[Structure and activity of insulin. 8. Exchange of histidine for alanine in synthetic B-chains].
Explore the source record for details and available documents.
Biomedical subjects
Publications and source records attributed to K Eisele.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Inhibition of 3':5'-cyclic-AMP-5'-nucleotidohydrolase (EC 3.1.4.17) type II (cAMP-phosphodiesterase) by sodium molybdate was studied: While determination of inorganic phosphate and 5'-ribonucleotide phosphohydrolase (5'-nucleotidase) (EC 3.1.3.5) activity was not disturbed by sodium molybdate in concentrations up to 10 mM, cAMP-phosphodiesterase was inhibited by millimolar concentrations of molybdate. The half maximal effect was observed at about 2 mM sodium molybdate (0.75 mM cAMP in the assay).
The androgen receptor of murine preputial gland showed in binding experiments a biphasic saturation curve and a biphasic Scatchard plot. The receptor converted from an 8.5-9 S form to a 4.5-5 S form in high ionic strength buffer. The apparent dissociation constant was KD 0.5 +/- 0.2 nM for the 8.5-9 S receptor form. A 6.5-7 S receptor form could be detected in some experiments. The ligand specificity was evaluated by competition experiments: testosterone greater than androstenedione greater than dihydrotestosterone greater than androstanediol greater than estradiol greater than progesterone greater than dexamethasone. The receptor of murine preputial gland was less stable than the androgen receptor of skeletal muscle of the same mice.
With the nuclear exchange assay and the nuclear retention assay it is shown that the androgen insensitivity of Tfm mice is probably due to a defect of the nuclear acceptor sites for the testosterone receptor complex. Further on the results obtained point strongly to the possibility that hormone free androgen receptor is localized in the nuclei and in the cytoplasma according to the "equilibrium model". A practicable method for separation of unbound steroids from nuclei is described.
Seven tripeptides with the sequence L-Arg-D,L-X-L-Phe were synthesised. Three of these peptides showed antibiotical activity on fungi. The amino- and the carboxylic terminus of the peptide L-Arg-D,L-Phe-L-Phe, which showed antibiotical activity, were changed to give the sequences L-X-D,L-Phe-L-Phe or L-Arg-D,L-Phe-L-X respectively. The resulting tripeptides showed no antibiotical activity.