Development and biological evaluation of[
| Autor: | Noeen, Malik, Rick, Kornelsen, Siobhan, McCormick, Nadine, Colpo, Helen, Merkens, Shreya, Bendre, Francois, Benard, Vesna, Sossi, Ralf, Schirrmacher, Paul, Schaffer |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Male
Dose-Response Relationship Drug Molecular Structure Leucine-Rich Repeat Serine-Threonine Protein Kinase-2 Rats Molecular Docking Simulation Rats Sprague-Dawley Mice Structure-Activity Relationship Drug Development Positron-Emission Tomography Animals Humans Tissue Distribution Protein Kinase Inhibitors |
| Zdroj: | European journal of medicinal chemistry. 211 |
| ISSN: | 1768-3254 |
| Popis: | Among all genetic mutations of LRRK2, the G2019S mutation is the most commonly associated with the late-onset of Parkinson's disease (PD). Hence, one potential therapeutic approach is to block the hyperactivity of mutated LRRK2 induced by kinase inhibition. To date, only a few LRRK2 kinase inhibitors have been tested for in vivo quantification of target engagement by positron emission tomography (PET). In this study, we performed biological evaluations of two radiolabeled kinase inhibitors i.e. [Radiosyntheses of [Radiofluorinations resulted in radiochemical yields (RCYs) of 25 ± 1.3% (n = 6) ([In the presence of GNE-0877 as a blocking agent, the specific binding of [ |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect