Biochemical and Biophysical Research Communications
Key amino acids for differential coupling of α1-adrenergic receptor subtypes to Gs☆
Section snippets
Materials and methods
Materials. The following drugs and reagents were used: 2-[2-(4-hydroxy-3-[125I]iodo-phenyl)ethylaminomethyl]-α-tetralone ([125I]HEAT) (specific activity, 2200 Ci mmol−1; New England Nuclear, Boston, MA, USA); [methyl-3H]thymidine (specific activity, 2 Ci mmol−1; New England Nuclear, Boston, MA, USA); phentolamine mesylate (Novartis Pharmaceutical, Summit, NJ, USA); (−)-noradrenaline bitartrate, phenylephrine, dl-propranolol hydrochloride, and 3-isobutyl-1-methylxanthine (IBMX) (Sigma Chemical,
Chimeric receptors
To determine the region responsible for the α1-AR subtype-specific differential effects on cell proliferation, we first constructed a series of α1A/α1D-CRs. The structures of these chimeras (AAD, ADA, ADD, DDA, DAD, and DAA) are shown in Fig. 2. They consist of three components that belong to either the wild-type humanα1A-AR or α1D-AR. The first component is from the amino-terminal extracellular tail to TMD V. The second component is the ICL III and the third component is from TMD III to the
Acknowledgements
This investigation was partially supported by research grants from the Scientific Fund of the Ministry of Education, Science and Culture of Japan, the Japan Health Science Foundation, and the Ministry of Human Health and Welfare.
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Abbreviations: AR, α1-adrenergic receptor; CHO, Chinese hamster ovary; CHOα1A, CHO cells stably expressing cloned α1A-AR; CHOα1B, CHO cells stably expressing cloned α1B-AR; CHOα1D, CHO cells stably expressing cloned α1D-AR; NA, noradrenaline; α1A/α1D-CR, chimeric α1A and α1D-AR; CHOα1A/α1D-CR, CHO cells stably expressing α1A/α1D-CR; HEK, human embryonic kidney; TMD, transmembrane domain; ICL, intracellular loop; MAPK, mitogen-activated protein kinase; FCS, fetal calf serum.