Enhancing peptide ligand binding to vascular endothelial growth factor by covalent bond formation.

ABSTRACT: Formation of a stable covalent bond between a synthetic probe molecule and a specific site on a target protein has many potential applications in biomedical science. For example, the properties of probes used as receptor-imaging ligands may be improved by increasing their residence time on the targeted receptor. Among the more interesting cases are peptide ligands, the strongest of which typically bind to receptors with micromolar dissociation constants, and which may depend on processes other than simple binding to provide images. The side chains of cysteine, histidine, or lysine are attractive for chemical attachment to improve binding to a receptor protein, and a system based on acryloyl probes attaching to engineered cysteine provides excellent positron emission tomographic images in a

SUBMITTER: Marquez BV 

PROVIDER: S-EPMC3431436 | biostudies-literature | 2012 May

REPOSITORIES: biostudies-literature