XTENylation Service

XTEN is a kind of unstructured, hydrophilic and biodegradable protein polymer, which with large hydrodynamic volume and negative charge. The fusion expression of polypeptide drugs with XTEN by genetic engineering can enhance the stability and solubility of peptide drugs. Therefore, XTEN modification technology is often used to prolong the half-life of drugs. XTENs are non-repetitive amino acid sequence composed of six hydrophilic and chemically stable amino acids, which designs to improve the performance of protein and peptide pharmaceuticals. At present, XTEN technology has been applied to a variety of biological treatment methods including hormones, coagulation factors and peptides. It has broad application prospects in the rectangular mask of half-life extension of peptide and protein drugs.

Figure 1. XTENylation in the development of biobetters (Torres-Obreque K M et al. 2021).

There are several benefits of XTENylation:

• XTEN carries glutamate residues, which makes the fusion protein wiht a large negative charge;
• XTEN carries glutamate residues, which will reduce its affinity with the receptor, and avoid the clearance of receptor-mediated protein drugs;
• XTEN prolongs the half-life for protein and polypeptide therapeutics;
• With engineering of XTEN polymer, the fusion product can be easily expressed in cytosol in soluble form;
• XTEN fusion enhances the solubility and stability of the target peptide and protein;
• XTEN protein polymers has high biosafety due to it is biodegradable and will not accumulate in organs or cells.

At Profacgen, we can provide the XTENylation service based on our in-house recombinant protein expression and chemical coupling platform.

Figure 2. XTENylation of biologically active molecules (Anand R et al. 2018).

(A) Genetic fusion—a single polypeptide which includes both the therapeutic and bulking moieties;

(B) Chemical conjugation—XTEN is first expressed and purified as an intermediate and then conjugated to biologically active payloads

With our drug development platform, Profacgen can develop XTENylation modification methods according to the characteristics of drugs. If you are interested in our services, please feel free to contact us. We are looking forward to cooperating with you.