Drugging the PI3 kinome: from chemical tools to drugs in the clinic. (Q35622141)

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:20179189%20AND%20SRC:MED&resulttype=core&format=json

18 January 2020

review article

1 reference

title

Drugging the PI3 kinome: from chemical tools to drugs in the clinic (English)

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:20179189%20AND%20SRC:MED&resulttype=core&format=json

18 January 2020

1 reference

2

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:20179189%20AND%20SRC:MED&resulttype=core&format=json

18 January 2020

Florence Raynaud

series ordinal

3

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:20179189%20AND%20SRC:MED&resulttype=core&format=json

18 January 2020

author name string

Rob L M van Montfort

series ordinal

4

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:20179189%20AND%20SRC:MED&resulttype=core&format=json

18 January 2020

Paul Workman

series ordinal

1

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:20179189%20AND%20SRC:MED&resulttype=core&format=json

18 January 2020

language of work or name

English

0 references

publication date

23 February 2010

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18 January 2020

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:20179189%20AND%20SRC:MED&resulttype=core&format=json

18 January 2020

volume

70

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18 January 2020

page(s)

2146-2157

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18 January 2020

issue

6

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NVP-BEZ235, a novel dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor, elicits multifaceted antitumor activities in human gliomas

18 January 2020

cites work

1 reference

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12 July 2018

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Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941

12 July 2018

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AKT-independent signaling downstream of oncogenic PIK3CA mutations in human cancer

12 July 2018

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In vivo antitumor activity of MEK and phosphatidylinositol 3-kinase inhibitors in basal-like breast cancer models.

12 July 2018

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A crowdsourcing evaluation of the NIH chemical probes

12 July 2018

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Suppression of HER2/HER3-mediated growth of breast cancer cells with combinations of GDC-0941 PI3K inhibitor, trastuzumab, and pertuzumab

12 July 2018

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Ligand-independent HER2/HER3/PI3K complex is disrupted by trastuzumab and is effectively inhibited by the PI3K inhibitor GDC-0941

12 July 2018

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Gene expression patterns in mismatch repair-deficient colorectal cancers highlight the potential therapeutic role of inhibitors of the phosphatidylinositol 3-kinase-AKT-mammalian target of rapamycin pathway

12 July 2018

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Structure-based design of molecular cancer therapeutics

12 July 2018

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PIK3CA mutations in human solid tumors: role in sensitivity to various therapeutic approaches

12 July 2018

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Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAFV600E mutational status and sustained extracellular signal-regulated kinase/mitogen-activated protein kinase pathway suppression.

12 July 2018

1 reference

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PI 3-kinase and cancer: changing accents

12 July 2018

1 reference

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Molecular pharmacology of phosphatidylinositol 3-kinase inhibition in human glioma

12 July 2018

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Take your PIK: phosphatidylinositol 3-kinase inhibitors race through the clinic and toward cancer therapy

12 July 2018

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

12 July 2018

1 reference

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Drug discovery approaches targeting the PI3K/Akt pathway in cancer

12 July 2018

1 reference

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PI3K pathway alterations in cancer: variations on a theme

12 July 2018

1 reference

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PTEN-deficient cancers depend on PIK3CB.

12 July 2018

1 reference

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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

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3242038

Targeting the PI3K-AKT-mTOR pathway: progress, pitfalls, and promises

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3242038

Discovery of drug-resistant and drug-sensitizing mutations in the oncogenic PI3K isoform p110 alpha

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3242038

Essential roles of PI(3)K-p110beta in cell growth, metabolism and tumorigenesis

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3242038

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

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3242038

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

12 July 2018

1 reference

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The selectivity of protein kinase inhibitors: a further update

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3242038

Application of meso scale technology for the measurement of phosphoproteins in human tumor xenografts

12 July 2018

1 reference

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Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors

12 July 2018

1 reference

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

12 July 2018

1 reference

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Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors.

12 July 2018

1 reference

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Pharmacodynamic biomarkers for molecular cancer therapeutics

12 July 2018

1 reference

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New approaches to molecular cancer therapeutics

12 July 2018

1 reference

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Synthesis and biological evaluation of imidazo[1,2-a]pyridine derivatives as novel PI3 kinase p110alpha inhibitors

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3242038

Drugging the cancer kinome: progress and challenges in developing personalized molecular cancer therapeutics

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3242038

Synthesis and biological evaluation of 4-morpholino-2-phenylquinazolines and related derivatives as novel PI3 kinase p110alpha inhibitors

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3242038

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

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3242038

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

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3242038

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

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3242038

Developments in the CCP4 molecular-graphics project

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3242038

NIH Molecular Libraries Initiative

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3242038

The CCP4 suite: programs for protein crystallography

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3242038

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3242038

High frequency of mutations of the PIK3CA gene in human cancers

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3242038

Auditing the pharmacological accounts for Hsp90 molecular chaperone inhibitors: unfolding the relationship between pharmacokinetics and pharmacodynamics.

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3242038

The specificities of protein kinase inhibitors: an update

12 July 2018

1 reference

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Protein kinases--the major drug targets of the twenty-first century?

12 July 2018

1 reference

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The phosphoinositide 3-kinase pathway

12 July 2018

1 reference

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Synthesis and function of 3-phosphorylated inositol lipids

12 July 2018

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

12 July 2018

1 reference

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Specificity and mechanism of action of some commonly used protein kinase inhibitors

12 July 2018

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

12 July 2018

1 reference

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

12 July 2018

1 reference

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A specific inhibitor of phosphatidylinositol 3-kinase, 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one (LY294002)

12 July 2018

1 reference

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Dissecting isoform selectivity of PI3K inhibitors: the role of non-conserved residues in the catalytic pocket

12 July 2018

1 reference

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The PI3K inhibitor arsenal: choose your weapon!

25 September 2018

1 reference

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Chemically targeting the PI3K family

25 September 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3242038

25 September 2018

Drugging the PI3 kinome.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3242038

Structural insights into phosphoinositide 3-kinase catalysis and signalling

25 September 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3242038

Inhibition of the phagocytosis-induced respiratory burst by the fungal metabolite wortmannin and some analogues

15 November 2018

1 reference

PubMed

12 December 2020

Drugging the cancer genome: new challenges of infrequent and combinatorial targets

1 reference

PubMed

12 December 2020

1 reference

12 December 2020

The p110delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors

1 reference

PubMed

12 December 2020

10.1158/0008-5472.CAN-09-4355

Identifiers

DOI

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:20179189%20AND%20SRC:MED&resulttype=core&format=json

18 January 2020

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:20179189%20AND%20SRC:MED&resulttype=core&format=json

18 January 2020

1 reference