Aqueous two-phase partition studies of glucocorticoid receptors exposed to limited trypsination. 1983

P A Andreasen

In a previous investigation the properties of glucocorticoid receptors exposed to partial proteolysis by chymotrypsin were studied by aqueous two-phase partitioning (Andreasen, P.A. and Gehring, U. (1981) Eur. J. Biochem. 120, 443-449). This paper describes studies of the properties of cytosolic glucocorticoid receptors submitted to limited trypsination, employing phase partitioning of rat thymocyte cytosol labelled with tritiated triamcinolone acetonide. Trypsin treatment of labelled cytosol at 0 degrees C does not result in any dissociation of steroid from the receptor. The partition properties of the trypsin-treated receptors exposed to receptor-activating conditions are indistinguishable from those of the activated native and chymotrypsin-treated receptors, although the trypsin-treated receptors have lost the affinity for DNA and dextran sulphate. Trypsin treatment of cytosol not exposed to receptor-activating conditions results in a rapid change in the receptor partition coefficients identical to that following chymotrypsin treatment. However, during incubations under conditions at which activation of native and chymotrypsin-treated receptors is very slow, the trypsin-treated receptor is converted to a form with partition properties indistinguishable from those of the activated receptors. During exposure of the cytosol to activating conditions, the time-course of the partition coefficient of the trypsin-treated receptors is only slightly different from that of the native and chymotrypsin-treated receptors, but the trypsin-treated receptors are far less susceptible to the activation inhibitors ATP, Li+ and MoO42-. We conclude that the proteolytic cleavages induced by trypsin in the non-activated receptor do not lead to any immediate changes in the charge and surface properties of the receptor different from those following chymotrypsin treatment, but that the trypsin-treated receptor is not able to maintain a non-activated state and a normal susceptibility to activation inhibitors.

UI MeSH Term Description Entries
D008094 Lithium An element in the alkali metals family. It has the atomic symbol Li, atomic number 3, and atomic weight [6.938; 6.997]. Salts of lithium are used in treating BIPOLAR DISORDER. Lithium-7,Lithium 7
D011189 Potassium Chloride A white crystal or crystalline powder used in BUFFERS; FERTILIZERS; and EXPLOSIVES. It can be used to replenish ELECTROLYTES and restore WATER-ELECTROLYTE BALANCE in treating HYPOKALEMIA. Slow-K,Chloride, Potassium
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
D011987 Receptors, Steroid Proteins found usually in the cytoplasm or nucleus that specifically bind steroid hormones and trigger changes influencing the behavior of cells. The steroid receptor-steroid hormone complex regulates the transcription of specific genes. Corticosteroid Receptors,Receptors, Corticosteroid,Steroid Receptors,Corticosteroid Receptor,Receptors, Steroids,Steroid Receptor,Receptor, Corticosteroid,Receptor, Steroid,Steroids Receptors
D006868 Hydrolysis The process of cleaving a chemical compound by the addition of a molecule of water.
D000255 Adenosine Triphosphate An adenine nucleotide containing three phosphate groups esterified to the sugar moiety. In addition to its crucial roles in metabolism adenosine triphosphate is a neurotransmitter. ATP,Adenosine Triphosphate, Calcium Salt,Adenosine Triphosphate, Chromium Salt,Adenosine Triphosphate, Magnesium Salt,Adenosine Triphosphate, Manganese Salt,Adenylpyrophosphate,CaATP,CrATP,Manganese Adenosine Triphosphate,MgATP,MnATP,ATP-MgCl2,Adenosine Triphosphate, Chromium Ammonium Salt,Adenosine Triphosphate, Magnesium Chloride,Atriphos,Chromium Adenosine Triphosphate,Cr(H2O)4 ATP,Magnesium Adenosine Triphosphate,Striadyne,ATP MgCl2
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013997 Time Factors Elements of limited time intervals, contributing to particular results or situations. Time Series,Factor, Time,Time Factor
D014222 Triamcinolone Acetonide An esterified form of TRIAMCINOLONE. It is an anti-inflammatory glucocorticoid used topically in the treatment of various skin disorders. Intralesional, intramuscular, and intra-articular injections are also administered under certain conditions. Azmacort,Cinonide,Kenacort A,Kenalog,Kenalog 40,Tricort-40,Acetonide, Triamcinolone,Tricort 40,Tricort40
D014357 Trypsin A serine endopeptidase that is formed from TRYPSINOGEN in the pancreas. It is converted into its active form by ENTEROPEPTIDASE in the small intestine. It catalyzes hydrolysis of the carboxyl group of either arginine or lysine. EC 3.4.21.4. Tripcellim,Trypure,beta-Trypsin,beta Trypsin

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