TY - JOUR
T1 - A reduction of epidermal growth factor receptor is involved in brefelamide-induced inhibition of phosphorylation of ERK in human astrocytoma cells
AU - Honma, Shigeyoshi
AU - Saito, Masaki
AU - Kikuchi, Haruhisa
AU - Saito, Yoshinori
AU - Oshima, Yoshiteru
AU - Nakahata, Norimichi
AU - Yoshida, Makoto
PY - 2009/8/15
Y1 - 2009/8/15
N2 - 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 Tyr1068, 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.
AB - 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 Tyr1068, 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.
KW - Astrocytoma
KW - Brefelamide
KW - Epidermal growth factor receptor
KW - Extracellular signal-regulated kinase
KW - Growth inhibition
UR - http://www.scopus.com/inward/record.url?scp=67749111371&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=67749111371&partnerID=8YFLogxK
U2 - 10.1016/j.ejphar.2009.06.030
DO - 10.1016/j.ejphar.2009.06.030
M3 - Article
C2 - 19559020
AN - SCOPUS:67749111371
SN - 0014-2999
VL - 616
SP - 38
EP - 42
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
IS - 1-3
ER -