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2014 | 19 | 2 |

Tytuł artykułu

Transport of 3 - bromopyruvate across the human erythrocyte membrane

Warianty tytułu

Języki publikacji

EN

Abstrakty

EN
3-Bromopyruvic acid (3-BP) is a promising anticancer compound because it is a strong inhibitor of glycolytic enzymes, especially glyceraldehyde 3-phosphate dehydrogenase. The Warburg effect means that malignant cells are much more dependent on glycolysis than normal cells. Potential complications of anticancer therapy with 3-BP are side effects due to its interaction with normal cells, especially erythrocytes. Transport into cells is critical for 3-BP to have intracellular effects. The aim of our study was the kinetic characterization of 3-BP transport into human erythrocytes. 3-BP uptake by erythrocytes was linear within the first 3 min and pH-dependent. The transport rate decreased with increasing pH in the range of 6.0–8.0. The Km and Vm values for 3-BP transport were 0.89 mM and 0.94 mmol/(l cells x min), respectively. The transport was inhibited competitively by pyruvate and significantly inhibited by DIDS, SITS, and 1-cyano-4-hydroxycinnamic acid. Flavonoids also inhibited 3-BP transport: the most potent inhibition was found for luteolin and quercetin.

Wydawca

-

Rocznik

Tom

19

Numer

2

Opis fizyczny

p.201-214,fig.,ref.

Twórcy

  • Department of Biochemistry and Cell Biology, University of Rzeszow, Zelwerowicza 4, 35-601 Rzeszow, Poland
autor
  • Department of Molecular Biophysics, University of Lodz, Lodz, Poland
  • Institute of Genetics and Microbiology, University of Wroclaw, Wroclaw, Poland
autor
  • KoDiscovery LLC, UM BioPark, Innovation Center, Suites 502 E&F, 801 West Baltimore Street, Baltimore, MD 21201, USA
autor
  • Department of Biochemistry and Cell Biology, University of Rzeszow, Zelwerowicza 4, 35-601 Rzeszow, Poland
  • Department of Molecular Biophysics, University of Lodz, Lodz, Poland

Bibliografia

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Typ dokumentu

Bibliografia

Identyfikatory

Identyfikator YADDA

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