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It is an monocarboxylate transporter 1 (MCT1) inhibitors,MCT1 mediates lactate uptake. AZD-3965 is currently being evaluated in phase I/II clinical trials.
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GOVERN1688: ½ð±Ò+4, ¡ï¡ï¡ï¡ï¡ï×î¼Ñ´ð°¸, лл´óÉñ 2013-08-05 20:58:39
AZD-3965 ÊÇÒ»¸ö×î½ü±»°¢Ë¹Àû¿µÓÐÏÞ¹«Ë¾(ÊÀ½çµÚËÄ´óÖÆÒ©¹«Ë¾)ÑÐÖÆ¿ª·¢µÄÒ»¸ö¿¹Ö×ÁöÐÂÒ©£¬°ÐµãÊÇMCT1¡£Ä¿Ç°ÔÚÁÙ´²IIÆÚÊÔÑé½×¶Î¡£

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1. Bueno V, Binet I, Steger U, Bundick R, Ferguson D, Murray C, et al. The specific monocarboxylate
transporter (MCT1) inhibitor, AR-C117977, a novel immunosuppressant, prolongs allograft survival
in the mouse. Transplantation 2007; 84:1204-7; PMID:17998878; https://dx.doi.org/10.1097/01.
tp.0000287543.91765.41.

2. Ovens MJ, Davies AJ, Wilson MC, Murray CM,Halestrap AP. AR-C155858 is a potent inhibitor
of monocarboxylate transporters MCT1 and MCT2 that binds to an intracellular site involving transmembrane
helices 7¨C10. Biochem J 2010; 425:523-30; PMID:19929853; https://dx.doi.org/10.1042/BJ20091515
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