Bradykinin receptors undergo ligand-induced desensitization
| Autor: | Ruth A. Roberts, W. J. Gullick |
|---|---|
| Rok vydání: | 1990 |
| Předmět: |
Chemistry
Receptors Bradykinin medicine.medical_treatment Cell Membrane Cell Bradykinin Biochemistry Rats Receptors Neurotransmitter Cell membrane Kinetics chemistry.chemical_compound medicine.anatomical_structure medicine Biophysics Animals Neurotransmitter metabolism Binding site Bradykinin receptor Receptor Cells Cultured Desensitization (medicine) |
| Zdroj: | Biochemistry. 29:1975-1979 |
| ISSN: | 1520-4995 0006-2960 |
| DOI: | 10.1021/bi00460a002 |
| Popis: | Bradykinin binds to specific cell surface receptors on Rat13 fibroblasts with a high affinity (2.1 nM). Prolonged exposure of cells to the ligand causes a concentration-dependent decline in surface levels of the 2.1 nM receptor from 40,000 receptors per cell to undetectable levels with a t1/2 of approximately 2 h. The decline occurs in parallel with the appearance of an equal number of lower affinity binding sites (40 nM), suggesting that ligand exposure causes desensitization by an alteration in receptor affinity. The affinity change is characterized by a faster rate of ligand dissociation while the rate of association remains unaltered. The observed desensitization is dependent on the presence of active cellular metabolism since (i) it does not occur in whole cells maintained at 4 degrees C and (ii) membranes prepared from Rat13 cells retain their high-affinity sites at 37 degrees C despite extensive ligand exposure. |
| Databáze: | OpenAIRE |
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