Biomaterial Database

Glucocorticoid receptors in human synovial tissue and relative receptor affinities of glucocorticoid-21-esters. 1988

M Pörtner, and H Möllmann, and P Rohdewald

Institut für Pharmazeutische Chemie, Westfälische Wilhelms-Universität Münster, West Germany.

A dexamethasone binding protein was detected in cytosol of 11 human synovial tissues from patients with chronic polyarthritis. The apparent dissociation constant (KD) ranged from 3.3 to 17.1 (mean, 7.0 +/- 4.3) nmol/liter, and the receptor concentration (Ro) from 17 to 65 (mean, 42 + 15) fmol/mg protein. Results of competition assays with an excess of unlabeled aldosterone, estradiol, pregnenolone, and testosterone confirmed that the binding protein had characteristics of a glucocorticoid receptor. With the use of diisopropylfluorophosphate (DFP) for esterase inhibition, and considering the purity of the starting material and the hydrolysis products, we could determine the relative receptor affinities of glucocorticoid-21-esters. In contrast to the high affinity of the glucocorticoid-17-ester examined, esterification in position 21 abolishes binding affinities. Glucocorticoid-21-esters are true prodrugs for which the glucocorticoid action is caused only by the corresponding glucocorticoid alcohol.

UI	MeSH Term	Description	Entries
D008168	Lung	Either of the pair of organs occupying the cavity of the thorax that effect the aeration of the blood.	Lungs
D011965	Receptors, Glucocorticoid	Cytoplasmic proteins that specifically bind glucocorticoids and mediate their cellular effects. The glucocorticoid receptor-glucocorticoid complex acts in the nucleus to induce transcription of DNA. Glucocorticoids were named for their actions on blood glucose concentration, but they have equally important effects on protein and fat metabolism. Cortisol is the most important example.	Corticoid Type II Receptor,Glucocorticoid Receptors,Glucocorticoids Receptor,Corticoid II Receptor,Corticoid Type II Receptors,Glucocorticoid Receptor,Receptors, Corticoid II,Receptors, Corticoid Type II,Receptors, Glucocorticoids,Corticoid II Receptors,Glucocorticoids Receptors,Receptor, Corticoid II,Receptor, Glucocorticoid,Receptor, Glucocorticoids
D002851	Chromatography, High Pressure Liquid	Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.	Chromatography, High Performance Liquid,Chromatography, High Speed Liquid,Chromatography, Liquid, High Pressure,HPLC,High Performance Liquid Chromatography,High-Performance Liquid Chromatography,UPLC,Ultra Performance Liquid Chromatography,Chromatography, High-Performance Liquid,High-Performance Liquid Chromatographies,Liquid Chromatography, High-Performance
D005938	Glucocorticoids	A group of CORTICOSTEROIDS that affect carbohydrate metabolism (GLUCONEOGENESIS, liver glycogen deposition, elevation of BLOOD SUGAR), inhibit ADRENOCORTICOTROPIC HORMONE secretion, and possess pronounced anti-inflammatory activity. They also play a role in fat and protein metabolism, maintenance of arterial blood pressure, alteration of the connective tissue response to injury, reduction in the number of circulating lymphocytes, and functioning of the central nervous system.	Glucocorticoid,Glucocorticoid Effect,Glucorticoid Effects,Effect, Glucocorticoid,Effects, Glucorticoid
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D006868	Hydrolysis	The process of cleaving a chemical compound by the addition of a molecule of water.
D013583	Synovial Membrane	The inner membrane of a joint capsule surrounding a freely movable joint. It is loosely attached to the external fibrous capsule and secretes SYNOVIAL FLUID.	Synovium,Membrana Synovialis Capsulae Articularis,Membrane, Synovial,Membranes, Synovial,Synovial Membranes
D066298	In Vitro Techniques	Methods to study reactions or processes taking place in an artificial environment outside the living organism.	In Vitro Test,In Vitro Testing,In Vitro Tests,In Vitro as Topic,In Vitro,In Vitro Technique,In Vitro Testings,Technique, In Vitro,Techniques, In Vitro,Test, In Vitro,Testing, In Vitro,Testings, In Vitro,Tests, In Vitro,Vitro Testing, In