Computer graphics in drug design: molecular modeling of thyroid hormone-prealbumin interactions

J Med Chem. 1982 Jul;25(7):785-90. doi: 10.1021/jm00349a004.

Abstract

Computer graphics modeling of the thyroxine-prealbumin complex provides a detailed picture of the interactions between thyroxine and prealbumin. A wide variety of thyroid hormone analogue-prealbumin complexes were modeled by calculating the molecular surfaces of the analogues and the prealbumin hormone-binding site. Analogues with high binding affinity were observed to fill more of the hormone-binding site than low-affinity analogues. These surface models described many aspects of the hormone-protein interaction which were not obvious using simple wire models and led us to develop a model which accounts for thyroid hormone-prealbumin structure-activity relationships and ultimately to predict and measure the relative binding affinities of four previously untested thyroid hormone analogues to prealbumin.

Publication types

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

MeSH terms

  • Chemical Phenomena
  • Chemistry, Pharmaceutical
  • Chemistry, Physical
  • Computers
  • Humans
  • Models, Molecular
  • Prealbumin / metabolism*
  • Protein Binding
  • Serum Albumin / metabolism*
  • Structure-Activity Relationship
  • Thyroid Hormones / blood*
  • X-Ray Diffraction

Substances

  • Prealbumin
  • Serum Albumin
  • Thyroid Hormones