The dissociation of testosterone- and 5 alpha-dihydrotestosterone-receptor complexes formed within cultured human genital skin fibroblasts. 1983

M Kaufman, and L Pinsky

We have studied the rate and character with which testosterone (T) and 5 alpha-dihydrotestosterone (DHT) dissociate from the androgen receptor both within intact cultured genital skin fibroblasts of a subject with 5 alpha-reductase deficiency and after the androgen-receptor complexes have been extracted from the cells. Within the cells, the kinetics of the dissociative process for each hormone was first-order, but T dissociated four times faster than DHT. An Arrhenius plot of the variation of the dissociation rate constants with temperature for T was linear and yielded an activation energy of 28 kcal/mol. This value is identical with the one previously determined for activated DHT-receptor complexes. T-receptor complexes extracted from the cells dissociated with complex kinetics: at 37 degrees C the rate constants of the "fast" and "slow" components were 40 and 14 X 10(-3) min-1, respectively. In contrast, DHT-receptor complexes extracted from the cells dissociated with first-order kinetics and at a rate identical to that observed within cells, except after exposure to pyridoxal 5'-phosphate (5 mM) or concentration by Amicon (B-15) filtration, when their dissociation kinetics became complex. We interpret these data to mean that, within the cells, both T- and DHT-receptor complexes exist predominantly in the activated state whereas, when extracted from the cells, DHT-receptor complexes remain activated, unless perturbed, while T-receptor complexes become unstable spontaneously, probably by reverting to a preactivated state.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008297 Male Males
D010413 Penis The external reproductive organ of males. It is composed of a mass of erectile tissue enclosed in three cylindrical fibrous compartments. Two of the three compartments, the corpus cavernosa, are placed side-by-side along the upper part of the organ. The third compartment below, the corpus spongiosum, houses the urethra. Glans Penis,Penis, Glans
D011732 Pyridoxal Phosphate This is the active form of VITAMIN B 6 serving as a coenzyme for synthesis of amino acids, neurotransmitters (serotonin, norepinephrine), sphingolipids, aminolevulinic acid. During transamination of amino acids, pyridoxal phosphate is transiently converted into pyridoxamine phosphate (PYRIDOXAMINE). Pyridoxal 5-Phosphate,Pyridoxal-P,Phosphate, Pyridoxal,Pyridoxal 5 Phosphate,Pyridoxal P
D011944 Receptors, Androgen Proteins, generally found in the CYTOPLASM, that specifically bind ANDROGENS and mediate their cellular actions. The complex of the androgen and receptor migrates to the CELL NUCLEUS where it induces transcription of specific segments of DNA. Androgen Receptors,5 alpha-Dihydrotestosterone Receptor,Androgen Receptor,Dihydrotestosterone Receptors,Receptor, Testosterone,Receptors, Androgens,Receptors, Dihydrotestosterone,Receptors, Stanolone,Stanolone Receptor,Testosterone Receptor,5 alpha Dihydrotestosterone Receptor,Androgens Receptors,Receptor, 5 alpha-Dihydrotestosterone,Receptor, Androgen,Receptor, Stanolone,Stanolone Receptors,alpha-Dihydrotestosterone Receptor, 5
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
D002478 Cells, Cultured Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others. Cultured Cells,Cell, Cultured,Cultured Cell
D005260 Female Females
D005347 Fibroblasts Connective tissue cells which secrete an extracellular matrix rich in collagen and other macromolecules. Fibroblast
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man

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