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BRET-based RAS biosensors that show a novel small molecule is an inhibitor of RAS-effector protein-protein interactions

Abstract:

The RAS family of proteins is amongst the most highly mutated in human cancers and has so far eluded drug therapy. Currently, much effort is being made to discover mutant RAS inhibitors and in vitro screening for RAS-binding drugs must be followed by cell-based assays. Here, we have developed a robust set of bioluminescence resonance energy transfer (BRET)-based RAS biosensors that enable monitoring of RAS-effector interaction inhibition in living cells. These include KRAS, HRAS and NRAS and ...

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Publication status:
Published
Peer review status:
Peer reviewed
Version:
Publisher's Version

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Publisher copy:
10.7554/elife.37122

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Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
Weatherall Insti. of Molecular Medicine
Role:
Author
ORCID:
0000-0002-2643-3897
More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
Weatherall Insti. of Molecular Medicine
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry; Organic Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
Weatherall Insti. of Molecular Medicine
Role:
Author
More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
Weatherall Insti. of Molecular Medicine
Role:
Author
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Publisher:
eLife Sciences Publications Publisher's website
Journal:
eLife Journal website
Volume:
7
Issue:
1
Pages:
e37122
Publication date:
2018-07-10
Acceptance date:
2018-06-16
DOI:
EISSN:
2050-084X
Pubs id:
pubs:867653
URN:
uri:7de0281c-0b57-409e-9ca2-732b667eb9e1
UUID:
uuid:7de0281c-0b57-409e-9ca2-732b667eb9e1
Local pid:
pubs:867653

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