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Updated: Jan 20, 2026

Automation of a Positron-emission Tomography PET Radiotracer Synthesis Protocol for Clinical Production
Published on: October 26, 2018
Synthesis and Structure-Affinity Relationship of Small Molecules for Imaging Human CD80 by Positron Emission
Marco F Taddio1, Linjing Mu1,2, Claudia A Castro Jaramillo1
1Center for Radiopharmaceutical Sciences ETH, PSI and USZ, Department of Chemistry and Applied Biosciences , ETH Zurich , CH-8093 Zurich , Switzerland.
Abstract:
The costimulatory molecule CD80 is an early marker for immune activation. It is upregulated on activated antigen-presenting cells. We aimed at developing a tracer for imaging CD80 by positron emission tomography (PET). Novel CD80 ligands were synthesized and tested by SPR for affinity to human CD80 (hCD80) and displacement of endogenous ligands. Several compounds bound with one-digit nanomolar affinity to hCD80 and displaced CTLA-4 and CD28 at nanomolar concentrations. A structure-affinity relationship study revealed relevant moieties for strong affinity to hCD80 and positions for further modifications. Lead compound MT107 (7f) was radiolabeled with carbon-11. In vitro, [11C]MT107 showed specific binding to hCD80-positive tissue and high plasma protein binding. In vivo, [11C]MT107 accumulated in liver, gall bladder, and intestines but only scarcely in hCD80-positive xenografts. The unfavorable in vivo performance may result from high plasma protein binding and extensive biliary excretion.
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