Literature DB >> 30810314

Discovery of N-(4-[18F]Fluoro-5-methylpyridin-2-yl)isoquinolin-6-amine (JNJ-64326067), a New Promising Tau Positron Emission Tomography Imaging Tracer.

Frederik J R Rombouts1, Lieven Declercq, José-Ignacio Andrés2, Astrid Bottelbergs1, Lu Chen3, Laura Iturrino2, Joseph E Leenaerts1, Jonas Mariën1, Fengbin Song3, Cindy Wintmolders1, Stijn Wuyts1, Chunfang A Xia4, Paula Te Riele1, Guy Bormans, Rik Vandenberghe, Hartmuth Kolb4, Diederik Moechars1.   

Abstract

In Alzheimer's disease, the density and spread of aggregated tau protein track well with neurodegeneration and cognitive decline, making the imaging of aggregated tau a compelling biomarker. A structure-activity relationship exploration around an isoquinoline hit, followed by an exploration of tolerated fluorination positions, allowed us to identify 9 (JNJ-64326067), a potent and selective binder to aggregated tau with a favorable pharmacokinetic profile and no apparent off-target binding. This was confirmed in rat and monkey positron emission tomography studies using [18F]9.

Entities:  

Year:  2019        PMID： 30810314     DOI： 10.1021/acs.jmedchem.8b01759

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  7 in total

1.  Structure-Activity Relationships of Radioiodinated 6,5,6-Tricyclic Compounds for the Development of Tau Imaging Probes.

Authors:  Hiroyuki Watanabe; Haruka Tatsumi; Sho Kaide; Yoichi Shimizu; Shimpei Iikuni; Masahiro Ono
Journal:  ACS Med Chem Lett       Date:  2020-01-09       Impact factor: 4.345

2.  Discovery and preclinical characterization of [18F]PI-2620, a next-generation tau PET tracer for the assessment of tau pathology in Alzheimer's disease and other tauopathies.

Authors:  Heiko Kroth; Felix Oden; Jerome Molette; Hanno Schieferstein; Francesca Capotosti; Andre Mueller; Mathias Berndt; Heribert Schmitt-Willich; Vincent Darmency; Emanuele Gabellieri; Cédric Boudou; Tanja Juergens; Yvan Varisco; Efthymia Vokali; David T Hickman; Gilles Tamagnan; Andrea Pfeifer; Ludger Dinkelborg; Andreas Muhs; Andrew Stephens
Journal:  Eur J Nucl Med Mol Imaging       Date:  2019-07-01       Impact factor: 9.236

3.  Isoquinolinamine FX-9 Exhibits Anti-Mitotic Activity in Human and Canine Prostate Carcinoma Cell Lines.

Authors:  Jan Torben Schille; Ingo Nolte; Eva-Maria Packeiser; Laura Wiesner; Jens Ingo Hein; Franziska Weiner; Xiao-Feng Wu; Matthias Beller; Christian Junghanss; Hugo Murua Escobar
Journal:  Int J Mol Sci       Date:  2019-11-07       Impact factor: 5.923

4.  Evaluation of [18F]-JNJ-64326067-AAA tau PET tracer in humans.

Authors:  Suzanne L Baker; Karine Provost; Wesley Thomas; A J Whitman; Mustafa Janabi; Mark E Schmidt; Maarten Timmers; Hartmuth C Kolb; Gil D Rabinovici; William J Jagust
Journal:  J Cereb Blood Flow Metab       Date:  2021-07-14       Impact factor: 6.960

5.  Clinical evaluation of [18F] JNJ-64326067, a novel candidate PET tracer for the detection of tau pathology in Alzheimer's disease.

Authors:  Mark E Schmidt; Luc Janssens; Diederik Moechars; Frederik J R Rombouts; Maarten Timmers; Olivier Barret; Cristian C Constantinescu; Jennifer Madonia; David S Russell; Christine M Sandiego; Hartmuth Kolb
Journal:  Eur J Nucl Med Mol Imaging       Date:  2020-06-13       Impact factor: 9.236

Review 6.  Recent Developments in Positron Emission Tomography Tracers for Proteinopathies Imaging in Dementia.

Authors:  Ruiqing Ni; Roger M Nitsch
Journal:  Front Aging Neurosci       Date:  2022-01-03       Impact factor: 5.750

7.  Discriminatory ability of next-generation tau PET tracers for Alzheimer's disease.

Authors:  Steven Y Yap; Barbara Frias; Melissa C Wren; Michael Schöll; Nick C Fox; Erik Årstad; Tammaryn Lashley; Kerstin Sander
Journal:  Brain       Date:  2021-09-04       Impact factor: 13.501
  7 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.