Distinct expression and ligand-binding profiles of two constitutively active GPR17 splice variants.

ABSTRACT:

Background and purpose

In humans and non-human primates, the 7TM receptor GPR17 exists in two isoforms differing only by the length of the N-terminus. Of these, only the short isoform has previously been characterized. Hence, we investigated gene expression and ligand-binding profiles of both splice variants and furthermore uncovered and characterized constitutive activity of both isoforms.

Experimental approach

Expression levels of the hGPR17 isoforms were determined in several brain regions as well as heart and kidney using quantitative RT-PCR. A CREB reporter assay and [(35)S]-GTPgammaS binding were employed to assess the constitutive activity and the activation by UDP, UDP-glucose and -galactose and the cysteinyl leukotrienes LTC(4) and LTD(4). Leukotriene binding and in

SUBMITTER: Benned-Jensen T 

PROVIDER: S-EPMC2839267 | biostudies-literature | 2010 Mar

REPOSITORIES: biostudies-literature