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Titolo:
CHARACTERIZATION OF THE CATECHOLAMINE EXTRANEURONAL UPTAKE, CARRIER IN HUMAN GLIOMA CELL-LINES SK-MG-1 AND SKI-1 IN RELATION TO (2-CHLOROETHYL)-3-SARCOSINAMIDE-1-NITROSOUREA (SARCNU) SELECTIVE CYTOTOXICITY
Autore:
NOE AJ; MARCANTONIO D; BARTON J; MALAPETSA A; PANASCI LC;
Indirizzi:
SIR MORTIMER B DAVIS JEWISH HOSP,LADY DAVIS INST MED RES,3755 COTE STE CATHERINE RD MONTREAL PQ H3T 1E2 CANADA SIR MORTIMER B DAVIS JEWISH HOSP,LADY DAVIS INST MED RES MONTREAL PQ H3T 1E2 CANADA
Titolo Testata:
Biochemical pharmacology
fascicolo: 12, volume: 51, anno: 1996,
pagine: 1639 - 1648
SICI:
0006-2952(1996)51:12<1639:COTCEU>2.0.ZU;2-P
Fonte:
ISI
Lingua:
ENG
Soggetto:
GUINEA-PIG TRACHEALIS; AMINO-ACID AMIDES; TRANSPORT MECHANISM; MALIGNANT GLIOMAS; NORADRENALINE TRANSPORT; SMOOTH-MUSCLE; O-METHYLATION; CHEMOTHERAPY; INHIBITORS; SARCOSINAMIDE;
Keywords:
CHLOROETHYLNITROSOUREA; GLIOMA; UPTAKE(2); NOREPINEPHRINE; EPINEPHRINE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
47
Recensione:
Indirizzi per estratti:
Citazione:
A.J. Noe et al., "CHARACTERIZATION OF THE CATECHOLAMINE EXTRANEURONAL UPTAKE, CARRIER IN HUMAN GLIOMA CELL-LINES SK-MG-1 AND SKI-1 IN RELATION TO (2-CHLOROETHYL)-3-SARCOSINAMIDE-1-NITROSOUREA (SARCNU) SELECTIVE CYTOTOXICITY", Biochemical pharmacology, 51(12), 1996, pp. 1639-1648

Abstract

Transport of (2-chloroethyl)-3-sarcosinamide-1-nitrosourea (SarCNU) and (-)-norepinephrine was investigated in SarCNU-sensitive SK-MG-1 and-resistant SKI-1 human glioma cell lines. [H-3]SarCNU influx was inhibited by SarCNU, sarcosinamide, and (+/-)-epinephrine in SK-MG-1 cellswith competitive inhibition observed by (+/-)-epinephrine (K-i = 140 /- 12 mu M) and (+/-)-norepinephrine (K-i = 255 +/- 41 mu M). No effect on influx was detected in SKI-1 cells. [H-3](-)-Norepinephrine influx was linear to 15 sec in both cell lines and temperature dependent only in SK-MG-1 cells. Influx of [H-3](-)-norepinephrine was found to be saturable in SK-MG-1 (K-m = 148 +/- 28 mu M, V-max = 1.23 +/- 0.18 pmol/mu L intracellular water/sec) but not in SKI-1 cells. In SK-MG-1 cells, [H-3](-)-norepinephrine influx was found to be inhibited competitively by (-)-epinephrine (K-i = 111 +/- 7 mu M) and SarCNU (K-i = 1.48 +/- 0.22 mM). Ouabain and KCl were able to inhibit the: [H-3]norepinephrine influx in SK-MG-1 cells, consistent with influx being driven by membrane potential. Several catecholamine uptake(2) inhibitors were able to reduce significantly the influx of [H-3](-)-norepinephrine and[H-3]SarCNU with no inhibition by a catecholarnine uptake(2) inhibitor. These findings suggest that increased sensitivity of SK-MG-1 to SarCNU is secondary to enhanced accumulation of SarCNU mediated via the catecholamine extraneuronal uptake(2) transporter, which is not detectable in SKI-1 cells. The introduction of SarCNU into clinical trials will confirm ii increased uptake via the catecholamine extraneuronal uptake(2) transporter will result in increased antitumor activity.

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Documento generato il 16/07/20 alle ore 16:42:29