Metal Chelators / Radioligands

Molecular imaging has become an indispensable tool in modern diagnostics in biomedical research and therapeutic fields. Modern imaging techniques increasingly rely on the use of radioactive isotopes of certain metal ions, often in combination with targeting peptides.

Custom synthesis of such peptide conjugates, in which a chelating agent is covalently linked to the peptide, is also available at Pepscan. The modifications can be made at the N-terminus or at the C-terminus via a C-terminal lysine. These conjugates are able to give very stable complexes of many metals or with radioactive isotopes of metals currently used in Nuclear Medicine (In-111, Y-90,Tc-99m, Lu-177, Ga-68).

Pepscan routinely applies a variety of chelating agents, such DOTA, DTPA, NOTA and TETA.

DOTA

DOTA (1,4,7,10-tetraazacyclododecane-N,N’,N”,N”’-tetraacetic acid)

DTPA

DTPA (Diethylenetriaminepentaacetic Anhydride)

NOTA

NOTA (1,4,7-triazacyclononane-N,N’,N”-triacetic acid)

TETA

TETA (1,4,8,11-tetraazacyclotetradecane-1,4,8,11-tetraacetic acid)

Selected references for Metal Chelator peptides

Nielsen et al: Nucl. Med. Biol (2016) – PMID 27474962. (68)Ga-labeled phage-display selected peptides as tracers for positron emission tomography imaging of Staphylococcus aureus biofilm-associated infections: Selection, radiolabelling and preliminary biological evaluation.