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Non-covalent albumin-binding ligands for extending the circulating half-life of small biotherapeutics.

ABSTRACT: Peptides and small protein scaffolds are gaining increasing interest as therapeutics. Similarly to full-length antibodies, they can bind a target with a high binding affinity and specificity while remaining small enough to diffuse into tissues. However, despite their numerous advantages, small biotherapeutics often suffer from a relatively short circulating half-life, thus requiring frequent applications that ultimately restrict their ease of use and user compliance. To overcome this limitation, a large variety of half-life extension strategies have been developed in the last decades. Linkage to ligands that non-covalently bind to albumin, the most abundant serum protein with a circulating half-life of ?19 days in humans, represents one of the most successful approaches for the generation of long-lasting biotherapeutics with improved pharmacokinetic properties and superior efficacy in the clinic.

SUBMITTER: Zorzi A

PROVIDER: S-EPMC6644573 | biostudies-literature | 2019 Jul

REPOSITORIES: biostudies-literature

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Non-covalent albumin-binding ligands for extending the circulating half-life of small biotherapeutics.

Zorzi Alessandro A Linciano Sara S Angelini Alessandro A

MedChemComm 20190606 7

Peptides and small protein scaffolds are gaining increasing interest as therapeutics. Similarly to full-length antibodies, they can bind a target with a high binding affinity and specificity while remaining small enough to diffuse into tissues. However, despite their numerous advantages, small biotherapeutics often suffer from a relatively short circulating half-life, thus requiring frequent applications that ultimately restrict their ease of use and user compliance. To overcome this limitation, ...[more]

PMID: 31391879

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