alpha-Cl-alpha-Br-phosphonoacetic acid is a potent and selective inhibitor of Na+/Pi cotransport across renal cortical brush border membrane.
alpha-Cl-alpha-Br-phosphonoacetic acid is a potent and selective inhibitor of Na+/Pi cotransport across renal cortical brush border membrane.
复制标题
α-Cl-α-Br-膦酰乙酸是一种有效的、选择性的 Na /Pi 跨肾皮质刷状缘膜共转运抑制剂。
DOI：
10.1016/s0006-291x(88)81348-2
复制
发表时间：
1988
影响因子：
3.1
通讯作者：
Dousa,TP
中科院分区：
文献类型：
--
作者：
Hoppe,A;McKenna,CE;Harutunian,V;Levy,JN;Dousa,TP
We found that α-Cl-α-Br-phosphonoacetate (ClBrPAA) is a competitive, solute-specific inhibitor of Na+/Pi cotransport across renal cortical brush border membrane. Inhibition by ClBrPAA (Ki = 62 μM) is more than three times more effective than inhibition by phosphonoformate (PFA), the most potent Na+/Pi cotransport inhibitor known to date, and 26 times more effective than the parent compound, phosphonoacetate (PAA). These observations indicate that substitution of bromine and chlorine atoms at the α-carbon of PAA greatly enhances its efficacy as a competitive inhibitor of Na+/Pi cotransport. As ClBrPAA is much less inhibitory than PAA and PFA towards viral DNA polymerases and did not inhibit human α-DNA polymerase (ref. 10), the results also demonstrate that Na+/Pi cotransport inhibition can be dissociated from inhibition of DNA polymerases by phosphonocarboxylate compounds.
