The carboxyl terminus of mouse delta-opioid receptor is not required for agonist-dependent activation.
The pharmacological effects caused by use of opiate are exerted through the opioid receptors (ORs). ORs couple to the inhibitory G protein (Gi) and result in decreased cAMP levels upon activation by specific agonists. To initiate study of the structure-function relationship during this process, we first ectopically expressed the wild-type delta OR and a C-terminally truncated mutant in CHO cells to investigate the necessity of its C-terminus. The binding potency of both the wild-type and truncated delta ORs to ligands including DPDPE, DSLET, DAGO, and U-50488 was compared. Their membrane localization and ability to mediate signal transduction were also studied. We conclude that the C-terminus of delta OR is not essential for plasma membrane targeting, ligand specificity, and agonist-dependent activation.
Zhu
X
X
Shanghai Research Center of Life Sciences, Peoples' Republic of China.
Wang
C
C
Cheng
Z
Z
Wu
Y
Y
Zhou
D
D
Pei
G
G
D000595:Amino Acid Sequence / Q000502:physiology*; D000818:Animals; D001692:Biological Transport; D016466:CHO Cells; D002460:Cell Line; D006224:Cricetinae; D004174:Diprenorphine / Q000378:metabolism; D020881:Enkephalin, D-Penicillamine (2,5)-; D004743:Enkephalin, Leucine / Q000031:analogs & derivatives / Q000378:metabolism; D004745:Enkephalins / Q000378:metabolism; D006801:Humans; D007668:Kidney / Q000196:embryology; D051379:Mice; D017465:Receptors, Opioid, delta / Q000737:chemistry* / Q000502:physiology*; D015398:Signal Transduction; D014162:Transfection
D004745:Enkephalins; D017465:Receptors, Opioid, delta; D004174:Diprenorphine; D004743:Enkephalin, Leucine; C034318:enkephalin, Ser(2), Leu(5), Thr(6)-; D020881:Enkephalin, D-Penicillamine (2,5)-