Method for inhibiting adenylosuccinate synthetase activity...

C - Chemistry – Metallurgy – 12 – Q

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C12Q 1/68 (2006.01) A61K 31/195 (2006.01) A61K 31/198 (2006.01) A61P 35/00 (2006.01) C12Q 1/25 (2006.01) G01N 33/50 (2006.01)

Patent

CA 2244733

An in vivo method for depleting mammalian cells of adenosine 5'-monophosphate (AMP) useful in the treatment of certain cancers is provided. According to the method, a population of cells is obtained from a host and assayed for loss of methylthioadenosine phosphorylase (MTAse) activity. MTAse catabolizes methylthioadenosine to adenine for endogenous salvage incorporation into the intracellular AMP pool. The preferred method for assaying loss of MTAse activity is a hybridization technique for detection of a homozygous loss of the gene which encodes with a therapeutically effective amount of an agent which inhibits the activity of adenylsuccinate synthetase, which converts inosine 5'-monophosphate to AMP, thus depleting the tumor cells of substrates for de novo AMP production. L-alanosine is the preferred ASS inhibitory agent for use in the method of the invention. The figure is a nucleotide sequence for genomic MTAse (SEQ. ID. No. 1) wherein the exons are underlined.

L'invention concerne un procédé in vivo de déplétion de cellules mammaliennes de l'adénosine 5' monophosphate (AMP) utile dans le traitement de certains cancers. Selon ce procédé, on prélève chez un hôte une population de cellules et on les analyse en vue de déterminer la perte de l'activité de méthylthioadenosine phosphorylase (MTAse). MTase catabolise méthylthioadenosine en adénine en vue d'incorporer la récupération endogène dans le pool intracellulaire de l'AMP. Le procédé préféré de détermination de la perte de l'activité de MTase est une technique d'hybridation en vue de détecter une perte homozygote du gène codant une quantité thérapeutiquement efficace d'un agent qui inhibe l'activité de l'adénylsuccinate synthétase, convertit l'inosine 5'-monophosphate en AMP, appauvrissant ainsi les cellules tumorales des substrats pour une production de novo de l'AMP. L-alanosine est l'agent inhibiteur préféré de l'adénylsuccinate synthétase (ASS) qui est destinée à être utilisée dans ce procédé. La figure (1) est une séquence nucléotidique pour MTAse génomique (No. ID. SEQ. 1) dans laquelle les exons sont soulignés.

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