Peptide drugs have been expected to be molecularly-targeted drugs for all biological macromolecules, but their binding affinity to “androgable” proteins, sensitivity to proteolytic enzymes, cell membrane permeability, and pharmacokinetics （rapid elimination from the kidneys） The development of drugs for “androgynous” proteins is difficult as it is, mainly because of the following problems The α-helix cross-linked peptides consisting only of hydrocarbons, in which our CEO is involved as a developer, are known as a basic technology for drug discovery that solves these problems.

Against this background, we have developed β-strand cross-linked peptides, which are almost unprecedented in the world. α-helix cross-linked peptides fix α-helix by cross-linking, whereas β-strand cross-linked peptides destabilize conformations other than β-strand. The β-strand cross-linked peptides are designed to destabilize conformations other than the β strand. Quantum chemical calculations show that the β-strand is more stable than the α-helix, 310-helix, and PPII helix, a result consistent with the molecular design. We also found that the cross-linked peptides are more permeable to cell membranes than wild-type peptides.

[patent application]
β-strand bridge peptides

Patented Inventions
・Cross-linked peptides
・Artificial amino acids with more than 3000 substituents at the β-position (substituents that improve cell membrane permeability)