A glycosyltransferase inhibitor from a molecular fragment library simultaneously interferes with metal ion and substrate binding

Rene Jørgensen*, Lena Lisbeth Grimm, Nora Sindhuwinata, Thomas Peters, Monica M. Palcic

*Corresponding author

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review


A fragmented approach: 3-Phenyl-5-piperazino-1,2,4-thiadiazole (designated "compound382" in the Ro5 Maybridge Fragment Library, see scheme) is demonstrated to be an effective inhibitor of human blood group glycosyltransferaseB. The compound interferes with both acceptor and donor binding and also displaces the Mn 2+ ion in the binding pocket.

TidsskriftAngewandte Chemie - International Edition
Udgave nummer17
Sider (fra-til)4171-4175
Antal sider5
StatusUdgivet - 23 apr. 2012
Udgivet eksterntJa

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