Journal
THERANOSTICS
Volume 6, Issue 2, Pages 243-253Publisher
IVYSPRING INT PUBL
DOI: 10.7150/thno.14322
Keywords
Exendin-4; Evans blue; Albumin-binding; PET; Abextide
Categories
Funding
- National Natural Science Foundation of China [81471684, 81371596]
- Intramural Research Program, National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health
- China Scholarship Council (CSC)
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The efficacy of therapeutic drugs is highly dependent on their optimal in vivo pharmacokinetics. Albumin conjugation is considered to be one of the most effective means of protracting the short lifespan of peptides and proteins. In this study, we proposed a novel platform for developing long lasting therapeutics by conjugating a small molecular albumin binding moiety, truncated Evans blue, to either peptides or proteins. Using the anti-diabetic peptide drug Exendin-4 as a model peptide, we synthesized a new long-acting Exendin-4 derivative (denoted as Abextide). Through complexation with albumin in situ, the biological half-life of Abextide was significantly extended. The hypoglycemic effect of Abextide was also improved remarkably over Exendin-4. Thus, Abextide has considerable potential to treat type 2 diabetes. This strategy as a general technology platform can be applied to other small molecules and biologics for the development of long-acting therapeutic drugs.
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