(Q33552984)

28 July 2017

title

Discovery of PDK1 kinase inhibitors with a novel mechanism of action by ultrahigh throughput screening (English)

1 reference

28 July 2017

Jannik N Andersen

9

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Alan B. Northrup

7

object named as

Alan Northrup

1 reference

28 July 2017

Ekaterina V Bobkova

1

1 reference

28 July 2017

Michael J Weber

2

1 reference

28 July 2017

Zangwei Xu

3

1 reference

28 July 2017

Yan-Ling Zhang

4

1 reference

28 July 2017

Joon Jung

5

1 reference

28 July 2017

Peter Blume-Jensen

6

1 reference

28 July 2017

Priya Kunapuli

8

1 reference

28 July 2017

Ilona Kariv

10

1 reference

28 July 2017

language of work or name

English

0 references

publication date

12 April 2010

1 reference

Journal of Biological Chemistry

28 July 2017

number of pages

9

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based on heuristic

inferred from page(s)

published in

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28 July 2017

volume

285

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28 July 2017

issue

24

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28 July 2017

page(s)

18838-18846

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Development of high-throughput TR-FRET and AlphaScreen assays for identification of potent inhibitors of PDK1.

28 July 2017

cites work

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

Structure and allosteric effects of low-molecular-weight activators on the protein kinase PDK1

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

The current status of drug discovery against the human kinome

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

Identification of allosteric PIF-pocket ligands for PDK1 using NMR-based fragment screening and 1H-15N TROSY experiments

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

Wild-type BRAF is required for response to panitumumab or cetuximab in metastatic colorectal cancer

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

Small-molecule inhibitors of PDK1.

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

A quantitative atlas of mitotic phosphorylation

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

The use of differential scanning fluorimetry to detect ligand interactions that promote protein stability

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

The hallmark of AGC kinase functional divergence is its C-terminal tail, a cis-acting regulatory module

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

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

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

Global, in vivo, and site-specific phosphorylation dynamics in signaling networks

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

Steady-state kinetic mechanism of PDK1.

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

Thermodynamic stability of carbonic anhydrase: measurements of binding affinity and stoichiometry using ThermoFluor.

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

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

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

PDK1, the master regulator of AGC kinase signal transduction

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

Interactions of LY333531 and other bisindolyl maleimide inhibitors with PDK1

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

PDK1 and PKB/Akt: ideal targets for development of new strategies to structure-based drug design

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

Crystal structure of PTP1B complexed with a potent and selective bidentate inhibitor

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

The protein kinase complement of the human genome

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

High-density miniaturized thermal shift assays as a general strategy for drug discovery

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

The PIF-binding pocket in PDK1 is essential for activation of S6K and SGK, but not PKB.

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

A 3-phosphoinositide-dependent protein kinase-1 (PDK1) docking site is required for the phosphorylation of protein kinase Czeta (PKCzeta ) and PKC-related kinase 2 by PDK1

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

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

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

The Chk1 protein kinase and the Cdc25C regulatory pathways are targets of the anticancer agent UCN-01

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

PDK1 acquires PDK2 activity in the presence of a synthetic peptide derived from the carboxyl terminus of PRK2.

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

Phosphorylation sites in the autoinhibitory domain participate in p70(s6k) activation loop phosphorylation

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

A highly specific inhibitor of human p38 MAP kinase binds in the ATP pocket

14 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2881806

KRAS wild-type state predicts survival and is associated to early radiological response in metastatic colorectal cancer treated with cetuximab

14 July 2018

1 reference

https://api.crossref.org/works/10.1074%2FJBC.M109.089946

Studies of the mechanism of selectivity of protein tyrosine phosphatase 1B (PTP1B) bidentate inhibitors using molecular dynamics simulations and free energy calculations

21 January 2018

1 reference

https://api.crossref.org/works/10.1074%2FJBC.M109.089946

Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor

21 January 2018

1 reference

https://api.crossref.org/works/10.1074%2FJBC.M109.089946

3,5-Diphenylpent-2-enoic acids as allosteric activators of the protein kinase PDK1: structure-activity relationships and thermodynamic characterization of binding as paradigms for PIF-binding pocket-targeting compounds.

21 January 2018

1 reference

https://api.crossref.org/works/10.1074%2FJBC.M109.089946

21 January 2018

Identifiers

DOI

10.1074/JBC.M109.089946

1 reference

28 July 2017

1 reference

28 July 2017

1 reference