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In Vivo Half-Life Extension of BMP1/TLL Metalloproteinase Inhibitors Using Small-Molecule Human Serum Albumin Binders

Scientific article

In Vivo Half-Life Extension of BMP1/TLL Metalloproteinase Inhibitors Using Small-Molecule Human Serum Albumin Binders

Vantourout JC
GSK
March 15, 2021
Bioconjug Chem
https://pubmed.ncbi.nlm.nih.gov/33523652

This article is currently being updated. View its version on PubMed.

https://pubmed.ncbi.nlm.nih.gov/33523652

Research summary

This study explores how conjugating a BMP1/TLL inhibitor to a small-molecule non‑covalent human serum albumin (HSA) binder (AlbuBinder 1) dramatically extends its in vivo half‑life in mice.

Key outcome of the study

AlbuBinder–inhibitor conjugate showed >20‑fold increased half‑life (>48 h vs. 3 h), maintaining BMP1/TLL inhibition—demonstrating albumin-binding as an effective pharmacokinetic enhancement strategy.

Model

GenOway-developed HSA knock‑in mouse (HSA KI/KI), expressing human serum albumin in place of endogenous albumin

Highlighted article
TARGET:
Albumin (Alb)
Synonyms:
HSA, Serum albumin

Keywords

Pharmacokinetics, Half‑life extension, Albumin-binding therapeutics, Protease inhibition

Technical specifications

Knockin, Human serum albumin locus, Homozygous HSA expression, Pharmacokinetic modeling

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