It is an monocarboxylate transporter 1 (MCT1) inhibitors,MCT1 mediates lactate uptake. AZD-3965 is currently being evaluated in phase I/II clinical trials.
参考文献如下:
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 7–10. Biochem J 2010; 425:523-30; PMID:19929853; https://dx.doi.org/10.1042/BJ20091515,
实验性抗癌药物吧?这个难度有点大,属于商业机密吧
很明显,这个是商业机密,有可能涉及到10亿美刀研发经费的问题,如果有人告诉你这个结构式,就涉及违法,要坐牢的
It is an monocarboxylate transporter 1 (MCT1) inhibitors,MCT1 mediates lactate uptake. AZD-3965 is currently being evaluated in phase I/II clinical trials.
AZD-3965 是一个最近被阿斯利康有限公司(世界第四大制药公司)研制开发的一个抗肿瘤新药,靶点是MCT1。目前在临床II期试验阶段。
参考文献如下:
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 7–10. Biochem J 2010; 425:523-30; PMID:19929853; https://dx.doi.org/10.1042/BJ20091515,