Structure-based design of a bisphosphonate 5'(3')-deoxyribonucleotidase inhibitor

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22330%2F15%3A43899484" target="_blank" >RIV/60461373:22330/15:43899484 - isvavai.cz</a>
Alternative codes found
RIV/68378050:_____/15:00448427 RIV/61388963:_____/15:00448427
Result on the web
<a href="http://dx.doi.org/10.1039/c5md00235d" target="_blank" >http://dx.doi.org/10.1039/c5md00235d</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1039/c5md00235d" target="_blank" >10.1039/c5md00235d</a>

Result language
angličtina
Original language name
Structure-based design of a bisphosphonate 5'(3')-deoxyribonucleotidase inhibitor
Original language description
Cellular 5'-nucleotidases regulating nucleotide/nucleoside pools are capable of dephosphorylating phosphomonoesters of important nucleoside analogue drugs, thus decreasing their therapeutic efficacy. Based on previously known inhibitor-enzyme complex structures, we developed a promising inhibitor by mimicking the phosphate ion and achieved 50- and 100-fold increases in the inhibitory potency towards cdN and mdN, respectively. Crystal structures of both complexes showed major differences in the inhibitor binding mode towards both enzymes.
Czech name
—
Czech description
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Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
CE - Biochemistry
OECD FORD branch
—

Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2015
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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