Thyroid hormone export in rat FRTL-5 thyroid cells and mouse NIH-3T3 cells is carrier-mediated, verapamil-sensitive, and stereospecific

Endocrinology. 1999 Nov;140(11):4948-54. doi: 10.1210/endo.140.11.7127.

Abstract

Export of L-T3 out of the cell is one factor governing the cellular T3 content and response. We previously observed in liver-derived cells that T3 export was inhibited by verapamil, suggesting that it is due to either ATP-binding cassette/multidrug resistance (MDR1/mdr1b) or multidrug resistance-related (MRP1/mrp1) proteins. To test this hypothesis we measured T3 export in FRTL-5, NIH-3T3, and rat hepatoma (HTC) cells that varied in expression of these proteins. FRTL-5 and NIH-3T3 cells were found to contain a T3 efflux mechanism that is verapamil inhibitable, saturable, and stereospecific. By contrast, T3 efflux in HTC cells was slow and unaffected by verapamil. Neither FRTL-5 nor NIH-3T3 cells express mdrlb, but all three cell types express mrpl, as assessed by immunoblotting. Overexpression of MDR1 in NIH-3T3 cells did not enhance verapamil-inhibitable T3 efflux. Photoaffinity labeling of FRTL-5 and NIH-3T3 cells with [125I]L-T3 revealed a labeled 90- to 100-kDa protein that was not present in HTC cells. Verapamil and excess nonradioactive L-T3, but not D-T3, inhibited labeling of this protein. The lack of correlation between T3 efflux and MDR1 and mrpl expression and the finding of a photoaffinity-labeled putative transport protein smaller than MDR1 or mrp1 protein (approximately 170 kDa) suggest that a novel protein is involved in the transport of T3 out of cells.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • 3T3 Cells
  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / genetics
  • ATP-Binding Cassette Transporters / genetics
  • Animals
  • Biological Transport
  • Calcium Channel Blockers / pharmacology*
  • Carrier Proteins / metabolism*
  • Cell Line
  • Gene Expression
  • Immunoblotting
  • Liver Neoplasms, Experimental / metabolism
  • Mice
  • Multidrug Resistance-Associated Proteins
  • Photoaffinity Labels
  • Rats
  • Thyroid Gland / metabolism*
  • Triiodothyronine / metabolism*
  • Verapamil / pharmacology*

Substances

  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • ATP-Binding Cassette Transporters
  • Calcium Channel Blockers
  • Carrier Proteins
  • Multidrug Resistance-Associated Proteins
  • Photoaffinity Labels
  • Triiodothyronine
  • Verapamil