Christopher Sean Esslinger,Michael P. Kavanaugh,Brent Lyda,Nicholas R. Natale
申请号：
US14515103
公开号：
US20150056138A1
申请日:
2014.10.15
申请国别(地区):
US
年份:
2015
代理人:
摘要：
The invention features compounds and methods relating to hydroxy-proline analog inhibitors of the ASCT1 and ASCT2 neutral amino acid transporters useful for diagnostic purposes. These analogs are potent and selective inhibitors of ASCT2 and ASCT1-mediated amino acid transport as evidenced by significantly reduced glutamine or alanine transport-associated currents or radiolabeled substrate (amino acid) uptake in Xenopus oocytes expressing ASCT2 or ASCT1. Selectivity has been established in the same manner whereby reduced substrate associated current or substrate uptake is unobserved in Xenopus oocytes expressing ATA2, SN1, or EAAT(s) (excitatory amino acid transporter). The compounds and methods of the invention include radiolabeled inhibitors that can be used in research or clinical applications (e.g., for the treatment of cancer or ischemia-related central nervous system injury).
