Amino acids labeled with [99mTc(CO)3]+ and recognized by the L-type amino acid transporter LAT1
| Autor: | Hector Knight, Paul Schmutz, Jae Kyoung Pak, Roger Alberto, John Mertens, Yu Liu, Matthias Bauwens |
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| Rok vydání: | 2006 |
| Předmět: |
chemistry.chemical_classification
Models Molecular Carbon Monoxide Molecular Structure Stereochemistry Technetium Large Neutral Amino Acid-Transporter 1 Transporter General Chemistry Conjugated system Biochemistry Small molecule Catalysis Amino acid Structure-Activity Relationship Colloid and Surface Chemistry chemistry Moiety Amino acid transporter Amino Acids Alkyl |
| Zdroj: | Journal of the American Chemical Society. 128(50) |
| ISSN: | 0002-7863 |
| Popis: | We have synthesized amino acids conjugated at the alpha-carbon through an alkyl spacer to a small tripod ligand. The tripod coordinates to the fac-[M(CO)3]+ moiety (M = Re, 99mTc). Depending on the lengths of the spacers, these metal complexes with pendent alpha-amino acids are recognized and transported by the l-type amino acid transporter LAT1. The best result was achieved with a butyl spacer. The Ki value of the corresponding complex is comparable to that of the artificial amino acid BCH. Efflux of [3H]-l-phenylalanine shows that the labeled amino acids do not only bind to the transporter but are transported into the cells. These are the first metal-labeled small molecules which are actively internalized to the intracellular space. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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