Synthesis and Structure-Affinity Relationship of Small Molecules for Imaging Human CD80 by Positron Emission Tomography.

Animals B7-1 Antigen / analysis Binding Sites Humans Mice Mice, SCID Molecular Structure Neoplasms, Experimental / diagnostic imaging Positron Emission Tomography Computed Tomography Small Molecule Libraries / chemical synthesis

Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
12 09 2019
Historique:
pubmed: 21 8 2019
medline: 1 7 2020
entrez: 21 8 2019
Statut: ppublish

Résumé

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 (

Identifiants

DOI: 10.1021/acs.jmedchem.9b00858 PMID: 31430137
pubmed: 31430137
doi: 10.1021/acs.jmedchem.9b00858
doi:

Substances chimiques

B7-1 Antigen 0
CD80 protein, human 0
Small Molecule Libraries 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

8090-8100

Auteurs

Marco F Taddio (MF)

Center for Radiopharmaceutical Sciences ETH, PSI and USZ, Department of Chemistry and Applied Biosciences , ETH Zurich , CH-8093 Zurich , Switzerland.
ORCID: 0000-0003-2477-5575

Linjing Mu (L)

Center for Radiopharmaceutical Sciences ETH, PSI and USZ, Department of Chemistry and Applied Biosciences , ETH Zurich , CH-8093 Zurich , Switzerland.
Department of Nuclear Medicine , University Hospital Zurich , CH-8091 Zurich , Switzerland.

Claudia A Castro Jaramillo (CA)

Center for Radiopharmaceutical Sciences ETH, PSI and USZ, Department of Chemistry and Applied Biosciences , ETH Zurich , CH-8093 Zurich , Switzerland.

Tanja Bollmann (T)

Center for Radiopharmaceutical Sciences ETH, PSI and USZ, Department of Chemistry and Applied Biosciences , ETH Zurich , CH-8093 Zurich , Switzerland.

Dominik M Schmid (DM)

Center for Radiopharmaceutical Sciences ETH, PSI and USZ, Department of Chemistry and Applied Biosciences , ETH Zurich , CH-8093 Zurich , Switzerland.

Lukas P Muskalla (LP)

Laboratory for Catalysis and Sustainable Chemistry , Paul Scherrer Institute , CH-5232 Villigen PSI , Switzerland.

Tim Gruene (T)

Laboratory for Catalysis and Sustainable Chemistry , Paul Scherrer Institute , CH-5232 Villigen PSI , Switzerland.
X-ray Structure Analysis Centre, Faculty of Chemistry , University of Vienna , A-1090 Vienna , Austria.

Aristeidis Chiotellis (A)

Center for Radiopharmaceutical Sciences ETH, PSI and USZ, Department of Chemistry and Applied Biosciences , ETH Zurich , CH-8093 Zurich , Switzerland.

Simon M Ametamey (SM)

Center for Radiopharmaceutical Sciences ETH, PSI and USZ, Department of Chemistry and Applied Biosciences , ETH Zurich , CH-8093 Zurich , Switzerland.
ORCID: 0000-0003-4285-6731

Roger Schibli (R)

Center for Radiopharmaceutical Sciences ETH, PSI and USZ, Department of Chemistry and Applied Biosciences , ETH Zurich , CH-8093 Zurich , Switzerland.

Stefanie D Krämer (SD)

Center for Radiopharmaceutical Sciences ETH, PSI and USZ, Department of Chemistry and Applied Biosciences , ETH Zurich , CH-8093 Zurich , Switzerland.
ORCID: 0000-0002-0426-4340

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Synthesis and Structure-Affinity Relationship...
questionsmedicales.fr › Facteurs biologiques › Protéines et peptides de signalisation intercellulaire › Antigènes B7 › Antigène CD80 › Synthesis and Structure-Affinity Relationship...
questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Sites de fixation › Synthesis and Structure-Affinity Relationship...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Synthesis and Structure-Affinity Relationship...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Synthesis and Structure-Affinity Relationship...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Souches mutantes de souris › Souris SCID › Synthesis and Structure-Affinity Relationship...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Synthesis and Structure-Affinity Relationship...
questionsmedicales.fr › Techniques d'investigation › Modèles animaux › Tumeurs expérimentales › Synthesis and Structure-Affinity Relationship...
questionsmedicales.fr › Diagnostic › Techniques et procédures diagnostiques › Techniques de diagnostic radioisotopique › Scintigraphie › Tomoscintigraphie › Tomographie par émission de positons › Tomographie par émission de positons couplée à la tomodensitométrie › Synthesis and Structure-Affinity Relationship...
questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Produits chimiques de laboratoire › Bibliothèques de petites molécules › Synthesis and Structure-Affinity Relationship...