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 similar to 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.

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

LINCIANO, SARA
Writing – Original Draft Preparation
;
Angelini A.
Writing – Review & Editing
2019-01-01

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 similar to 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.
2019
10
File in questo prodotto:
File Dimensione Formato  
Non-covalent albumin-binding ligands to extend the circulating half-life of small biotherapeutics_Pre-print.pdf

non disponibili

Tipologia: Documento in Pre-print
Licenza: Accesso chiuso-personale
Dimensione 5.42 MB
Formato Adobe PDF
5.42 MB Adobe PDF   Visualizza/Apri

I documenti in ARCA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10278/3717437
Citazioni
  • ???jsp.display-item.citation.pmc??? 44
  • Scopus 116
  • ???jsp.display-item.citation.isi??? 105
social impact