Search

Your search keyword '"Ming Min Hsai"' showing total 2 results
Start Over Author "Ming Min Hsai"
2 results on '"Ming Min Hsai"'

1. Design and Evaluation of [18F]CHDI-650 as a Positron Emission Tomography Ligand to Image Mutant Huntingtin Aggregates

Author

Longbin Liu, Peter D. Johnson, Michael E. Prime, Vinod Khetarpal, Christopher J. Brown, Luca Anzillotti, Daniele Bertoglio, Xuemei Chen, Samuel Coe, Randall Davis, Anthony P. Dickie, Simone Esposito, Elise Gadouleau, Paul R. Giles, Catherine Greenaway, James Haber, Christer Halldin, Scott Haller, Sarah Hayes, Todd Herbst, Frank Herrmann, Manuela Heßmann, Ming Min Hsai, Yaser Khani, Adrian Kotey, Angelo Lembo, John E. Mangette, Gwendolyn A. Marriner, Richard W. Marston, Matthew R. Mills, Edith Monteagudo, Anton Forsberg-Morén, Sangram Nag, Laura Orsatti, Christine Sandiego, Sabine Schaertl, Joanne Sproston, Steven Staelens, Jack Tookey, Penelope A. Turner, Andrea Vecchi, Maria Veneziano, Ignacio Muñoz-Sanjuan, Jonathan Bard, and Celia Dominguez

Subjects
Drug Discovery, Molecular Medicine, Settore CHIM/08 - Chimica Farmaceutica, Settore CHIM/06
Published
2022

2. [11C]CHDI-626, a PET Tracer Candidate for Imaging Mutant Huntingtin Aggregates with Reduced Binding to AD Pathological Proteins

Author

Vinod Khetarpal, Catherine Greenaway, Samantha Ensor, Randall Davis, Michael Conlon, Andrea Varrone, Frank Herrmann, Laura Orsatti, Xuemei Chen, Martina Nibbio, Christer Halldin, Vladimir Stepanov, Simone Esposito, Daniel Clark-Frew, Ladislav Mrzljak, Christoph Scheich, Sabine Schaertl, Todd Herbst, Ming Min Hsai, Peter Johnson, Samuel Coe, Jonathan Bard, John Wityak, Michael Prime, Katarina Varnäs, Adrian Kotey, Lee Matthew, Sangram Nag, Manuela Heßmann, Celia Dominguez, Samantha Green, James C. Haber, Xinjie Gai, Longbin Liu, Edith Monteagudo, Anton Forsberg Morén, John E. Mangette, Christopher J. Brown, Matthew R. Mills, Ignacio Munoz-Sanjuan, Joanne Sproston, and Sarah Hayes

Subjects
Huntingtin, medicine.diagnostic_test, Chemistry, Mutant, Medium spiny neuron, Positron emission tomography, Free fraction, Drug Discovery, medicine, Cancer research, Molecular Medicine, Neuronal degeneration, Pet tracer, Pathological
Abstract

The expanded polyglutamine-containing mutant huntingtin (mHTT) protein is implicated in neuronal degeneration of medium spiny neurons in Huntington's disease (HD) for which multiple therapeutic approaches are currently being evaluated to eliminate or reduce mHTT. Development of effective and orthogonal biomarkers will ensure accurate assessment of the safety and efficacy of pharmacologic interventions. We have identified and optimized a class of ligands that bind to oligomerized/aggregated mHTT, which is a hallmark in the HD postmortem brain. These ligands are potentially useful imaging biomarkers for HD therapeutic development in both preclinical and clinical settings. We describe here the optimization of the benzo[4,5]imidazo[1,2-a]pyrimidine series that show selective binding to mHTT aggregates over Aβ- and/or tau-aggregates associated with Alzheimer's disease pathology. Compound [11C]-2 was selected as a clinical candidate based on its high free fraction in the brain, specific binding in the HD mouse model, and rapid brain uptake/washout in nonhuman primate positron emission tomography imaging studies.

Published
2021

Catalog

Books, media, physical & digital resources
See catalog results