Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity (Q27678097)

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26 January 2020

title

Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity (English)

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5

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7

Benjamin P Fauber

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10

David Stokoe

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26 January 2020

author name string

Till Maurer

1

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26 January 2020

Lindsay S Garrenton

2

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Angela Oh

3

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Keith Pitts

4

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Nicholas J Skelton

6

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Borlan Pan

8

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Shiva Malek

9

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Mary J C Ludlam

11

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Krista K Bowman

12

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Jiansheng Wu

13

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Anthony M Giannetti

14

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Melissa A Starovasnik

15

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Ira Mellman

16

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Peter K Jackson

17

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Joachim Rudolph

18

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Weiru Wang

19

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Guowei Fang

20

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language of work or name

English

0 references

publication date

19 March 2012

1 reference

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Proceedings of the National Academy of Sciences of the United States of America

26 January 2020

number of pages

6

1 reference

based on heuristic

inferred from page(s)

published in

1 reference

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volume

109

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issue

14

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26 January 2020

page(s)

5299-5304

1 reference

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Stabilizing a weak binding state for effectors in the human ras protein by cyclen complexes

26 January 2020

cites work

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3325706

Structural evidence for feedback activation by Ras.GTP of the Ras-specific nucleotide exchange factor SOS

20 March 2017

1 reference

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The structural basis of the activation of Ras by Sos

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3325706

The Ras-RasGAP Complex: Structural Basis for GTPase Activation and Its Loss in Oncogenic Ras Mutants

20 March 2017

1 reference

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The 2.2 A crystal structure of the Ras-binding domain of the serine/threonine kinase c-Raf1 in complex with Rap1A and a GTP analogue

20 March 2017

1 reference

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Molecular switch for signal transduction: structural differences between active and inactive forms of protooncogenic ras proteins

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3325706

The guanine nucleotide-binding switch in three dimensions

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3325706

Live-cell microscopy reveals small molecule inhibitor effects on MAPK pathway dynamics

20 March 2017

1 reference

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A Ras-induced conformational switch in the Ras activator Son of sevenless

20 March 2017

1 reference

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Hyperactive Ras in developmental disorders and cancer

20 March 2017

1 reference

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An orthosteric inhibitor of the Ras-Sos interaction

7 April 2017

1 reference

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First experimental identification of Ras-inhibitor binding interface using a water-soluble Ras ligand.

29 September 2017

1 reference

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From fragment to clinical candidate--a historical perspective.

29 September 2017

1 reference

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Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases.

29 September 2017

1 reference

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Sulindac-derived Ras pathway inhibitors target the Ras-Raf interaction and downstream effectors in the Ras pathway

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3325706

Inhibitors of Ras/Raf-1 interaction identified by two-hybrid screening revert Ras-dependent transformation phenotypes in human cancer cells.

29 September 2017

1 reference

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Group epitope mapping by saturation transfer difference NMR to identify segments of a ligand in direct contact with a protein receptor

29 September 2017

1 reference

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Detection and structural characterization of ras oncoprotein-inhibitors complexes by electrospray mass spectrometry

29 September 2017

1 reference

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Ras oncoprotein inhibitors: the discovery of potent, ras nucleotide exchange inhibitors and the structural determination of a drug-protein complex

29 September 2017

1 reference

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Analysis of intrinsic and CDC25-stimulated guanine nucleotide exchange of p21ras-nucleotide complexes by fluorescence measurements

29 September 2017

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/22431598

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Pseudomonas aeruginosa Exoenzyme S ADP-ribosylates Ras at Multiple Sites

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/22431598

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12 December 2020

based on heuristic

Identifiers

DOI

10.1073/PNAS.1116510109

2 references

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26 January 2020

ADS bibcode

2012PNAS..109.5299M

0 references

1 reference

2 references

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26 January 2020

PubMed publication ID

22431598

2 references

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