Article
Imaging Mutant Huntingtin Aggregates: Development of a Potential PET Ligand.
Journal of medicinal chemistry - 13 Aug 2020
Liu Longbin, Prime Michael E, Lee Matt R, Khetarpal Vinod, Brown Christopher J, Johnson Peter D, Miranda-Azpiazu Patricia, Chen Xuemei, Clark-Frew Daniel, Coe Samuel, Davis Randall, Dickie Anthony, Ebneth Andreas, Esposito Simone, Gadouleau Elise, Gai Xinjie, Galan Sebastien, Green Samantha, Greenaway Catherine, Giles Paul, Halldin Christer, Hayes Sarah, Herbst Todd, Herrmann Frank, Heßmann Manuela, Jia Zhisheng, Kiselyov Alexander, Kotey Adrian, Krulle Thomas, Mangette John E, Marston Richard W, Menta Sergio, Mills Matthew R, Monteagudo Edith, Nag Sangram, Nibbio Martina, Orsatti Laura, Schaertl Sabine, Scheich Christoph, Sproston Joanne, Stepanov Vladimir, Svedberg Marie, Takano Akihiro, Taylor Malcolm, Thomas Wayne, Toth Miklós, Vaidya Darshan, Vanräs Katarina, Weddell Derek, Wigginton Ian, Wityak John, Mrzljak Ladislav, Munoz-Sanjuan Ignacio, Bard Jonathan A, Dominguez Celia
Abstract excerpt
Mutant huntingtin (mHTT) protein carrying the elongated N-terminal polyglutamine (polyQ) tract misfolds and forms protein aggregates characteristic of Huntington's disease (HD) pathology. A high-affinity ligand specific for mHTT aggregates could serve as a positron emission tomography (PET) imaging biomarker for HD therapeutic development and disease progression. To identify such compounds with binding affinity...
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