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Papers In Press, published online ahead of print May 31, 2001
Department of Neurology, GlaxoSmithKline, Harlow, Essex CM19 5AW
Corresponding Author: David_C_Harrison{at}gsk.com
A novel human G protein-coupled receptor, named AXOR12, exhibiting 81% homology to the rat orphan receptor GPR54, was cloned from a human brain cDNA library. Heterologous expression of AXOR12 in mammalian cells permitted the identification of three surrogate agonist peptides, all with a common C-terminal amidated motif. High potency agonism, indicative of a cognate ligand, was evident from peptides derived from KiSS-1, a gene whose expression prevents metastasis in melanoma cells. Quantitative reverse transcriptase-polymerase chain reaction (RT-PCR) was used to study the expression of AXOR12 and KiSS-1 in a variety of tissues. Highest levels of expression of AXOR12 mRNA were observed in brain, pituitary gland and placenta. The highest levels of KiSS-1 gene expression were observed in placenta and brain. A polyclonal antibody raised to the C-terminus of AXOR12 was generated and used to show localization of the receptor to neurons in the cerebellum, cerebral cortex and brainstem. The biological significance of these expression patterns and the nature of the putative cognate ligand for AXOR12 are discussed.
J. Biol. Chem, 10.1074/jbc.M102743200
Submitted on March 28, 2001
Revised on May 23, 2001
Accepted on May 31, 2001
AXOR12: A novel human G protein-coupled receptor, activated by the peptide KiSS-1
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