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Cover Feature: A Comparative Study of in vitro Assays for Predicting the Nonspecific Binding of PET Imaging Agents in vivo (ChemMedChem 7/2020)
Author(s) -
Gobbi Luca,
Mercier Joël,
BangAndersen Benny,
Nicolas JeanMarie,
Reilly John,
Wagner Björn,
Whitehead David,
Briard Emmanuelle,
Maguire R. Paul,
Borroni Edilio,
Auberson Yves P.
Publication year - 2020
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201000140
Subject(s) - in vivo , pet imaging , chemistry , positron emission tomography , in vitro , cover (algebra) , membrane , feature (linguistics) , biophysics , plasma protein binding , biochemistry , biology , neuroscience , philosophy , mechanical engineering , linguistics , microbiology and biotechnology , engineering
The Cover Feature shows the two possible fates of a positron emission tomography (PET) imaging agent approaching its target: a nonspecific interaction with the membranes, or specific binding to the target protein. Quantifying and reducing the nonspecific binding of imaging agents during their chemical optimization is critical to ensure image quality. We show that the chromatographic hydrophilicity index on immobilized artificial membranes CHI(IAM) is the most effective method to predict V NS , a direct measure of nonspecific binding in the living human brain. More information can be found in the Full Paper by Yves Auberson, Luca Gobbi, Joël Mercier, Benny Bang‐Andersen et al..