Evidence for a single class of thrombin-binding sites of human platelets

Biochemistry. 1976 May 18;15(10):2144-9. doi: 10.1021/bi00655a018.

Abstract

We previously demonstrated that human platelets bind a small number of thrombin molecules with high affinity and a larger number with relatively lower affinity (Tollefsen, D. M., Feagler, J. R., and Majerus, P. W. (1974), J. Biol. Chem. 249, 2646). In the present report, equilibrium binding studies using [125I]DIP-thrombin (diisopropylphosphoryl-thrombin) over the range of 0.0002-10 U/ml yield a Hill coefficient of 0.775. Measurements of the rate of dissociation of [125I]DIP-thrombin bound to platelets at relatively high affinity (0.04 U/ml added) indicate a much faster dissociation in the presence of 14 U/ml unlabeled DIP-thrombin (T 1/2 = 1.0 min) than in its absence (T 1/2 - 140 min). [125I]DIP-thrombin bound at low affinity (1.0U/ml added) dissociates from platelets with a T 1/2 = 1.7 min in the absence of unlabeled DIP-thrombin. These results suggest a negative cooperative interaction among receptor sites for thrombin; i.e., as thrombin binds to unoccupied sites, high-affinity receptors are apparently converted to low-affinity receptors. In an attempt to detect whether there is heterogeneity of thrombin receptors, [125I]DIP-thrombin was covalently cross-linked to intact platelets using 1 mM glutaraldehyde. A single complex (apparent molecular weight, 200 000) containing [125I]DIP-thrombin was formed throughout a range of thrombin concentrations in which both high- and low-affinity binding was observed. Since incorporation of [125I]DIP-thrombin into this complex did not occur in the absence of platelets and was inhibited by unlabeled thrombin, the complex may represent thrombin cross-linked to its receptor. We conclude that a single class of receptor sites can account for both high- and low-affinity binding of thrombin to platelets, although interaction between nonidentical sites cannot be excluded.

Publication types

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

MeSH terms

  • Binding Sites
  • Blood Platelets / metabolism*
  • Glutaral
  • Humans
  • Kinetics
  • Macromolecular Substances
  • Protein Binding
  • Thrombin / metabolism*

Substances

  • Macromolecular Substances
  • Thrombin
  • Glutaral