Perfluoroalkylation Based Half-Life Extension Service
For Research Use Only. Not for Clinical Use.
In recent years, many chemical groups are used to prolong therapeutic proteins' half-life, among which perfluoroalkyl modification has attracted more attention for its unique mechanism and stable self-assembly performance. After perfluoroalkyl modification, the proteins obtain controllable self-segregating ability while increasing lipid solubility, which can improve pharmacokinetic properties while maintaining the original efficacy. It has been proved that perfluoroalkylation is a novel and available method to extend half-life in drug delivery. Creative Biolabs is an outstanding service provider that offers the most comprehensive and professional perfluoroalkylation based half-life extension service to advance clients' projects.
Introduction of Perfluoroalkylation Based Half-Life Extension Service
Perfluorinated carbon compounds exhibit more hydrophobic than similar hydrocarbon, which has been exploited to increase the lipophilicity and prolong the half-life of various drugs. However, perfluoroalkyl group tends also to be poorly soluble in hydrocarbon solvents even though bearing high hydrophobicity. This novel phase partitioning properties can cause self-assembly of perfluorinated peptides or proteins to form oligomeric state in vivo. Compared with alkyl residue mediated self-assembly, perfluoroalkylation based aggregation states show high stability in either hydrophilic environment or hydrophobic environment. This self-assembly effect can escape from endogenous degradation and extend the half-life of protein drugs.
Moreover, the perfluoroalkyl chain structure can control the level of fluorous interactions between the perfluoroalkyl proteins, then cause different scenarios for self-assembly. This result suggests that suitable perfluoroalkyl modification will lead to a multivalent effect and further enhance the bioavailability as well as potency. Therefore, perfluoroalkylation based half-life extension strategy became more popular in new drugs development owing to its conveniences, satisfactory effect, and low cast.
Applications of Perfluoroalkylation Based Half-Life Extension Service
- Fluorinated amino acid involvement
Some scientists use protein synthesis techniques to replace a few hydrophobic amino acid residues in natural proteins with fluorinated groups, such as hexafluoroleucine, and hexafluorovaline. Due to the hydrophobicity of fluorocarbons the natural folding of active domain will be maintained after fluorinated amino acid is introduced, which ensures the potency. However, the involvement of fluorinated amino acid stabilizes the 3D structures of proteins and rescue them from recognition of endogenous protease.
Fig.1 The leucine and hexafluoroleucine zipper domain. (Neil, 2000)
- Perfluoroalkylation Modification
Perfluoroalkyl can also be involved in therapeutic protein molecules by chemical modification. In recent studies, various perfluoroalkyl derivative group has been attached with protein drugs with covalent binding to mediate protein drugs intermolecular polymerization. The oligomeric state of protein self-assembly in the solution can be controlled by changing the length and structure of perfluoroalkyl groups, which is important in their half-life extension. This method is simple, inexpensive, and has great potential for clinical research.
Fig.2 Illustration of perfluoroalkyl insulin self-assembly. (Malik, 2012)
Perfluoroalkylation technology extends the half-life of protein drugs in a creative, easy, and economical way. It is widely suitable for most proteins and has rich application value. Please don't hesitate to contact us for more details.
References
- Neil, E.; et al. Towards the nonstick egg: designing fluorous proteins. Chemistry & biology. 2000, 7(7), R153-R157.
- Malik, L.; et al. Perfluoroalkyl chains direct novel self-assembly of insulin. Langmuir. 2012, 28(2), 593-603.
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For Research Use Only. Not for Clinical Use.