Modulation of enzymatic structure, activity, and/or...

Details Modulation of enzymatic structure, activity, and/or... Modulation of enzymatic structure, activity, and/or...

A - Human Necessities

61

K

A61K 31/19 (2006.01) A61K 31/385 (2006.01) A61P 35/00 (2006.01) C12N 9/02 (2006.01) C12N 9/12 (2006.01) C12N 9/16 (2006.01) C12Q 1/00 (2006.01) C12Q 1/32 (2006.01) G01N 33/48 (2006.01)

Patent

CA 2717511

A pharmaceutically-acceptable modulator of the structure, activity, or expression level of an enzyme complex, such as the pyruvate dehydrogenase (PD) complex, in the mitochondria of warm-blooded ani-mals, including humans, and methods of use thereof, comprises an effective amount of at least one lipoic acid derivative and at least one pharma-ceutically-acceptable carrier thereof. By preventing the detoxification of toxic metabolites of anaerobic glycolysis through inhibition of the activity of the PD complex E1.alpha. subunit, the modulator increases PD kinase activity and concomitantly decreases PD phosphatase activity, obliging increased oxidative phosphorylation activity in the mitochondrion. As a cell charac-terized by hyperprolif eration, such as a tumor cell, cannot also generate acetyl-CoA and NADH because of the action of the modulator in inhibiting the action of the E2 subunit of the PD complex, the mitochondrial mem-brane polarization is lost, facilitating cell death.

Un modulateur pharmaceutiquement acceptable de la structure, de lactivité ou du taux dexpression dun complexe enzymatique, par exemple le complexe de pyruvate déshydrogénase (PD), dans les mitochondries des animaux à sang chaud, y compris lhomme, et ses procédés dutilisation, comprend une quantité efficace dau moins un dérivé de lacide lipoïque et dau moins un vecteur pharmaceutiquement acceptable de celui-ci. En empêchant la détoxication de métabolites toxiques de la glycolyse anaérobie par inhibition de lactivité de la sous-unité Ela du complexe PD, le modulateur augmente lactivité kinase de la PD et réduit simultanément lactivité phosphatase de la PD, obligeant un accroissement de lactivité de la phosphorylation oxydative dans la mitochondrie. Comme une cellule caractérisée par une hyperprolifération, par exemple une cellule tumorale, ne peut pas générer lacétyl-CoA et le NADH à cause de laction du modulateur qui inhibe laction de la sous-unité E2 du complexe PD, la polarisation de la membrane mitochondriale est perdue, ce qui facilite la mort de la cellule.

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