When theory meets experiment: the PD-1 challenge

J Mol Model. 2017 Oct 10;23(11):308. doi: 10.1007/s00894-017-3482-x.

Abstract

Applying atomistic computational modeling to drug discovery has proven to be a hugely successful approach, allowing drug-receptor interactions to be predicted and drugs to be optimized for potency, selectivity, and safety. However, when it comes to predicting protein-protein interactions and to rationally designing regulators of these interactions, computational tools often fail. Here, we report one of the rare instances where state-of-the-art computer simulations, guided by experiment, were able to correctly predict one of the most sophisticated protein-protein interactions. We revisit our previous discovery of the complex of human PD-1 with the ligand PD-L1 and compare our earlier findings with the recently published crystal structure of the same complex. Side-by-side comparison of the model of the complex with its crystal structure reveals outstanding agreement and suggests that our protein-protein prediction workflow could be applied to similar problems.

Keywords: Protein–protein docking; Protein–protein interactions; ZDOCK; hPD-1/hPD-L1.

MeSH terms

  • B7-H1 Antigen / chemistry
  • B7-H1 Antigen / metabolism*
  • Computational Biology / methods
  • Computer Simulation*
  • Drug Discovery / methods*
  • Humans
  • Ligands
  • Models, Molecular*
  • Programmed Cell Death 1 Receptor / chemistry
  • Programmed Cell Death 1 Receptor / metabolism*
  • Protein Interaction Mapping / methods*

Substances

  • B7-H1 Antigen
  • CD274 protein, human
  • Ligands
  • PDCD1 protein, human
  • Programmed Cell Death 1 Receptor