Mechanism of antineoplastic activity of lonidamine

详细信息    查看全文

• 作者：Kavindra Nath^a ; ^{kavindra.nath@uphs.upenn.edu} ; Lili Guo^b ; Bethany Nancolas^c ; David S. Nelson^a ; Alexander A. Shestov^a ; Seung-Cheol Lee^a ; Jeffrey Roman^a ; Rong Zhou^a ; Dennis B. Leeper^d ; Andrew P. Halestrap^c ; Ian A. Blair^b ; Jerry D. Glickson^a
• 关键词：LND ; lonidamine ; MIBG ; meta-iodobenzyl guanidine ; FCCP ; carbonyl cyanide 4-(trifluoromethoxy) phenylhydrazone ; GSH ; glutathione ; ROS ; reactive oxygen species ; SDH ; succinate dehydrogenase ; SQR ; succinate-ubiquinone reductase ; TCA ; tricarboxylic acid ; TTFA ; 4 ; 4 ; 4-trifluoro-1-(2-thienyl)-1 ; 3-butanedione ; QH2 ; ubiquinone dihydride ; NAD ; nicotinamide adenine dinucleotide ; FAD ; flavin adenine dinucleotide ; MRS ; magnetic resonance spectroscopy ; MCT ; monocarboxylate transporter ; MPC ; mitochondrial pyru
• 刊名：Biochimica et Biophysica Acta (BBA) - Reviews on Cancer
• 出版年：2016
• 出版时间：December 2016
• 年：2016
• 卷：1866
• 期：2
• 页码：151-162
• 全文大小：1123 K
• 卷排序：1866

文摘

Mitochondrial pyruvate carrier (MPC) has highest affinity for lonidamine (LND). Followed by monocarboxylate transporters (MCTs) with MCT1, MCT2 and MCT4 Inhibition of the MPC and MCTs is essential for lowering intracellular pH (pHi). Inhibition of the MPC may suffice to produce tumor de-energization. De-energization also involves inhibition of the ETC (Electron Transport Chain).