Antibody-enabled small-molecule drug discovery

Nat Rev Drug Discov. 2012 Jun 29;11(7):519-25. doi: 10.1038/nrd3756.


Although antibody-based therapeutics have become firmly established as medicines for serious diseases, the value of antibodies as tools in the early stages of small-molecule drug discovery is only beginning to be realized. In particular, antibodies may provide information to reduce risk in small-molecule drug discovery by enabling the validation of targets and by providing insights into the design of small-molecule screening assays. Moreover, antibodies can act as guides in the quest for small molecules that have the ability to modulate protein-protein interactions, which have traditionally only been considered to be tractable targets for biological drugs. The development of small molecules that have similar therapeutic effects to current biologics has the potential to benefit a broader range of patients at earlier stages of disease.

Publication types

  • Review

MeSH terms

  • Animals
  • Antibodies, Monoclonal / chemistry*
  • Crystallography, X-Ray
  • Drug Delivery Systems / methods
  • Drug Discovery / methods*
  • Drug Discovery / trends
  • Humans
  • Immunoglobulin Fab Fragments / chemistry*
  • Muromonab-CD3 / chemistry
  • Reproducibility of Results


  • Antibodies, Monoclonal
  • Immunoglobulin Fab Fragments
  • Muromonab-CD3