Abstract:
:Brefelamide is an aromatic amide isolated from Dictyostelium cellular slime molds. We found that brefelamide has a potent inhibitory growth effect measured by MTT assay in 1321N1 human astrocytoma cells. The inhibition was associated with reduced phosphorylation of extracellular signal-regulated kinase (ERK). Brefelamide inhibited epidermal growth factor (EGF)-induced phosphorylation of ERK in a concentration-dependent manner. Furthermore, brefelamide diminished EGF-induced phosphorylation of EGF receptor at Tyr(1068), a Grb2 binding site that leads to an activation of the Ras/Raf/ERK system. Brefelamide also reduced the expression level of the EGF receptor. These results suggest that one of the mechanisms of action of brefelamide is assumed to be inhibition of phosphorylation of ERK through a reduction of EGF receptor activity in 1321N1 human astrocytoma cells.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Honma S,Saito M,Kikuchi H,Saito Y,Oshima Y,Nakahata N,Yoshida Mdoi
10.1016/j.ejphar.2009.06.030subject
Has Abstractpub_date
2009-08-15 00:00:00pages
38-42issue
1-3eissn
0014-2999issn
1879-0712pii
S0014-2999(09)00545-7journal_volume
616pub_type
杂志文章abstract::We have described here the changes of the biophysical and pharmacological properties of the sarcolemmal ATP-sensitive K+ channels (KATP) of rat skeletal muscle fibres, occurring from an early postnatal period (5 days) to adulthood (210 days). The age-dependent changes of the mean current of the KATP channel (channel a...
journal_title:European journal of pharmacology
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