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Asymmetric synthesis and affinity of potent sialyltransferase inhibitors based on transition-state analogues

✍ Scribed by Danielle Skropeta; Ralf Schwörer; Tobias Haag; Richard R. Schmidt

Book ID
111583748
Publisher
Springer US
Year
2004
Tongue
English
Weight
321 KB
Volume
21
Category
Article
ISSN
1573-4986

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Enzymatic sialyl transfer with CMP-Neu5Ac as donor can be inhibited by CDP. Therefore phosphonates 1 a,b, 2 and 3 were synthesized as substrate analogues. With a(2 ± 6)-sialyltransferase from rat liver (EC 2.4.99.1) only moderate inhibition was found for these compounds. In order to obtain transitio