| Literature DB >> 7518678 |
K Tamura1, T Fujimura, K Iwasaki, S Sakuma, T Fujitsu, K Nakamura, K Shimomura, T Kuno, C Tanaka, M Kobayashi.
Abstract
Tacrolimus(FK506) is a strong immuno-suppressant and shows its activity through inhibiting IL-2 mRNA transcription by forming pentameric complex with intracellular receptor(FK506 binding protein 12 kDa or FKBP12), Ca2+, calmodulin, and calcineurin. Here, we report the binding activity to FKBP12, the pentameric complex formation and Con-A response inhibiting activities of 7 metabolites. C15-demethylated metabolite(M-3) needed higher quantity to compete in Con-A assay and in pentamer formation assay, although it binds more strongly to FKBP12. The result suggests that the ability to form a pentameric complex is not a two step reaction with the first binding to FKBP12, but a single step reaction by components for the pentamer formation.Entities:
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Year: 1994 PMID： 7518678 DOI： 10.1006/bbrc.1994.1947
Source DB: PubMed Journal: Biochem Biophys Res Commun ISSN： 0006-291X Impact factor: 3.575