C - Chemistry – Metallurgy – 12 – N
Patent
C - Chemistry, Metallurgy
12
N
C12N 9/99 (2006.01) A01N 43/40 (2006.01) A61K 38/00 (2006.01) A61K 45/00 (2006.01) C12N 9/10 (2006.01) C12N 9/12 (2006.01) G01N 31/00 (2006.01)
Patent
CA 2320228
General methods for monitoring the activity of MurG, a GlcNAc transferase involved in bacterial cell wall biosynthesis, is disclosed. More particularly, the synthesis of simplified substrate analogs of Lipid I (the natural substrate for MurG), which function as acceptors for UDP-GlcNAc in an enzymatic reaction catalyzed by MurG, is described. Assays using the substrate analogs of the invention are further disclosed, which are useful for identifying a variety of other substrates, including inhibitors of MurG activity, for facilitating mechanistic and/or structural studies of the enzyme and for other uses. High throughput assays are also described.
La présente invention concerne des procédés généraux permettant de surveiller l'activité de la MurG, une GlcNAc transférase impliquée dans la biosynthèse de la paroi cellulaire bactérienne. L'invention concerne en particulier la synthèse d'analogues simplifiés du substrat "lipide 1" (le substrat naturel de la MurG), qui fonctionnent comme accepteurs de l'UDP-GlcNAc dans une réaction enzymatique catalysée par la MurG. L'invention se rapporte également à des analyses faisant appel aux analogues de substrat précités, qui sont utilisés pour identifier plusieurs autres substrats, y compris des inhibiteurs de l'activité de la MurG, pour faciliter les études mécanistes et/ou structurelles de l'enzyme et dans d'autres applications. L'invention se rapporte enfin à des analyses à haut rendement.
Ge Min
Kahne Suzanne Walker
Men Hongbin
Park Peter
Princeton University
Robic
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