Assessment of the low inhibitory specificity of oxamate, aminooxyacetate and dichloroacetate on cancer energy metabolism

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• 作者：Rafael Moreno-Sá ; nchez ; ^{rafael.moreno@cardiologia.org.mx} ; ^{morenosanchez@hotmail.com} ; Á ; lvaro Marí ; n-Herná ; ndez ; Isis Del Mazo-Monsalvo ; Emma Saavedra ; Sara Rodrí ; guez-Enrí ; quez
• 关键词：AAT ; aspartate aminotransferase ; Ala ; alanine ; AlaT ; alanine aminotransferase ; ALD ; aldolase ; AOA ; aminooxyacetate ; Asp ; aspartate ; CS ; citrate synthase ; 2-DOG ; 2-deoxyglucose ; DCA ; dichloroacetate ; DHAP ; dihydroxyacetone phosphate ; ENO ; enolase ; Ery4P ; erythrose-4-phosphate ; FFAs ; free fatty acids ; Fru6P ; fructose-6-phosphate ; Fru1 ; 6BP ; fructose-1 ; 6-bisphosphate ; GAPDH ; glyceraldehyde-3-phosphate dehydrogenase ; Glc6P ; glucose-6-phosphate ; Glc6PDH ; glucose-6-phosphate dehydrogenase ; G3P ; glycera
• 刊名：Biochimica et Biophysica Acta (BBA) - General Subjects
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：1861
• 期：1
• 页码：3221-3236
• 全文大小：1431 K
• 卷排序：1861

文摘

Oxamate, aminooxyacetate (AOA) and dichloroacetate (DCA) are not specific drugs. Oxamate, AOA and DCA inhibit several glycolytic and OxPhos enzymesOxamate inhibition induces Fru1,6BP and DHAP accumulation. High Fru1,6BP and DAHP levels inhibit HK, HPI, TPI and GAPDH activities. Kinetic modeling shows that oxamate must affect several enzymes to block glycolysis.