Intermediates and enzymes of the non-mevalonate isoprenoid...

C - Chemistry – Metallurgy – 12 – N

Patent

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C12N 9/16 (2006.01) A61K 31/045 (2006.01) C07C 33/025 (2006.01) C07F 9/09 (2006.01) C07F 9/113 (2006.01) C07H 19/10 (2006.01) C12N 5/00 (2006.01) C12N 9/02 (2006.01) C12N 15/52 (2006.01) C12N 15/53 (2006.01) C12N 15/55 (2006.01) C12P 9/00 (2006.01) C12Q 1/34 (2006.01) C07B 61/00 (2006.01)

Patent

CA 2443874

The invention provides a protein in a form that is functional for the enzymatic conversion of 2C-methyl-D-erythritol 2,4-cyclodiphosphate to 1- hydroxy-2-methyl-2-butenyl 4-diphosphate notably in its (E)-form of the non- mevalonate biosynthetic pathway to isoprenoids. The invention also provides a protein in a form that is functional for the enzymatic conversion of 1-hydroxy- 2-methyl-2butenyl 4-diphosphate, notably in its (E)-form, to isopentenyl diphosphate and/or dimethylallyl diphosphate. Further, screening methods for inhibitors of these proteins are provided. Further, 1-hydroxy-2-methyl-2- butenyl 4-diphosphate is provided and chemical and enzymatic methods of its preparation.

L'invention concerne une protéine se présentant sous une forme fonctionnelle pour la conversion enzymatique de 2 C -méthyl-D-érythritol 2,4-cyclodiphosphate en 1-hydroxy-2-méthyl-2-butényl 4-diphosphate, notamment sous sa forme ( E ), de la voie biosynthétique non mévalonate des isoprénoïdes. L'invention concerne également une protéine se présentant sous une forme fonctionnelle pour la conversion enzymatique de 1-hydroxy-2-méthyl-2-butényl 4-diphosphate, notamment sous sa forme ( E</i>), en isopentényl diphosphate et/ou diméthylallyl diphosphate. L'invention concerne en outre des méthodes de criblage d'inhibiteurs de ces protéines. L'invention concerne enfin le 1-hydroxy-2-méthyl-2-butényl 4-diphosphate, ainsi que des procédés chimiques et enzymatiques de préparation de celui-ci.

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