%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 }