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Small molecule inhibitors of RAS-effector protein interactions derived using an intracellular antibody fragment

Abstract:

Targeting specific protein-protein interactions (PPIs) is an attractive concept for drug development, but hard to implement since intracellular antibodies do not penetrate cells and most small-molecule drugs are considered unsuitable for PPI inhibition. A potential solution to these problems is to select intracellular antibody fragments to block PPIs, use these antibody fragments for target validation in disease models and finally derive small molecules overlapping the antibody-binding site. ...

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

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Publisher copy:
10.1038/s41467-018-05707-2

Authors


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Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
RDM; Weatherall Insti. of Molecular Medicine
More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
RDM; Weatherall Insti. of Molecular Medicine
ORCID:
0000-0001-5937-4101
More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
RDM; Weatherall Insti. of Molecular Medicine
More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
RDM; Weatherall Insti. of Molecular Medicine
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Grant:
100842/Z/12/Z
099246/Z/12/Z
Publisher:
Springer Nature Publisher's website
Journal:
Nature Communications Journal website
Volume:
9
Pages:
Article: 3169
Publication date:
2018-08-09
Acceptance date:
2018-07-18
DOI:
EISSN:
2041-1723
ISSN:
2041-1723
Pubs id:
pubs:905387
URN:
uri:48753db5-3859-408e-9c03-781d78d6d0f9
UUID:
uuid:48753db5-3859-408e-9c03-781d78d6d0f9
Local pid:
pubs:905387
Language:
English

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