Content of research

Cyclic peptides are an ideal molecular form for exploring biologically active compounds (drug discovery) and the design of molecular tools in life science. Cyclization of the peptide backbone can control their conformational stability, orientation, and symmetry. However, peptide cyclization requires specific dilution conditions and complex basic protection strategies. We found that combining a hydrogen-bond-controlled solvent system and a base-free condensation agent system enables the efficient cyclization of poorly soluble peptides under highly concentrated conditions. The simplicity of this technology gives a wide range of applications for drug discovery and life sciences by facilitating the free design and mass production of cyclic peptides.

Potential for social implementation

• ・Pharmaceuticals and agrochemicals
• ・Bioprobe development
• ・Development of organic materials
• ・Development of nanomachines

Appealing points to industry and local governments

Coordination stabilization upon cyclization of peptides can maximize the target action and suppress side effects and metabolic rate. It is also easy to control the symmetry, orientation and coordination stability of peptides, providing a high degree of freedom for nanomachine design. Using peptides, we can lower the barrier between molecular design and acquisition of compounds for drug discovery, bio-tools and nanomachines.