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National Repository of Grey Literature 1 records found  Search took 0.00 seconds. 
Bi-substrate inhobitors of human pyrimidine 5’-nucleosidases
 Šimák, Ondřej ; Pachl, Petr ; Jandušík, T. ; Brynda, Jiří ; Buděšínský, Miloš ; Rosenberg, Ivan
The work is aimed at the synthesis of bi-substrate inhibitors of 5’-nucleosidases. The pyrimidine nucleobase of lead compound was derivatized in the 5-position with various phosphonic acids differing in conformational flexibility and in the length of alkyl side chain carrying phosphonate group. The phosphonic acid with optimal linker can reach the phosphate binding side and make strong interaction with the enzyme. Inhibition activity of such inhibitors and crystal structure of inhibitor-enzyme complex will be presented.
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