Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. (Q35560868)

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29 February 2020

title

Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen (English)

1 reference

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29 February 2020

1 reference

ChEBI release 2020-05-28

23

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29 February 2020

Florence Raynaud

27

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29 February 2020

Paul A Clarke

28

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29 February 2020

26

Felix Rohdich

1 reference

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29 February 2020

author name string

Aurélie Mallinger

1

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29 February 2020

Simon Crumpler

2

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29 February 2020

Mark Pichowicz

3

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29 February 2020

Dennis Waalboer

4

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29 February 2020

Mark Stubbs

5

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29 February 2020

Olajumoke Adeniji-Popoola

6

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29 February 2020

Bozena Wood

7

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29 February 2020

Elizabeth Smith

8

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29 February 2020

Ching Thai

9

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29 February 2020

Alan T Henley

10

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29 February 2020

Katrin Georgi

11

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29 February 2020

William Court

12

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29 February 2020

Steve Hobbs

13

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29 February 2020

Gary Box

14

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29 February 2020

Maria-Jesus Ortiz-Ruiz

15

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29 February 2020

Melanie Valenti

16

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29 February 2020

Alexis De Haven Brandon

17

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29 February 2020

Robert TePoele

18

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29 February 2020

Birgitta Leuthner

19

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29 February 2020

Wynne Aherne

21

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29 February 2020

Oliver Poeschke

22

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29 February 2020

Dirk Wienke

24

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29 February 2020

Christina Esdar

25

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29 February 2020

Suzanne A Eccles

29

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29 February 2020

Frank Stieber

30

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29 February 2020

Kai Schiemann

31

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29 February 2020

Julian Blagg

32

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29 February 2020

Paul Workman

20

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29 February 2020

language of work or name

English

0 references

publication date

13 February 2015

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:25680029%20AND%20SRC:MED&resulttype=core&format=json

Journal of Medicinal Chemistry

29 February 2020

published in

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29 February 2020

volume

58

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29 February 2020

page(s)

1717-1735

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29 February 2020

issue

4

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Bioactivation potential of thiophene-containing drugs.

29 February 2020

cites work

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Can we safely target the WNT pathway?

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Biotransformation and bioactivation reactions of alicyclic amines in drug molecules

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Development of novel dual binders as potent, selective, and orally bioavailable tankyrase 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=4767141

Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974.

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Tankyrases as drug targets

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

A novel tankyrase small-molecule inhibitor suppresses APC mutation-driven colorectal tumor growth.

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Wnt pathway inhibition via the targeting of Frizzled receptors results in decreased growth and tumorigenicity of human tumors

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

A useful approach to identify novel small-molecule inhibitors of Wnt-dependent transcription

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Targeting Wnt signaling: can we safely eradicate cancer stem cells?

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Rap1 stabilizes beta-catenin and enhances beta-catenin-dependent transcription and invasion in squamous cell carcinoma of the head and neck

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Wnt/beta-catenin signaling: components, mechanisms, and diseases

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Proximal events in Wnt signal transduction

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Wnt pathway aberrations including autocrine Wnt activation occur at high frequency in human non-small-cell lung carcinoma

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and 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=4767141

The potential for targeting oncogenic WNT/beta-catenin signaling in therapy.

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

The first five years of the Wnt targetome

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Wnt/beta-catenin/CBP signaling maintains long-term murine embryonic stem cell pluripotency

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Mining the Wnt pathway for 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=4767141

Theoretical prediction of relative and absolute pKa values of aminopyridines.

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Cadherins and catenins in breast 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=4767141

Wnt/beta-catenin signaling pathway as a novel cancer drug target

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

A small molecule inhibitor of beta-catenin/CREB-binding protein transcription [corrected]

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

The beta-catenin/TCF-4 complex imposes a crypt progenitor phenotype on colorectal cancer cells

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Linking colorectal cancer to Wnt 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=4767141

Development of a bicistronic vector driven by the human polypeptide chain elongation factor 1alpha promoter for creation of stable mammalian cell lines that express very high levels of recombinant proteins

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Mutational analysis of the APC/beta-catenin/Tcf pathway in colorectal 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=4767141

The APC gene product in normal and tumor cells

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Inactivation of both APC alleles in human and mouse tumors

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Closed- and open-state binding of 4-aminopyridine to the cloned human potassium channel Kv1.5.

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

2-[[(4-Amino-2-pyridyl)methyl]sulfinyl]benzimidazole H+/K+-ATPase inhibitors. The relationship between pyridine basicity, stability, and activity

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Effect of cathepsin K inhibitors on bone resorption

12 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4767141

Proof-of-principle: oncogenic beta-catenin is a valid molecular target for the development of pharmacological inhibitors

26 September 2018

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/25680029

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1021/JM501436M

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:25680029%20AND%20SRC:MED&resulttype=core&format=json

29 February 2020

1 reference

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29 February 2020

1 reference

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