Structure-activity relationship study of small-molecule inhibitor of Atg12-Atg3 protein-protein interaction
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F24%3A00598057" target="_blank" >RIV/61388963:_____/24:00598057 - isvavai.cz</a>
Alternative codes found
RIV/60461373:22330/24:43929822
Result on the web
<a href="https://doi.org/10.1016/j.bmcl.2024.129939" target="_blank" >https://doi.org/10.1016/j.bmcl.2024.129939</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.bmcl.2024.129939" target="_blank" >10.1016/j.bmcl.2024.129939</a>
Alternative languages
Result language
angličtina
Original language name
Structure-activity relationship study of small-molecule inhibitor of Atg12-Atg3 protein-protein interaction
Original language description
Autophagy is a catabolic process that was described to play a critical role in advanced stages of cancer, wherein it maintains tumor cell homeostasis and growth by supplying nutrients. Autophagy is also described to support alternative cellular trafficking pathways, providing a non-canonical autophagy-dependent inflammatory cytokine secretion mechanism. Therefore, autophagy inhibitors have high potential in the treatment of cancer and acute inflammation. In our study, we identified compound 1 as an inhibitor of the ATG12-ATG3 protein-protein interaction. We focused on the systematic modification of the original hit 1, a casein kinase 2 (CK2) inhibitor, to find potent disruptors of ATG12-ATG3 protein-protein interaction. A systematic modification of the hit structure led us to a wide plethora of compounds that maintain its ATG12-ATG3 inhibitory activity, which could act as a viable starting point to design new compounds with diverse therapeutic applications.
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
10401 - Organic chemistry
Result continuities
Project
<a href="/en/project/EH22_008%2F0004607" target="_blank" >EH22_008/0004607: New Technologies for Translational Research in Pharmaceutical Sciences /NETPHARM</a><br>
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2024
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Bioorganic and Medicinal Chemistry Letters
ISSN
0960-894X
e-ISSN
1464-3405
Volume of the periodical
112
Issue of the periodical within the volume
November
Country of publishing house
GB - UNITED KINGDOM
Number of pages
6
Pages from-to
129939
UT code for WoS article
001309826500001
EID of the result in the Scopus database
2-s2.0-85203245928