Publication: Synthesis and structure-affinity relationship of small molecules for imaging human CD80 by positron emission tomography
Synthesis and structure-affinity relationship of small molecules for imaging human CD80 by positron emission tomography
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Taddio, M. F., Mu, L., Castro Jaramillo, C. A., Bollmann, T., Schmid, D. M., Muskalla, L. P., Gruene, T., Chiotellis, A., Ametamey, S. M., Schibli, R., & Krämer, S. D. (2019). Synthesis and structure-affinity relationship of small molecules for imaging human CD80 by positron emission tomography. Journal of Medicinal Chemistry, 62(17), 8090–8100. https://doi.org/10.1021/acs.jmedchem.9b00858
Abstract
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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
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- Taddio, Marco F
- Mu, Linjing
- Castro Jaramillo, Claudia A
- Bollmann, Tanja
- Schmid, Dominik M
- Muskalla, Lukas P
- Gruene, Tim
- Chiotellis, Aristeidis
- Ametamey, Simon M
- Schibli, Roger
- Krämer, Stefanie D
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Taddio, M. F., Mu, L., Castro Jaramillo, C. A., Bollmann, T., Schmid, D. M., Muskalla, L. P., Gruene, T., Chiotellis, A., Ametamey, S. M., Schibli, R., & Krämer, S. D. (2019). Synthesis and structure-affinity relationship of small molecules for imaging human CD80 by positron emission tomography. Journal of Medicinal Chemistry, 62(17), 8090–8100. https://doi.org/10.1021/acs.jmedchem.9b00858