Methods and compositions for bisubstrate inhibitors of...

A - Human Necessities – 61 – K

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A61K 31/40 (2006.01) A61K 31/00 (2006.01) A61K 31/165 (2006.01) A61K 31/4045 (2006.01) A61P 25/00 (2006.01)

Patent

CA 2380798

The present invention provides a method of producing a bisubstrate inhibitor in a cell, comprising introducing into the cell an alkylating derivative of an acetyl acceptor substrate for an acetyltransferase present in the cell. Further provided is a method of inhibiting the activity of an acetyltransferase in a cell, comprising introducing into the cell an alkylating derivative of an acetyl acceptor substrate for an acetyltransferase present in the cell under conditions whereby a bisubstrate inhibitor will be produced, thereby inhibiting the activity of the acetyltransferase in the cell.

L'invention concerne une technique permettant de produire un inhibiteur à deux substrats dans une cellule, qui consiste à introduire dans ladite cellule un dérivé d'alkylation d'un substrat receveur d'acétyle destiné à une acétyltransférase présente dans cette cellule. L'invention concerne également une technique permettant d'inhiber l'activité d'une acétyltransférase dans une cellule, qui consiste à introduire dans ladite cellule un dérivé d'alkylation d'un substrat receveur d'acétyle destiné à une acétyltransférase présente dans cette cellule, dans des conditions permettant de produire un inhibiteur à deux substrat, ce qui permet d'inhiber l'activité de l'acétyltransférase dans la cellule.

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