Discovery Service of Diverse and High-Affinity Cyclic Peptides(Generation & Development of Affinity lingands)

FUJIFILM

Peptides are gathering significant attention not only for their affinity and specificity towards a diverse array of target proteins but also for their tissue permeability (oral suitability) and ease of chemical synthesis. Notably, cyclic peptides that incorporate non-natural amino acids are expected to function as PPI inhibitors for both intracellular and extracellular targets. Additionally, they are anticipated to act as DDS ligands, facilitating the delivery and accumulation of nucleic acid-based medicines and other drugs in targeted tissues due to their exceptional binding affinity and stability.

The FUJIFILM Group offers a comprehensive suite of contract services. Our core offerings are the use of mRNA display technology to acquire peptides with strong, specific binding to target proteins, coupled with expedited structural optimization activity screening and of these hit peptides (e.g., inhibition activity, selectivity, cellular activity). Additionally, we provide supporting services such as peptide chemical synthesis and the expression and purification of target proteins.

collaborated with PURE frex

Our service enables the acquisition of diverse high-affinity peptides from an extensive cyclic peptide library, which includes unnatural amino acids. Additionally, during the activity screening and structural optimization processes, our peptide enzymatic synthesis technology enhances rapid and comprehensive evaluation, thereby supporting the swift identification of lead peptides with desired properties.

Flow and Features of Peptide Discovery Services

Flow:

We receive target* () from the customer and return the structural information of the acquired peptides (: below).
*Required target protein: 0.1~0.5 mg, >90% in purity

Flow of discovery

Features:

  • Innovative improvements in mRNA display enable screening from >1013 peptides.
  • Practical biosynthesis & assays enable rapid selection and activity explorations.
    → Peptides with wide varieties and high-affinities(~nM) can be obtained with high success rate (If you are interested in details of our trackrecords, please feel free to contact us.).

Characteristics of Cyclic peptide with unnatural amino acids

Cyclic peptides with unnatural amino acids have the following characteristics:

  • Wide binding capacity and high specificity to undruggable targets.
  • Higher stability, lower immunogenicity, and higher tissue permeability than antibodies.
  • Being able to be chemically synthesized and be conjugated to other molecules.
    (CMC difficulty is also low.)

(We can also handle other peptides and small proteins.)

Technology①: mRNA display

  • Improved mRNA display allows screening from a huge library.
  • Many conditions (=cycle size, targets, selections) can be performed in parallel.
    A variety of hits have been obtained with a high success rate.
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Technology②: Biosynthesis & assays

Rapid selection and activity exploration by practical biosynthesis & assay combined with conventional chemical synthesis.

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Biosynthesis (in vitro translation): can be synthesized in short time (5~7days) parallelly (>103 peptides can be evaluated in a month)

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Result①: Screening of FGFR binding peptides

Diverse binding peptides were successfully obtained toward both of 2 FGFRs (fibroblast growth factor receptor).

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Result②: Power of biosynthetic screening

  • FGFR activatable peptide had been found through rapid and exhaustive cell activity screening with biosynthetic peptides from diverse hit peptides.
  • Optimized peptide showed same cell growth rate with the natural protein (bFGF) in MSC (Mesenchymal Stem Cell).
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Keywords: cyclic peptide, peptide drug, oligonucleotide drug, RNAi, miRNA, siRNA, antisense oligonucleotide, ASO, DDS, Ligand, Targeting, PPI inhibition, orally available, PO

For research use or further manufacturing use only. Not for use in diagnostic procedures.

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