NBTGR

NBTGR(p-Nitrobenzylthioguanosine)是核苷转运(nucleosidetransport)的有效抑制剂;抑制腺苷摄取的Ki值为70nM。

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Background

NBTGR (p-Nitrobenzylthioguanosine) is a potent inhibitor of nucleoside transport; inhibits adenosine uptake with a Ki of 70 nM.

A group of purine ribonucleosides with alkarylmercapto substituents at the purine 6-position are potent inhibitors of several aspects of nucleoside metabolism that involved the transfer of ribosyl groups. NBTGR is one of the compounds that inhibits nucleoside transport by human erythrocytes; initial rates of uridine uptake are reduced to zero upon exposure of cells to 1 μM NBTGR. The inhibitor is firmly bound because repeated washing cannot restore uridine transport capability to NBTGR-treated cells. NBTGR inhibits the influx of uridine, inosine, and cytidine, without inhibiting the uptake of the corresponding bases, or that of D-glucose or L-leucine. Uridine antagonizes the NBTGR inhibition of uidine transport in a concentration-dependent manner. NBTGR and related compounds appear to interact with the mechanism for the facilitated transport of nucleosides[2].

[1]. Turnheim K, et al. Inhibition of adenosine uptake in human erythrocytes by adenosine-5'-carboxamides, xylosyladenine, dipyridamole, hexobendine, and p-nitrobenzylthioguanosine. Biochem Pharmacol. 1978;27(18):2191-7. [2]. Parterson A, et al. Nucleoside Transport II Inhibition by p-Nitrobeazylthiogoanosine and Related Compounds. Can. J. Biochem. 49,271-274 (1971)