Original title: Bi-substrate inhobitors of human pyrimidine 5’-nucleosidases
Authors: Šimák, Ondřej ; Pachl, Petr ; Jandušík, T. ; Brynda, Jiří ; Buděšínský, Miloš ; Rosenberg, Ivan
Document type: Papers
Conference/Event: Symposium on Chemistry of Nucleic Acid Components /16./, Český Krumlov (CZ), 2014-06-08 / 2014-06-13
Year: 2014
Language: eng
Abstract: 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.
Keywords: 5’-nucleosidases; bi-substrate inhibitors; NPAs
Project no.: GA13-26526S (CEP), GA13-24880S (CEP), TA03010719 (CEP)
Funding provider: GA ČR, GA ČR, GA TA ČR
Host item entry: Chemistry of Nucleic Acid Components. 16th Symposium, ISBN 978-80-86241-50-0

Institution: Institute of Organic Chemistry and Biochemistry AS ČR (web)
Document availability information: Fulltext is available at the institute of the Academy of Sciences.
Original record: http://hdl.handle.net/11104/0234531

Permalink: http://www.nusl.cz/ntk/nusl-174779


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Research > Institutes ASCR > Institute of Organic Chemistry and Biochemistry
Conference materials > Papers