Human breast cancer cell line MDA-MB-231 expresses endogenous A2B
adenosine receptors mediating a Ca2+ signal
M. Panjehpour, M. Castro, and K. Klotz. Br J Pharmacol, 145 (2):
211-8(May 2005)Panjehpour, Mojtaba Castro, Marian Klotz, Karl-Norbert Comparative
Study England British journal of pharmacology Br J Pharmacol. 2005
May;145(2):211-8..
Abstract
1 Two human breast cancer cell lines, MCF-7 and MDA-MB-231, were screened
for the presence of functionally significant adenosine receptor subtypes.
2 MCF-7 cells did not contain adenosine receptors as judged by the
lack of an effect of nonselective agonists on adenylyl cyclase activity
or intracellular Ca(2+) levels. MDA-MB-231 cells showed both a stimulation
of adenylyl cyclase and a PLC-dependent increase in intracellular
Ca(2+) in response to nonselective adenosine receptor agonists. 3
Both adenosine-mediated responses in MDA-MB-231 cells were observed
with the nonselective agonists 5'-N-ethylcarboxamidoadenosine (NECA)
and 2-(3-hydroxy-3-phenyl)propyn-1-yladenosine-5'-N-ethyluronamide
(PHPNECA), but no responses were observed with agonists selective
for A(1), A(2A) or A(3) adenosine receptors. The Ca(2+) signal was
antagonized by 8-cyclopentyl-1,3-dipropylxanthine (DPCPX) and the
nonselective antagonist 9-ethyl-8-furyladenine (ANR 152), but not
by A(2A) or A(3) selective compounds. 4 In radioligand binding with
2-(3)H(4-(2-7-amino-2-(2-furyl)1,2,4triazolo2,3-a1,3,5triazin-5-y
laminoethyl)phenol) ((3)HZM 241385), a specific binding site with
a K(D) value of 87 nM and a B(max) value of 1600 fmol mg(-1) membrane
protein was identified in membranes from MDA-MB-231 cells. 5 The
pharmacological characteristics provide evidence for the expression
of an A(2B) adenosine receptor in MDA-MB-231 cells, which not only
mediates a stimulation of adenylyl cyclase but also couples to a
PLC-dependent Ca(2+) signal, most likely via G(q/11). The A(2B) receptor
in such cancer cells may serve as a target to control cell growth
and proliferation. 6 The selective expression of high levels of endogenous
A(2B) receptors coupled to two signaling pathways make MDA-MB-231
cells a suitable model for this human adenosine receptor subtype.
Panjehpour, Mojtaba Castro, Marian Klotz, Karl-Norbert Comparative
Study England British journal of pharmacology Br J Pharmacol. 2005
May;145(2):211-8.
%0 Journal Article
%1 Panjehpour2005
%A Panjehpour, M.
%A Castro, M.
%A Klotz, K. N.
%D 2005
%J Br J Pharmacol
%K *Calcium A2B/agonists/*biosynthesis Activation Adenosine Adenosine-5'-(N-ethylcarboxamide)/pharmacology Adenylate Assay Breast Cell Cyclase/metabolism Enzyme Female Hormone-Dependent Humans Line, Neoplasms Neoplasms, Radioligand Signaling Tumor/*metabolism Receptor
%N 2
%P 211-8
%T Human breast cancer cell line MDA-MB-231 expresses endogenous A2B
adenosine receptors mediating a Ca2+ signal
%U http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=15753948
%V 145
%X 1 Two human breast cancer cell lines, MCF-7 and MDA-MB-231, were screened
for the presence of functionally significant adenosine receptor subtypes.
2 MCF-7 cells did not contain adenosine receptors as judged by the
lack of an effect of nonselective agonists on adenylyl cyclase activity
or intracellular Ca(2+) levels. MDA-MB-231 cells showed both a stimulation
of adenylyl cyclase and a PLC-dependent increase in intracellular
Ca(2+) in response to nonselective adenosine receptor agonists. 3
Both adenosine-mediated responses in MDA-MB-231 cells were observed
with the nonselective agonists 5'-N-ethylcarboxamidoadenosine (NECA)
and 2-(3-hydroxy-3-phenyl)propyn-1-yladenosine-5'-N-ethyluronamide
(PHPNECA), but no responses were observed with agonists selective
for A(1), A(2A) or A(3) adenosine receptors. The Ca(2+) signal was
antagonized by 8-cyclopentyl-1,3-dipropylxanthine (DPCPX) and the
nonselective antagonist 9-ethyl-8-furyladenine (ANR 152), but not
by A(2A) or A(3) selective compounds. 4 In radioligand binding with
2-(3)H(4-(2-7-amino-2-(2-furyl)1,2,4triazolo2,3-a1,3,5triazin-5-y
laminoethyl)phenol) ((3)HZM 241385), a specific binding site with
a K(D) value of 87 nM and a B(max) value of 1600 fmol mg(-1) membrane
protein was identified in membranes from MDA-MB-231 cells. 5 The
pharmacological characteristics provide evidence for the expression
of an A(2B) adenosine receptor in MDA-MB-231 cells, which not only
mediates a stimulation of adenylyl cyclase but also couples to a
PLC-dependent Ca(2+) signal, most likely via G(q/11). The A(2B) receptor
in such cancer cells may serve as a target to control cell growth
and proliferation. 6 The selective expression of high levels of endogenous
A(2B) receptors coupled to two signaling pathways make MDA-MB-231
cells a suitable model for this human adenosine receptor subtype.
@article{Panjehpour2005,
abstract = {1 Two human breast cancer cell lines, MCF-7 and MDA-MB-231, were screened
for the presence of functionally significant adenosine receptor subtypes.
2 MCF-7 cells did not contain adenosine receptors as judged by the
lack of an effect of nonselective agonists on adenylyl cyclase activity
or intracellular Ca(2+) levels. MDA-MB-231 cells showed both a stimulation
of adenylyl cyclase and a PLC-dependent increase in intracellular
Ca(2+) in response to nonselective adenosine receptor agonists. 3
Both adenosine-mediated responses in MDA-MB-231 cells were observed
with the nonselective agonists 5'-N-ethylcarboxamidoadenosine (NECA)
and 2-(3-hydroxy-3-phenyl)propyn-1-yladenosine-5'-N-ethyluronamide
(PHPNECA), but no responses were observed with agonists selective
for A(1), A(2A) or A(3) adenosine receptors. The Ca(2+) signal was
antagonized by 8-cyclopentyl-1,3-dipropylxanthine (DPCPX) and the
nonselective antagonist 9-ethyl-8-furyladenine (ANR 152), but not
by A(2A) or A(3) selective compounds. 4 In radioligand binding with
[2-(3)H](4-(2-[7-amino-2-(2-furyl)[1,2,4]triazolo[2,3-a][1,3,5]triazin-5-y
lamino]ethyl)phenol) ([(3)H]ZM 241385), a specific binding site with
a K(D) value of 87 nM and a B(max) value of 1600 fmol mg(-1) membrane
protein was identified in membranes from MDA-MB-231 cells. 5 The
pharmacological characteristics provide evidence for the expression
of an A(2B) adenosine receptor in MDA-MB-231 cells, which not only
mediates a stimulation of adenylyl cyclase but also couples to a
PLC-dependent Ca(2+) signal, most likely via G(q/11). The A(2B) receptor
in such cancer cells may serve as a target to control cell growth
and proliferation. 6 The selective expression of high levels of endogenous
A(2B) receptors coupled to two signaling pathways make MDA-MB-231
cells a suitable model for this human adenosine receptor subtype.},
added-at = {2010-12-14T18:12:02.000+0100},
author = {Panjehpour, M. and Castro, M. and Klotz, K. N.},
biburl = {https://www.bibsonomy.org/bibtex/2beb051f87546f22b9182e9d6e38ffdcd/pharmawuerz},
endnotereftype = {Journal Article},
interhash = {5049cd0db093dae5d77ad76750d9e812},
intrahash = {beb051f87546f22b9182e9d6e38ffdcd},
issn = {0007-1188 (Print) 0007-1188 (Linking)},
journal = {Br J Pharmacol},
keywords = {*Calcium A2B/agonists/*biosynthesis Activation Adenosine Adenosine-5'-(N-ethylcarboxamide)/pharmacology Adenylate Assay Breast Cell Cyclase/metabolism Enzyme Female Hormone-Dependent Humans Line, Neoplasms Neoplasms, Radioligand Signaling Tumor/*metabolism Receptor},
month = May,
note = {Panjehpour, Mojtaba Castro, Marian Klotz, Karl-Norbert Comparative
Study England British journal of pharmacology Br J Pharmacol. 2005
May;145(2):211-8.},
number = 2,
pages = {211-8},
shorttitle = {Human breast cancer cell line MDA-MB-231 expresses endogenous A2B
adenosine receptors mediating a Ca2+ signal},
timestamp = {2010-12-14T18:20:21.000+0100},
title = {Human breast cancer cell line MDA-MB-231 expresses endogenous A2B
adenosine receptors mediating a Ca2+ signal},
url = {http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=15753948},
volume = 145,
year = 2005
}