The essential role for aromatic cluster in the β3 adrenergic receptor.

ABSTRACT:

Aim

To explore the function of the conserved aromatic cluster F213(5.47), F308(6.51), and F309(6.52) in human β3 adrenergic receptor (hβ3AR).

Methods

Point mutation technology was used to produce plasmid mutations of hβ3AR. HEK-293 cells were transiently co-transfected with the hβ3AR (wild-type or mutant) plasmids and luciferase reporter vector pCRE-luc. The expression levels of hβ3AR in the cells were determined by Western blot analysis. The constitutive signalling and the signalling induced by the β3AR selective agonist, BRL (BRL37344), were then evaluated. To further explore the interaction mechanism between BRL and β3AR, a three-dimensional complex model of β3AR and BRL was constructed by homology modelling and molecular docking.

Results

For F308(6.51), Ala and Le

SUBMITTER: Cai HY 

PROVIDER: S-EPMC4011317 | biostudies-literature | 2012 Aug

REPOSITORIES: biostudies-literature