Neuromedin U is a potent agonist at the orphan G protein-coupled receptor FM3
| Autor: | Nabil Elshourbagy, Jeffrey L. Mooney, Mcmillan Lynette Jane, Hsiao-Ling Wu, Sharon Butler, Angela M. Smith, Laura R. Fitzgerald, Shelagh Wilson, Philip G. Szekeres, Derk J. Bergsma, Jane Miller, Gillian I. Rennie, Alison I. Muir, Lisa D. Spinage, Stephanie E. Guerrera, Jon K. Chambers, Lisa Vawter, Paul R. Murdock |
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| Rok vydání: | 2000 |
| Předmět: |
Agonist
medicine.medical_specialty medicine.drug_class Inositol Phosphates Adipose tissue Receptors Cell Surface Biology Transfection Biochemistry Cell Line Neuromedin U receptor GTP-Binding Proteins Internal medicine medicine Humans RNA Messenger Cloning Molecular Receptor Molecular Biology Reverse Transcriptase Polymerase Chain Reaction Neuropeptides Membrane Proteins Cell Biology Receptors Neurotransmitter Endocrinology Mechanism of action Gene Expression Regulation Calcium medicine.symptom Neuromedin S Neuromedin U Endogenous agonist |
| Zdroj: | The Journal of biological chemistry. 275(27) |
| ISSN: | 0021-9258 |
| Popis: | Neuromedins are a family of peptides best known for their contractile activity on smooth muscle preparations. The biological mechanism of action of neuromedin U remains unknown, despite the fact that the peptide was first isolated in 1985. Here we show that neuromedin U potently activates the orphan G protein-coupled receptor FM3, with subnanomolar potency, when FM3 is transiently expressed in human HEK-293 cells. Neuromedins B, C, K, and N are all inactive at this receptor. Quantitative reverse transcriptase-polymerase chain reaction analysis of neuromedin U expression in a range of human tissues showed that the peptide is highly expressed in the intestine, pituitary, and bone marrow, with lower levels of expression seen in stomach, adipose tissue, lymphocytes, spleen, and the cortex. Similar analysis of FM3 expression showed that the receptor is widely expressed in human tissue with highest levels seen in adipose tissue, intestine, spleen, and lymphocytes, suggesting that neuromedin U may have a wide range of presently undetermined physiological effects. The discovery that neuromedin U is an endogenous agonist for FM3 will significantly aid the study of the full physiological role of this peptide. |
| Databáze: | OpenAIRE |
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