Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development (Q39781089)

14 September 2017

Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development (English)

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14 September 2017

16

Robert T Gampe

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14 September 2017

Jeffrey M Axten

1

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14 September 2017

Stuart P Romeril

2

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14 September 2017

Arthur Shu

3

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14 September 2017

Jeffrey Ralph

4

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14 September 2017

Jesús R Medina

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14 September 2017

Yanhong Feng

6

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14 September 2017

William Hoi Hong Li

7

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14 September 2017

Seth W Grant

8

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14 September 2017

Dirk A Heerding

9

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14 September 2017

Elisabeth Minthorn

10

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14 September 2017

Thomas Mencken

11

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14 September 2017

Nathan Gaul

12

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14 September 2017

Aaron Goetz

13

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14 September 2017

Thomas Stanley

14

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14 September 2017

Annie M Hassell

15

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14 September 2017

Charity Atkins

17

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14 September 2017

Rakesh Kumar

18

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14 September 2017

12 August 2013

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ACS Medicinal Chemistry Letters

14 September 2017

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14 September 2017

4

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14 September 2017

10

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14 September 2017

964-968

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PERK is required in the adult pancreas and is essential for maintenance of glucose homeostasis

14 September 2017

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https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027568

The unfolded protein response induces the angiogenic switch in human tumor cells through the PERK/ATF4 pathway

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027568

Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (P

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027568

The unfolded protein response: from stress pathway to homeostatic regulation

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027568

Transcriptional and post-transcriptional regulation of proangiogenic factors by the unfolded protein response

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027568

Transcriptional regulation of VEGF-A by the unfolded protein response pathway

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027568

Cell death and endoplasmic reticulum stress: disease relevance and therapeutic opportunities

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027568

The role of fluorine in medicinal chemistry

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027568

Fluorine in pharmaceuticals: looking beyond intuition

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027568

Signal integration in the endoplasmic reticulum unfolded protein response

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027568

Perk-dependent translational regulation promotes tumor cell adaptation and angiogenesis in response to hypoxic stress

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027568

Activation-dependent substrate recruitment by the eukaryotic translation initiation factor 2 kinase PERK.

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027568

ER stress-regulated translation increases tolerance to extreme hypoxia and promotes tumor growth

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027568

The PERK eukaryotic initiation factor 2 alpha kinase is required for the development of the skeletal system, postnatal growth, and the function and viability of the pancreas

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027568

Diabetes mellitus and exocrine pancreatic dysfunction in perk-/- mice reveals a role for translational control in secretory cell survival

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027568

Pancreatic eukaryotic initiation factor-2alpha kinase (PEK) homologues in humans, Drosophila melanogaster and Caenorhabditis elegans that mediate translational control in response to endoplasmic reticulum stress

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027568

Protein translation and folding are coupled by an endoplasmic-reticulum-resident kinase

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027568

Identification and characterization of pancreatic eukaryotic initiation factor 2 alpha-subunit kinase, PEK, involved in translational control

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027568

Characterization of a novel PERK kinase inhibitor with antitumor and antiangiogenic activity

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027568

Fluorine bonding--how does it work in protein-ligand interactions?

20 August 2018

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PubMed

https://pubmed.ncbi.nlm.nih.gov/24900593

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1021/ML400228E

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release_jwnromo24jgg3mseopbibv3fvy

14 September 2017

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Fatcat

https://api.fatcat.wiki/v0/release/jwnromo24jgg3mseopbibv3fvy

mapped directly with Wikidata item

24 November 2022

based on heuristic

1 reference

14 September 2017

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