Orexin/hypocretin receptor chimaeras reveal structural features important for orexin peptide distinction |
| |
Authors: | Putula Jaana Turunen Pauli M Johansson Lisa Näsman Johnny Ra Runar Korhonen Laura Kukkonen Jyrki P |
| |
Institution: | Biochemistry and Cell Biology, Department of Veterinary Biosciences, University of Helsinki, Helsinki, Finland. |
| |
Abstract: | We wanted to analyze the basis for the distinction between OX(1) and OX(2) orexin receptors by the known agonists, orexin-A, orexin-B and Ala(11), D-Leu(15)-orexin-B, of which the latter two show some selectivity for OX(2). For this, chimaeric OX(1)/OX(2) and OX(2)/OX(1) orexin receptors were generated. The receptors were transiently expressed in HEK-293 cells, and potencies of the agonists to elicit cytosolic Ca(2+) elevation were measured. The results show that the N-terminal regions of the receptor are most important, and the exchange of the area from the C-terminal part of the transmembrane helix 2 to the transmembrane helix 4 is enough to lead to an almost total change of the receptor's ligand profile. |
| |
Keywords: | |
本文献已被 ScienceDirect PubMed 等数据库收录! |
|