Reevaluating the substrate specificity of the L-type amino acid transporter (LAT1) was written by Chien, Huan-Chieh;Colas, Claire;Finke, Karissa;Springer, Seth;Stoner, Laura;Zur, Arik A.;Venteicher, Brooklynn;Campbell, Jerome;Hall, Colton;Flint, Andrew;Augustyn, Evan;Hernandez, Christopher;Heeren, Nathan;Hansen, Logan;Anthony, Abby;Bauer, Justine;Fotiadis, Dimitrios;Schlessinger, Avner;Giacomini, Kathleen M.;Thomas, Allen A.. And the article was included in Journal of Medicinal Chemistry in 2018.Recommanded Product: 35065-86-2 This article mentions the following:
The L-type amino acid transporter 1 (LAT1, SLC7A5) transports essential amino acids across the blood-brain barrier (BBB) and into cancer cells. To utilize LAT1 for drug delivery, potent amino acid promoieties are desired, as prodrugs must compete with millimolar concentrations of endogenous amino acids. To better understand ligand-transporter interactions that could improve potency, we developed structural LAT1 models to guide the design of substituted analogs of phenylalanine and histidine. Furthermore, we evaluated the structure-activity relationship (SAR) for both enantiomers of naturally occurring LAT1 substrates. Analogs were tested in cis-inhibition and trans-stimulation cell assays to determine potency and uptake rate. Surprisingly, LAT1 can transport amino acid-like substrates with wide-ranging polarities including those containing ionizable substituents. Addnl., the rate of LAT1 transport was generally nonstereoselective even though enantiomers likely exhibit different binding modes. Our findings have broad implications to the development of new treatments for brain disorders and cancer. In the experiment, the researchers used many compounds, for example, 3-Bromophenyl acetate (cas: 35065-86-2Recommanded Product: 35065-86-2).
3-Bromophenyl acetate (cas: 35065-86-2) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.Recommanded Product: 35065-86-2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary