Bicyclic peptide antagonists derived from genetically encoded combinatorial libraries.
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.
Ecole Polytechnique Fédérale de Lausanne, EPFL Institute of Chemical Sciences and Engineering, CH1015 Lausanne. christian.heinis@epfl.ch
Christian
C
Heinis
D001643:Bridged Bicyclo Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D019151:Peptide Library; D010456:Peptides, Cyclic / Q000138:chemical synthesis / Q000737:chemistry* / Q000235:genetics / Q000494:pharmacology; D020842:Plasma Kallikrein / Q000037:antagonists & inhibitors
D001643:Bridged Bicyclo Compounds; D004791:Enzyme Inhibitors; D008024:Ligands; D019151:Peptide Library; D010456:Peptides, Cyclic; D020842:Plasma Kallikrein