Bicyclic peptide antagonists derived from genetically encoded combinatorial libraries

Chimia (Aarau). 2011;65(9):677-9. doi: 10.2533/chimia.2011.677.

Abstract

Ligands based on bicyclic peptides can combine favourable properties of antibodies (good binding affinity and target specificity) and small molecule ligands (stability, access to chemical synthesis, diffusion properties) and might be suitable molecular structures for the development of therapeutics. By using a combinatorial methodology based on phage display and a chemical cyclisation reaction, we are generating bicyclic peptide antagonists of protein targets with therapeutic applications in mind.

MeSH terms

  • Bridged Bicyclo Compounds / chemical synthesis
  • Bridged Bicyclo Compounds / chemistry*
  • Bridged Bicyclo Compounds / pharmacology
  • Combinatorial Chemistry Techniques / methods*
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Ligands
  • Models, Molecular
  • Peptide Library*
  • Peptides, Cyclic / chemical synthesis
  • Peptides, Cyclic / chemistry*
  • Peptides, Cyclic / genetics
  • Peptides, Cyclic / pharmacology
  • Plasma Kallikrein / antagonists & inhibitors

Substances

  • Bridged Bicyclo Compounds
  • Enzyme Inhibitors
  • Ligands
  • Peptide Library
  • Peptides, Cyclic
  • Plasma Kallikrein