Calyculin A modulates the kinetic constants for the Na+-coupled taurine transport in Ehrlich ascites tumour cells

Biochim Biophys Acta. 1998 May 28;1371(2):335-44. doi: 10.1016/s0005-2736(98)00033-9.

Abstract

The effect of the phosphatase inhibitor calyculin A (cal A) on the kinetic parameters of the Na+-coupled taurine uptake via the taurine transporter in the Ehrlich ascites tumour cells has been investigated. Preincubation with cal A (100 nM) reduces the initial taurine influx by about 20%, but has no effect on the diffusional component of the taurine influx or on the taurine release from cells suspended in isotonic or in hypotonic medium. Thus, cal A-sensitive phosphatases only affect taurine transport mediated by the Na+-dependent taurine transporter. Cal A increases the Michaelis-Menten constant for binding of taurine to the transporter from 31+/-6 to 45+/-4 microM and reduces the taurine transport capacity from 210+/-20 to 170+/-10 nmol x g dry wt(-1) x min(-1) [corrected]. The Michaelis-Menten constant for binding of Na+ to the taurine transporter is concomitantly increased from 96+/-11 to 129+/-8 mM and the Na+:taurine coupling ratio for activation of the transport cycle is reduced from 3.3+/-0.6 to 2.4+/-0.2. This suggests that cal A-sensitive phosphatases maintain a high affinity of the taurine transporter towards Na+ and taurine as well as a high taurine transport capacity in unpertubated Ehrlich cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Biological Transport / drug effects
  • Carbon Radioisotopes
  • Carcinogens / pharmacology
  • Carcinoma, Ehrlich Tumor / enzymology
  • Carcinoma, Ehrlich Tumor / metabolism*
  • Carrier Proteins / metabolism*
  • Cell Size / drug effects
  • Female
  • Kinetics
  • Marine Toxins
  • Membrane Glycoproteins / metabolism*
  • Membrane Transport Proteins*
  • Mice
  • Oxazoles / pharmacology*
  • Phosphoprotein Phosphatases / antagonists & inhibitors
  • Sodium / metabolism*
  • Taurine / metabolism*
  • Tumor Cells, Cultured

Substances

  • Carbon Radioisotopes
  • Carcinogens
  • Carrier Proteins
  • Marine Toxins
  • Membrane Glycoproteins
  • Membrane Transport Proteins
  • Oxazoles
  • taurine transporter
  • Taurine
  • calyculin A
  • Sodium
  • Phosphoprotein Phosphatases