Iodinated Choline Transport-Targeted Tracers.
Pavel ŠvecZbyněk NovýJan KučkaMiloš PetříkOndrej SedlacekMartin KuchařBarbora LiškováMartina MedvedíkováKristýna KolouchováOndřej GroborzLenka LoukotováRafał Ł KonefałMarián HajdúchMartin HrubýPublished in: Journal of medicinal chemistry (2020)
We present a novel series of radioiodinated tracers and potential theranostics for diseases accompanied by pathological function of proteins involved in choline transport. Unlike choline analogues labeled with 11C or 18F that are currently used in the clinic, the iodinated compounds described herein are applicable in positron emission tomography, single-photon emission computed tomography, and potentially in therapy, depending on the iodine isotope selection. Moreover, favorable half-lives of iodine isotopes result in much less challenging synthesis by isotope exchange reaction. Six of the described compounds were nanomolar ligands, and the best compound possessed an affinity 100-fold greater than that of choline. Biodistribution data of 125I-labeled ligands in human prostate carcinoma bearing (PC-3) mice revealed two compounds with a biodistribution profile superior to that of [18F]fluorocholine.
Keyphrases
- positron emission tomography
- pet imaging
- computed tomography
- dual energy
- pet ct
- endothelial cells
- magnetic resonance imaging
- primary care
- image quality
- stem cells
- big data
- machine learning
- electronic health record
- cancer therapy
- magnetic resonance
- molecular docking
- gas chromatography
- mesenchymal stem cells
- bone marrow
- human health
- metabolic syndrome
- skeletal muscle
- solid state
- smoking cessation
- risk assessment