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Cloning and expression of three isoforms of the human EP 3 prostanoid receptor
Author(s) -
Adam Mohamed,
Boie Yves,
Rushmore Thomas H.,
Müller Gretchen,
Bastien Lison,
McKee Katherine T.,
Metters Kathleen M.,
Abramovitz Mark
Publication year - 1994
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(94)80358-7
Subject(s) - cloning (programming) , prostanoid , gene isoform , receptor , microbiology and biotechnology , molecular cloning , expression (computer science) , computational biology , chemistry , biology , genetics , gene expression , computer science , gene , programming language
Functional cDNA clones coding for three isoforms of the human prostaglandin E receptor EP 3 subtype have been isolated from kidney and uterus cDNA libraries. The three isoforms, designated hEP 3‐I , hEP 3‐II and hEP 3‐III , have open reading frames corresponding to 390, 388 and 365 amino acids, respectively. They differ only in the length and amino acid composition of their carboxy‐terminal regions, beginning at position 360. The human EP 3 receptor has seven predicted transmembrane spanning domains and therefore belongs to the G‐protein‐coupled receptor family. The rank order of potency for prostaglandins and related analogs in competition for [ 3 H]PGE 2 specific binding to membranes prepared from transfected COS cells was comparable for all three isoforms, and as predicted for the EP 3 receptor, with PGE 2 = PGE 1 > PGF 2α = iloprost > PGD 2 ⪢ U46619. In addition, the EP 3 ‐selective agonist MB28767 was a potent competing ligand with an IC 50 value of 0.3 nM, whereas the EP 1 ‐selective antagonist AH6909 gave IC 50 values of 2–7 μM and the EP 2 ‐selective agonist butaprost was inactive. In summary, we have cloned three isoforms of the human EP, receptor having comparable ligand binding properties.