The equilibrium and kinetic drug binding properties of the mouse P-gp1a and P-gp1b P-glycoproteins are similar
1999

Comparing Drug Binding in Mouse P-glycoproteins

publication

Author Information

Author(s): Taylor J C, Ferry D R, Higgins C F, Callaghan R

Primary Institution: Nuffield Department of Clinical Biochemistry & Cellular Science, University of Oxford

Hypothesis

The study investigates the biochemical differences in drug binding properties between mouse P-gp1a and P-gp1b isoforms.

Conclusion

The mouse P-gp1a and P-gp1b isoforms do not show significant functional differences in drug binding.

Supporting Evidence

  • The study found no detectable difference in the affinity or binding capacity of the two isoforms towards [3H]vinblastine.
  • The rate of association of [3H]vinblastine with P-gp was similar for both isoforms.
  • Modest differences were noted in the ability of certain agents to displace [3H]vinblastine binding.

Takeaway

The two types of P-glycoproteins in mice work similarly when it comes to binding drugs, even though they are found in different tissues.

Methodology

The study measured the affinity and binding capacity of the P-gp isoforms towards [3H]vinblastine and assessed the displacement by various agents.

Digital Object Identifier (DOI)

10.1038/sj.bjc.6690764

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