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4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer

31 March 2020

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The PTEN/PI3K/AKT signalling pathway in cancer, therapeutic implications

31 March 2020

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A transforming mutation in the pleckstrin homology domain of AKT1 in cancer

31 March 2020

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Phosphorylation of Ser-241 is essential for the activity of 3-phosphoinositide-dependent protein kinase-1: identification of five sites of phosphorylation in vivo

31 March 2020

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SNX2112, a synthetic heat shock protein 90 inhibitor, has potent antitumor activity against HER kinase-dependent cancers

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Characterization of structurally distinct, isoform-selective phosphoinositide 3'-kinase inhibitors in combination with radiation in the treatment of glioblastoma

31 March 2020

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https://api.crossref.org/works/10.1038%2FONC.2008.246

Hsp90: the vulnerable chaperone

31 March 2020

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https://api.crossref.org/works/10.1038%2FONC.2008.246

In vitro combination treatment with perifosine and UCN-01 demonstrates synergism against prostate (PC-3) and lung (A549) epithelial adenocarcinoma cell lines

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

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

31 March 2020

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https://api.crossref.org/works/10.1038%2FONC.2008.246

Inhibitors of protein kinase C. 2. Substituted bisindolylmaleimides with improved potency and selectivity

31 March 2020

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PI 3-kinase, Akt and cell survival

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

NVP-AUY922: a novel heat shock protein 90 inhibitor active against xenograft tumor growth, angiogenesis, and metastasis

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Phase II study of perifosine in previously untreated patients with metastatic melanoma

31 March 2020

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https://api.crossref.org/works/10.1038%2FONC.2008.246

A dual phosphoinositide-3-kinase alpha/mTOR inhibitor cooperates with blockade of epidermal growth factor receptor in PTEN-mutant glioma

31 March 2020

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https://api.crossref.org/works/10.1038%2FONC.2008.246

Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1.

31 March 2020

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https://api.crossref.org/works/10.1038%2FONC.2008.246

Identification of a PKB/Akt hydrophobic motif Ser-473 kinase as DNA-dependent protein kinase

31 March 2020

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https://api.crossref.org/works/10.1038%2FONC.2008.246

Survival-signaling pathway as a promising target for cancer chemotherapy

31 March 2020

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https://api.crossref.org/works/10.1038%2FONC.2008.246

Involvement of Hsp90 in signaling and stability of 3-phosphoinositide-dependent kinase-1.

31 March 2020

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https://api.crossref.org/works/10.1038%2FONC.2008.246

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

31 March 2020

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https://api.crossref.org/works/10.1038%2FONC.2008.246

Mutants of protein kinase A that mimic the ATP-binding site of protein kinase B (AKT)

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90.

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

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

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Optimization of 2,3,5-trisubstituted pyridine derivatives as potent allosteric Akt1 and Akt2 inhibitors

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Pharmacodynamic markers of perifosine efficacy

31 March 2020

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https://api.crossref.org/works/10.1038%2FONC.2008.246

Inhibition of protein kinase B/Akt. implications for cancer therapy

31 March 2020

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https://api.crossref.org/works/10.1038%2FONC.2008.246

Insulin-stimulated protein kinase B phosphorylation on Ser-473 is independent of its activity and occurs through a staurosporine-insensitive kinase

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

In vivo antitumor efficacy of 17-DMAG (17-dimethylaminoethylamino-17-demethoxygeldanamycin hydrochloride), a water-soluble geldanamycin derivative

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

The phosphatidylinositol 3-kinase inhibitor, PX-866, is a potent inhibitor of cancer cell motility and growth in three-dimensional cultures

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

The cyclooxygenase-2 inhibitor celecoxib induces apoptosis by blocking Akt activation in human prostate cancer cells independently of Bcl-2

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

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

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Targeting Akt and heat shock protein 90 produces synergistic multiple myeloma cell cytotoxicity in the bone marrow microenvironment

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

The phosphatidylinositol-3-kinase inhibitor PX-866 overcomes resistance to the epidermal growth factor receptor inhibitor gefitinib in A-549 human non-small cell lung cancer xenografts

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Heat shock protein 90 inhibitors. A text book example of medicinal chemistry?

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

NVP-AUY922: a small molecule HSP90 inhibitor with potent antitumor activity in preclinical breast cancer models

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Synergistic antileukemic interactions between 17-AAG and UCN-01 involve interruption of RAF/MEK- and AKT-related pathways

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Molecular cloning of a second form of rac protein kinase

31 March 2020

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https://api.crossref.org/works/10.1038%2FONC.2008.246

Molecular cloning and identification of a serine/threonine protein kinase of the second-messenger subfamily

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

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

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

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

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Structural insights into the regulation of PDK1 by phosphoinositides and inositol phosphates.

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Structural basis for UCN-01 (7-hydroxystaurosporine) specificity and PDK1 (3-phosphoinositide-dependent protein kinase-1) inhibition

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

7-hydroxystaurosporine (UCN-01) inhibition of Akt Thr308 but not Ser473 phosphorylation: a basis for decreased insulin-stimulated glucose transport

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Essential role of PDK1 in regulating cell size and development in mice

31 March 2020

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https://api.crossref.org/works/10.1038%2FONC.2008.246

Targeting serine/threonine protein kinase B/Akt and cell-cycle checkpoint kinases for treating cancer

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Enhancement of antitumor activity of the anti-EGF receptor monoclonal antibody cetuximab/C225 by perifosine in PTEN-deficient cancer cells

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

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

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Class IA phosphatidylinositol 3-kinase: from their biologic implication in human cancers to drug discovery

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

The Akt pathway: molecular targets for anti-cancer drug development

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Combination of trastuzumab and tanespimycin (17-AAG, KOS-953) is safe and active in trastuzumab-refractory HER-2 overexpressing breast cancer: a phase I dose-escalation study

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

PDK1, the master regulator of AGC kinase signal transduction

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Heat-shock protein 90 inhibitors as novel cancer chemotherapeutic agents

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

A phase II study of perifosine in androgen independent prostate cancer

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Phase I and pharmacodynamic study of 17-(allylamino)-17-demethoxygeldanamycin in adult patients with refractory advanced cancers

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

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

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Epidemiology and clinical burden of acute myeloid leukemia

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

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

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanamycin

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Anti-cancer alkyl-lysophospholipids inhibit the phosphatidylinositol 3-kinase-Akt/PKB survival pathway

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

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

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Interference with PDK1-Akt survival signaling pathway by UCN-01 (7-hydroxystaurosporine).

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

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

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

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

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Optimal classes of chemotherapeutic agents sensitized by specific small-molecule inhibitors of akt in vitro and in vivo

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Crystal structure of an Hsp90-geldanamycin complex: targeting of a protein chaperone by an antitumor agent

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Protein kinase B kinases that mediate phosphatidylinositol 3,4,5-trisphosphate-dependent activation of protein kinase B

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Dual Role of Phosphatidylinositol-3,4,5-trisphosphate in the Activation of Protein Kinase B

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Signalling profile and antitumour activity of the novel Hsp90 inhibitor NVP-AUY922 in multiple myeloma.

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Development of 17-allylamino-17-demethoxygeldanamycin hydroquinone hydrochloride (IPI-504), an anti-cancer agent directed against Hsp90.

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Synthesis and biological activities of novel 17-aminogeldanamycin derivatives

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Deregulation of the Akt pathway in human cancer

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Discovery of lactoquinomycin and related pyranonaphthoquinones as potent and allosteric inhibitors of AKT/PKB: mechanistic involvement of AKT catalytic activation loop cysteines

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

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

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Structural insights into phosphoinositide 3-kinase catalysis and signalling

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

UCN-01 in combination with topotecan in patients with advanced recurrent ovarian cancer: a study of the Princess Margaret Hospital Phase II consortium

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

DNA-dependent protein kinase in nonhomologous end joining: a lock with multiple keys?

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Regulation of class III (Vps34) PI3Ks

31 March 2020

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https://api.crossref.org/works/10.1038%2FONC.2008.246

Crystal structure of an activated Akt/protein kinase B ternary complex with GSK3-peptide and AMP-PNP

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Molecular mechanism for the regulation of protein kinase B/Akt by hydrophobic motif phosphorylation

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

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

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Inverse in silico screening for identification of kinase inhibitor targets.

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

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

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FONC.2008.246

31 March 2020

Identifiers

DOI

10.1038/ONC.2008.246

1 reference

19 August 2017

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