Therapeutic peptides isolated from natural resources or chemical libraries or rationally designed become increasingly important. Several approved peptide drugs such as GLP-1 analogs, insulin or human parathyroid hormone (PTH) have reached blockbuster sales. Others, like thymosin beta 4, the C-type natriuretic peptide (CNP) or relaxin, are currently undergoing clinical testing. However, with generally fast clearance, degradation by serum exopeptidases and often complex and expensive synthesis, this drug class faces challenges. PASylation®, the genetic fusion or chemical conjugation with a conformationally disordered polypeptide of Pro, Ala, and/or Ser offers an elegant solution to prolong the plasma half-life of peptides and enable efficient homogenous peptide production, leading to enhanced therapeutic action and reduced injection frequencies.
Tunable plasma half-life
- Expanded hydrodynamic volume
leading to extended circulation time - Shielding against plasma proteases
- Reduced injection frequency
- Expanded hydrodynamic volume
Chemical conjugation
- Various formats of activated PAS polypeptides
- Homogenous PAS polypeptide
Biodegradable PEG alternative
- PAS overcomes PEG hypersensitivity
- No organ accummulation during chronic treatment
Efficient recombinant production
- Genetic fusion: no cytoplasmic degradation, homogenous product & reduced costs
- Creation of long-acting bispecific peptides
- Design of long-acting bispecific peptides feasible
- High-yield secretory production of mature peptides (multiple g/L) demonstrated using an industry-standard expression system
SAN DIEGO, USA, and FREISING, Germany, 15th October, 2020: XL-protein and Antlia Bioscience Announce Collaboration to Develop Long-acting Peptide Therapy of Chronic Heart Failure using PASylation® Technology
Binder U., Skerra A. (2020) PASylated Thymosin α1: a long-acting immunostimulatory peptide for applications in oncology and virology. Int. J. Mol. Sci. 22, E124.
SAN DIEGO, USA, and FREISING, Germany, 18th December, 2018: Ajinomoto and XL-protein Forge Strategic Alliance to Develop PASylated Therapeutics Applying the Corynex® Platform.