Molecular cloning and characterization of rat P2Y4 nucleotide receptor
Molecular cloning and characterization of rat P2Y4 nucleotide receptor
An intronless open reading frame encoding a protein (361aa in length) was isolated from a rat genomic library probed with a DNA fragment from rat heart. This protein showed 83% sequence identity with the human P2Y4 (hP2Y4) receptor and represents a homologue of the human pyrimidinoceptor. However, the rP2Y4 receptor is not selective for uridine nucleotides and, instead, shows an agonist potency order of ITP=ATP=ADP(pure)=UTP=ATPγS=2-MeSATP=Ap4A>UDP(pure). ADP, ATPγS, 2-MeSATP and UDP are partial agonists. Thus, in terms of agonist profile, rP2Y4 is more like the P2U receptor subtype. The rP2Y4 receptor was reversibly antagonized by Reactive blue 2 but not by suramin which, otherwise, inhibits the hP2Y2 receptor (a known P2U receptor). Thus, rP2Y4 and the P2Y2 subtype appear to be structurally distinct forms of the P2U receptor (where ATP and UTP are equi-active) but can be distinguished as suramin-insensitive and suramin-sensitive P2U receptors, respectively.
428-430
Bogdanov, YD
0c970999-e191-4f1b-90d9-7bf25a5d5b4b
Wildman, SS
2875ccb4-7bf0-4826-93b5-6db474034a4b
Clements, MP
500394f2-42fc-49e2-b2b3-49ef8394b270
King, BF
61b71ca2-197e-4700-84bb-0e4696a5a1d1
Burnstock, G
01b80f44-c92a-4890-aa19-3a907695af8b
1 June 1998
Bogdanov, YD
0c970999-e191-4f1b-90d9-7bf25a5d5b4b
Wildman, SS
2875ccb4-7bf0-4826-93b5-6db474034a4b
Clements, MP
500394f2-42fc-49e2-b2b3-49ef8394b270
King, BF
61b71ca2-197e-4700-84bb-0e4696a5a1d1
Burnstock, G
01b80f44-c92a-4890-aa19-3a907695af8b
Bogdanov, YD, Wildman, SS, Clements, MP, King, BF and Burnstock, G
(1998)
Molecular cloning and characterization of rat P2Y4 nucleotide receptor.
British Journal of Pharmacology, 124 (3), .
(doi:10.1038/sj.bjp.0701880).
Abstract
An intronless open reading frame encoding a protein (361aa in length) was isolated from a rat genomic library probed with a DNA fragment from rat heart. This protein showed 83% sequence identity with the human P2Y4 (hP2Y4) receptor and represents a homologue of the human pyrimidinoceptor. However, the rP2Y4 receptor is not selective for uridine nucleotides and, instead, shows an agonist potency order of ITP=ATP=ADP(pure)=UTP=ATPγS=2-MeSATP=Ap4A>UDP(pure). ADP, ATPγS, 2-MeSATP and UDP are partial agonists. Thus, in terms of agonist profile, rP2Y4 is more like the P2U receptor subtype. The rP2Y4 receptor was reversibly antagonized by Reactive blue 2 but not by suramin which, otherwise, inhibits the hP2Y2 receptor (a known P2U receptor). Thus, rP2Y4 and the P2Y2 subtype appear to be structurally distinct forms of the P2U receptor (where ATP and UTP are equi-active) but can be distinguished as suramin-insensitive and suramin-sensitive P2U receptors, respectively.
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More information
Published date: 1 June 1998
Additional Information:
1998 British Pharmacological Society
Identifiers
Local EPrints ID: 469841
URI: http://eprints.soton.ac.uk/id/eprint/469841
ISSN: 0007-1188
PURE UUID: 1ec0cda1-6096-41b8-a9c5-990e79869ccd
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Date deposited: 27 Sep 2022 16:37
Last modified: 17 Mar 2024 03:37
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Author:
SS Wildman
Author:
MP Clements
Author:
BF King
Author:
G Burnstock
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