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An inverse relationship between receptor internalization and the fraction of laterally mobile receptors for the vasopressin renal‐type V 2 ‐receptor
Author(s) -
David A. Jans,
Reiner Peters,
Falk Fahrenholz
Publication year - 1990
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(90)81368-x
Subject(s) - internalization , vasopressin receptor , receptor , vasopressin , endocrinology , medicine , chemistry , microbiology and biotechnology , biology , antagonist
Lateral mobility of the vasopressin renal‐type V 2 ‐receptor was investigated in LLC‐PK 1 , porcine epithelial cells using the technique of fluorescence microphotolysis (photobleaching) and a rhodamine‐labelled vasopressin analogue. At various times after ligand addition, cells were analyzed for both receptor lateral mobility and ligand internalization. The V 2 ‐receptor mobile fraction diminished from 0.9 to 0.43 over 60 min at 37°C. whereas the apparent lateral diffusion coefficient remained essentially unchanged (2–3 × 10 −10 cm 2 s). Interestingly, the fraction of immobile V 2 ‐receptors corresponded exactly with the fraction of internalized receptors, implying a functional relationship. These observations together with comparable results reported for other polypeptide hormone receptors indicate a possible machanistic role for receptor immobilization in the desensitization of hormonal response.