Imaging Leucine-Rich Repeat Kinase 2 In Vivo with 18F-Labeled Positron Emission Tomography Ligand

18F-Labelled pyrrolopyrimidines reveal brain leucine-rich repeat kinase 2 expression implicated in Parkinson’s disease

(2021) Xueyuan Chen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Lewis Acid-Facilitated Radiofluorination of MN3PU: A LRRK2 Radiotracer

(2020) Noeen Malik et al.   MOLECULES

Development and biological evaluation of[18F]FMN3PA & [18F]FMN3PU for leucine-rich repeat kinase 2 (LRRK2) in vivo PET imaging

(2020) Noeen Malik et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and preliminary evaluation of [11C]GNE‐1023 as a novel potent PET probe for imaging leucine‐rich repeat kinase 2 (LRRK2) in Parkinson’s disease

(2019) Zhen Chen et al.   ChemMedChem

Identification and Development of an Irreversible Monoacylglycerol Lipase (MAGL) Positron Emission Tomography (PET) Radioligand with High Specificity

(2019) Lei Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Evaluation of 18F-Labeled Monoacylglycerol Lipase Inhibitors as Novel Positron Emission Tomography Probes

(2019) Zhen Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of a Novel Positron Emission Tomography (PET) Ligand for Imaging β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE-1) in Brain

(2018) Lei Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

In Vitro and in Vivo Evaluation of 11C-Labeled Azetidinecarboxylates for Imaging Monoacylglycerol Lipase by PET Imaging Studies

(2018) Ran Cheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chemistry for Positron Emission Tomography: Recent Advances in 11C-, 18F-, 13N- and 15O-labeling Reactions

(2018) Xiaoyun Deng et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Synthesis, pharmacology and preclinical evaluation of 11C-labeled 1,3-dihydro-2H-benzo[d]imidazole-2-ones for imaging γ8-dependent transmembrane AMPA receptor regulatory protein

(2018) Zhen Chen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The Discovery of a Novel Phosphodiesterase (PDE) 4B-Preferring Radioligand for Positron Emission Tomography (PET) Imaging

(2017) Lei Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity

(2017) Jack D. Scott et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and preliminary PET imaging of 11C and 18F isotopologues of the ROS1/ALK inhibitor lorlatinib

(2017) Thomas Lee Collier et al.   Nature Communications

Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging

(2016) Steven H. Liang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Discovery of LRRK2 inhibitors using sequential in silico joint pharmacophore space (JPS) and ensemble docking

(2015) Christian A. Lang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Leucine-rich Repeat Kinase 2 (LRRK2) Pharmacological Inhibition Abates α-Synuclein Gene-induced Neurodegeneration

(2015) João P. L. Daher et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Effect of selective LRRK2 kinase inhibition on nonhuman primate lung

(2015) Reina N. Fuji et al.   Science Translational Medicine

Differential LRRK2 expression in the cortex, striatum, and substantia nigra in transgenic and nontransgenic rodents

(2014) Andrew B. West et al.   JOURNAL OF COMPARATIVE NEUROLOGY

Discovery and Preclinical Profiling of 3-[4-(Morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a Highly Potent, Selective, Brain Penetrant, and in Vivo Active LRRK2 Kinase Inhibitor

(2014) Jaclyn L. Henderson et al.   JOURNAL OF MEDICINAL CHEMISTRY

In Vivo Imaging of Histone Deacetylases (HDACs) in the Central Nervous System and Major Peripheral Organs

(2014) Changning Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural biology of the LRRK2 GTPase and kinase domains: implications for regulation

(2014) Bernd K. Gilsbach et al.   Frontiers in Molecular Neuroscience

Design and Selection Parameters to Accelerate the Discovery of Novel Central Nervous System Positron Emission Tomography (PET) Ligands and Their Application in the Development of a Novel Phosphodiesterase 2A PET Ligand

(2013) Lei Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

The GTPase function of LRRK2

(2012) Jean-Marc Taymans   BIOCHEMICAL SOCIETY TRANSACTIONS

GSK2578215A; A potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor

(2012) Alastair D. Reith et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Characterization of TAE684 as a potent LRRK2 kinase inhibitor

(2012) Jinwei Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Current understanding of LRRK2 in Parkinson’s disease: biochemical and structural features and inhibitor design

(2012) Soumya Ray et al.   Future Medicinal Chemistry

Discovery of Highly Potent, Selective, and Brain-Penetrable Leucine-Rich Repeat Kinase 2 (LRRK2) Small Molecule Inhibitors

(2012) Anthony A. Estrada et al.   JOURNAL OF MEDICINAL CHEMISTRY

Roco kinase structures give insights into the mechanism of Parkinson disease-related leucine-rich-repeat kinase 2 mutations

(2012) B. K. Gilsbach et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Pharmacological Rescue of Mitochondrial Deficits in iPSC-Derived Neural Cells from Patients with Familial Parkinson's Disease

(2012) O. Cooper et al.   Science Translational Medicine

A Rat Model of Progressive Nigral Neurodegeneration Induced by the Parkinson's Disease-Associated G2019S Mutation in LRRK2

(2011) J. Dusonchet et al.   JOURNAL OF NEUROSCIENCE

Dopaminergic Neuronal Loss, Reduced Neurite Complexity and Autophagic Abnormalities in Transgenic Mice Expressing G2019S Mutant LRRK2

(2011) David Ramonet et al.   PLoS One

Using an in vitro cytotoxicity assay to aid in compound selection for in vivo safety studies

(2010) Nigel Greene et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

New Substructure Filters for Removal of Pan Assay Interference Compounds (PAINS) from Screening Libraries and for Their Exclusion in Bioassays

(2010) Jonathan B. Baell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibitors of leucine-rich repeat kinase-2 protect against models of Parkinson's disease

(2010) Byoung Dae Lee et al.   NATURE MEDICINE

LRRK2-mediated neurodegeneration and dysfunction of dopaminergic neurons in a Caenorhabditis elegans model of Parkinson's disease

(2010) Chen Yao et al.   NEUROBIOLOGY OF DISEASE

Impaired dopaminergic neurotransmission and microtubule-associated protein tau alterations in human LRRK2 transgenic mice

(2010) H.L. Melrose et al.   NEUROBIOLOGY OF DISEASE

LRRK2 enhances oxidative stress-induced neurotoxicity via its kinase activity

(2009) Hye Young Heo et al.   EXPERIMENTAL CELL RESEARCH

LRRK2 in Parkinson’s disease: biochemical functions

(2009) Vasanti S. Anand et al.   FEBS Journal

LRRK2 Modulates Vulnerability to Mitochondrial Dysfunction in Caenorhabditis elegans

(2009) S. Saha et al.   JOURNAL OF NEUROSCIENCE

Synthesis of11C,18F,15O, and13N Radiolabels for Positron Emission Tomography

(2008) Philip W. Miller et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Identification of compounds that inhibit the kinase activity of leucine-rich repeat kinase 2

(2008) Jason P. Covy et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

LRRK2in Parkinson's disease – drawing the curtain of penetrance: a commentary

(2008) Rejko Krüger   BMC Medicine

Molecular Imaging with PET

(2008) Simon M. Ametamey et al.   CHEMICAL REVIEWS

Molecular imaging in drug development

(2008) Jürgen K. Willmann et al.   NATURE REVIEWS DRUG DISCOVERY

A Drosophila model for LRRK2-linked parkinsonism

(2008) Z. Liu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA