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PMID:8626574

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Citation

Nagayama, Y, Tanaka, K, Hara, T, Namba, H, Yamashita, S, Taniyama, K and Niwa, M (1996) Involvement of G protein-coupled receptor kinase 5 in homologous desensitization of the thyrotropin receptor. J. Biol. Chem. 271:10143-8

Abstract

Homologous desensitization of G protein-coupled receptors involves agonist-dependent phosphorylation of receptors by G protein-coupled receptor kinases (GRKs). To identify GRK(s) that play a role in homologous desensitization of the thyrotropin (TSH) receptor, thyroid cDNA was amplified by polymerase chain reaction using degenerate oligonucleotide primers from highly conserved regions in GRK family. GRK5 is found in the predominant isoform expressed in the thyroid. Rat GRK5 cDNA was then isolated, which encodes a 590-amino acid protein with 95% homology to human and bovine homologs. Northern blot identified GRK5 mRNA of approximately 3, 8, and 10 kilobases with highest expression levels in lung > heart, kidney, colon > thyroid. In functional studies using a normal rat thyroid FRTL5 cells, overexpression of GRK5 by transfecting the plasmid capable of expressing the sense GRK5 RNA suppressed basal cAMP levels and augmented the extent of TSH receptor desensitization, whereas suppression of endogenous GRK5 expression by transfecting the antisense GRK5 construct increased basal cAMP levels and attenuated the extent of receptor desensitization. Although exogenously overexpressed GRK6 also enhanced TSH receptor desensitization, we conclude that GRK5, the predominant GRK isoform in the thyroid, appears to be mainly involved in homologous desensitization of the TSH receptor.

Links

PubMed

Keywords

Amino Acid Sequence; Animals; Base Sequence; DNA Primers/chemistry; Down-Regulation; G-Protein-Coupled Receptor Kinase 5; G-Protein-Coupled Receptor Kinases; GTP-Binding Proteins/metabolism; Gene Expression; Humans; Molecular Sequence Data; Protein-Serine-Threonine Kinases; RNA, Messenger/genetics; Rats; Receptor Protein-Tyrosine Kinases/genetics; Receptor Protein-Tyrosine Kinases/metabolism; Receptors, Thyrotropin/metabolism; Signal Transduction; Thyroid Gland/metabolism

Significance

Annotations

Gene product Qualifier GO Term Evidence Code with/from Aspect Extension Notes Status

RAT:GRK5

enables

GO:0004703: G protein-coupled receptor kinase activity

ECO:0000305: curator inference used in manual assertion

GO:0002029

F

Seeded From UniProt

complete

RAT:GRK5

involved_in

GO:0008277: regulation of G protein-coupled receptor signaling pathway

ECO:0000315: mutant phenotype evidence used in manual assertion

P

Seeded From UniProt

complete

RAT:GRK5

involved_in

GO:0002029: desensitization of G protein-coupled receptor signaling pathway

ECO:0000315: mutant phenotype evidence used in manual assertion

P

Seeded From UniProt

complete

HUMAN:GRK5

involved_in

GO:0007188: adenylate cyclase-modulating G protein-coupled receptor signaling pathway

ECO:0000304: author statement supported by traceable reference used in manual assertion

P

Seeded From UniProt

complete


See also

References

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