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Structural and functional characterization of a DARPin which inhibits Ras nucleotide exchange

Abstract:

Ras mutations are the oncogenic drivers of many human cancers and yet there are still no approved Ras-targeted cancer therapies. Inhibition of Ras nucleotide exchange is a promising new approach but better understanding of this mechanism of action is needed. Here we describe an antibody mimetic, DARPin K27, which inhibits nucleotide exchange of Ras. K27 binds preferentially to the inactive Ras GDP form with a Kd of 4 nM and structural studies support its selectivity for ...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1038/ncomms16111

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Institution:
University of Oxford
Division:
MSD
Department:
RDM
Role:
Author
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Publisher:
Nature Publishing Group Publisher's website
Journal:
Nature Communications Journal website
Volume:
8
Pages:
16111 (2017)
Publication date:
2017-07-14
Acceptance date:
2017-05-30
DOI:
EISSN:
2041-1723
Pmid:
28706291
Source identifiers:
709275
Language:
English
Keywords:
Pubs id:
pubs:709275
UUID:
uuid:6542179d-9e74-475b-af49-d00004fa38cf
Local pid:
pubs:709275
Deposit date:
2017-09-20

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