| RRC ID |
42838
|
| 著者 |
Onoue S, Liu B, Nemoto Y, Hirose M, Yajima T.
|
| タイトル |
Chemical synthesis and application of C-terminally 5-carboxyfluorescein-labelled thymopentin as a fluorescent probe for thymopoietin receptor.
|
| ジャーナル |
Anal Sci
|
| 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.
|
| 巻・号 |
22(12)
|
| ページ |
1531-5
|
| 公開日 |
2006-12-1
|
| DOI |
10.2116/analsci.22.1531
|
| PII |
JST.JSTAGE/analsci/22.1531
|
| PMID |
17159311
|
| MeSH |
Animals
Cell Line, Tumor
Fluoresceins
Fluorescent Dyes
Humans
Ligands
Peptide Fragments / pharmacology
Receptors, Peptide / analysis*
Receptors, Peptide / antagonists & inhibitors
Receptors, Peptide / chemistry
Secretin / pharmacology
Structure-Activity Relationship
Swine
Thymopentin* / chemistry
Thymopentin* / pharmacology
Thymopoietins / pharmacology
|
| IF |
2.049
|
| 引用数 |
6
|
|
WOS 分野
|
CHEMISTRY, ANALYTICAL
|
| リソース情報 |
| ヒト・動物細胞 |
MOLT-4(RCB0206) |
