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Chemical Synthesis and Application of C-Terminally 5-Carboxyfluorescein-labelled Thymopentin as a Fluorescent Probe for Thymopoietin Receptor
- Source :
- Analytical Sciences. 22:1531-1535
- Publication Year :
- 2006
- Publisher :
- Springer Science and Business Media LLC, 2006.
-
Abstract
- Thymopentin (TP5) is a synthetic pentapeptide fragment, which corresponds to position 32 - 36 of thymic polypeptide thymopoietin. Thymopoietin and TP5 display a variety of biological functions, including phenotypic differentiation of T cells and the regulation of immune systems. Previous chemical modification experiments suggested that there was an absolute requirement for N-terminal amino acids to maintain the biological activity of TP5. On the basis of this structure-activity relationship, we designed and synthesized the C-terminally 5-carboxyfluorescein-coupled TP5 (TP5-FAM) as a fluorescent probe for thymopoietin receptor. TP5-FAM could bind to the membrane of human lymphoid cell lines, MOLT-4 cells, in which the thymopoietin receptor is expressed. The binding is specific and saturable (K(d) = 33 microM). TP5 and human splenopentin are nearly equipotent inhibitors of TP5-FAM binding to the thymopoietin receptor, but porcine secretin did not show any significant inhibition of TP5-FAM binding to MOLT-4 cells. Thus, TP5-FAM is suggested to be a potent and biologically active ligand that would be useful for studying the binding and functional characteristics of the human thymopoietin receptor.
- Subjects :
- Receptors, Peptide
Swine
Thymopoietins
Ligands
Pentapeptide repeat
Analytical Chemistry
Structure-Activity Relationship
Secretin
Cell Line, Tumor
medicine
Animals
Humans
Structure–activity relationship
Thymopentin
Thymopoietin
Receptor
Fluorescent Dyes
chemistry.chemical_classification
biology
Chemistry
Biological activity
Fluoresceins
Peptide Fragments
Amino acid
Biochemistry
Cell culture
biology.protein
medicine.drug
Subjects
Details
- ISSN :
- 13482246 and 09106340
- Volume :
- 22
- Database :
- OpenAIRE
- Journal :
- Analytical Sciences
- Accession number :
- edsair.doi.dedup.....5c6f0df4b595ad1d92ebedf54827068c