Identification and Profiling of a Selective and Brain Penetrant Radioligand for in Vivo Target Occupancy Measurement of Casein Kinase 1 (CK1) Inhibitors

Author:

Wager Travis T.1ORCID,Galatsis Paul1,Chandrasekaran Ramalakshmi Y.12,Butler Todd W.12,Li Jianke12,Zhang Lei1,Mente Scot1,Subramanyam Chakrapani12,Liu Shenping1,Doran Angela C.3,Chang Cheng3,Fisher Katherine4,Grimwood Sarah4,Hedde Joseph R.4,Marconi Michael4,Schildknegt Klaas5

Affiliation:

1. Worldwide Medicinal Chemistry, Pfizer Worldwide Research and Development, 1 Portland, Cambridge, Massachusetts 02139, United States

2. Worldwide Medicinal Chemistry, Pfizer Worldwide Research and Development, 558 Eastern Point Rd, Groton, Connecticut 06340, United States

3. Pharmacokinetics, Dynamics, and Metabolism, Pfizer Worldwide Research and Development, 558 Eastern Point Rd, Groton, Connecticut 06340, United States

4. Internal Medicine Research Unit, Pfizer Worldwide Research and Development, 1 Portland, Cambridge, Massachusetts 02139, United States

5. Chemical Research and Development, Pharmaceutical Sciences, Pfizer Worldwide Research and Development, 558 Eastern Point Rd, Groton, Connecticut 06340, United States

Publisher

American Chemical Society (ACS)

Subject

Cell Biology,Cognitive Neuroscience,Physiology,Biochemistry,General Medicine

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1. CK1δ/ε kinases regulate TDP-43 phosphorylation and are therapeutic targets for ALS-related TDP-43 hyperphosphorylation;Neurobiology of Disease;2024-06

2. Casein kinase (CK) inhibitors;Current Molecular Targets of Heterocyclic Compounds for Cancer Therapy;2024

3. Challenges and Perspectives in Target Identification and Mechanism Illustration for Chinese Medicine;Chinese Journal of Integrative Medicine;2023-02-21

4. Protein kinase inhibitors as therapeutics in neurodegenerative and psychiatric disorders;Receptor Tyrosine Kinases in Neurodegenerative and Psychiatric Disorders;2023

5. POSITRON EMISSION TOMOGRAPHY NEUROIMAGING IN DRUG DISCOVERY AND DEVELOPMENT;2022 Medicinal Chemistry Reviews;2022-12-21

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