Set-up and screening of a fragment library targeting the 14-3-3 protein interface
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F67985823%3A_____%2F19%3A00511984" target="_blank" >RIV/67985823:_____/19:00511984 - isvavai.cz</a>
Alternative codes found
RIV/00216208:11310/19:10403396
Result on the web
<a href="https://pubs.rsc.org/en/content/articlelanding/2019/MD/C9MD00215D#!divAbstract" target="_blank" >https://pubs.rsc.org/en/content/articlelanding/2019/MD/C9MD00215D#!divAbstract</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1039/c9md00215d" target="_blank" >10.1039/c9md00215d</a>
Alternative languages
Result language
angličtina
Original language name
Set-up and screening of a fragment library targeting the 14-3-3 protein interface
Original language description
Protein-protein interactions (PPIs) are at the core of regulation mechanisms in biological systems and consequently became an attractive target for therapeutic intervention. PPIs involving the adapter protein 14-3-3 are representative examples given the broad range of partner proteins forming a complex with one of its seven human isoforms. Given the challenges represented by the nature of these interactions, fragment-based approaches offer a valid alternative for the development of PPI modulators. After having assembled a fragment set tailored on PPIs' modulation, we started a screening campaign on the sigma isoform of 14-3-3 adapter proteins. Through the use of both mono- and bi-dimensional nuclear magnetic resonance spectroscopy measurements, coupled with differential scanning fluorimetry, three fragment hits were identified. These molecules bind the protein at two different regions distant from the usual binding groove highlighting new possibilities for selective modulation of 14-3-3 complexes.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10608 - Biochemistry and molecular biology
Result continuities
Project
—
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2019
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
MedChemComm
ISSN
2040-2503
e-ISSN
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Volume of the periodical
10
Issue of the periodical within the volume
10
Country of publishing house
GB - UNITED KINGDOM
Number of pages
7
Pages from-to
1796-1802
UT code for WoS article
000490887100008
EID of the result in the Scopus database
2-s2.0-85073786665