Active transport of glutathione S-conjugate in human colon adenocarcinoma cells

Zhang, K; Wong, KP

HERO ID

629594

Reference Type

Journal Article

Year

1996

Language

English

PMID

8950221

HERO ID 629594
In Press No
Year 1996
Title Active transport of glutathione S-conjugate in human colon adenocarcinoma cells
Authors Zhang, K; Wong, KP
Journal Cancer Letters
Volume 108
Issue 1
Page Numbers 143-151
Abstract The formation of the glutathione S-conjugate of monochlorobimane (GSH- bimane) in human colon adenocarcinoma cells was identified by HPLC- fluorimetry and its transport from the cells was found to be temperature-sensitive, saturable and ATP-dependent. The apparent K(m) and Vmax values were 2.4 +/- 0.5 nmol GSH-bimane/10(6) cells and 0.5 +/- 0.1 nmol GSH-bimane/min per 10(6) cells, respectively. This active transport of GSH-bimane was inhibited by low micromolar concentrations of classical uncouplers of oxidative phosphorylation, namely carbonylcyanide p-trifluoromethoxyphenylhydrazone (FCCP), carbonylcyanide m-chlorophenylhydrazone (CCCP) and 2,4-dinitrophenol (DNP). The efflux of GSH-bimane was competitively inhibited by chlorambucil (CMB) and 1-chloro-2,4-dinitrobenzene (CDNB), two other substrates of GST. This study demonstrates the presence and kinetic measurements of the glutathione S-conjugate export (GS-X) pump in human colon cancer cells, an export pump whose function has been implicated in the phenomenon of multidrug resistance.
Doi 10.1016/S0304-3835(96)04457-6
Pmid 8950221
Wosid WOS:A1996VU65500020
Is Certified Translation No
Dupe Override No
Comments Scopus URL: https://www.scopus.com/inward/record.uri?eid=2-s2.0-0030581607&doi=10.1016%2fS0304-3835%2896%2904457-6&partnerID=40&md5=c2e8d1a5df67bf279882726c1d67f7c2
Is Public Yes
Language Text English
Keyword Glutathione S-conjugate pump; Human colon cancer cells; Monochlorobimane; Chlorambucil; Glutathione S-transferase
Is Qa No