Hormone binding sites

Galardy, R.E., Craig, L.C., Jamieson, J.D., and Printz, M.P. (1974) Photoaffinity labeling of peptide hormone binding sites./. Biol. Chem. 249, 3510-3518. 

Wedekind, F., Baer-Pontzen, K., Bala-Mohan, S., Choli, D., Zahn, H., and Brandenburg, D. (1989) Hormone binding site of the insulin receptor Analysis using photoaffinity-mediated avidin complexing. Biol. Chem. Hoppe-Seyler 370, 251-258. 

Several criteria determine whether a steroid-hormone-binding site is a putative receptor. First, the steroid-hormone-binding site must be present in hormone-responsive tissues or brain regions, and absent from nonresponsive ones. Second, it should bind steroids that are either active agonists or effective antagonists of the hormone effect, and should not bind steroids that are inactive in either sense. 

Our present information about the hormone binding domain, although still limited, comes from a combination of biochemical and genetic studies. The amino acid which reacts with the chemical affinity label dexamethasone 21-mesylate has now been identified as cysteine in position 656 of the rat glucocorticoid receptor [109]. This cysteine is therefore located within or very close to the hormone binding site. It corresponds to cysteine 644 of the mouse receptor (Fig. 2). 

Harvey S, Hayer S (1993) Parathyroid hormone binding sites in the brain. Peptides 14 1187-1191 Hata AN, Zent R, Breyer MD, Breyer RM (2003) Expression and molecular pharmacology of the mouse CRTH2 receptor. J Pharmacol Exp Ther 306 463-470 Haulica I, Neamtu C, Stratone A, Petrescu G, Branisteanu D, Rosea V, Slatineanu S (1986) Evidence for the involvement of cerebral renin-angiotensin system (RAS) in stress analgesia. Pain 27 237-245... 

Holtje, H.-D., Dali, N. A Molecular Modeling Study on the Hormone Binding Site of the Estrogen Receptor, Phar-mazie 1993, 48, 243-246. 

Grace CR, Perrin MFI, DiGmccio MR, Miller CL, Rivier JE, Vale WW, Rick R. NMR stmctnre and peptide hormone binding site... 

Cetirizine is the primary acid metabolite of hydroxyzine, resulting from complete oxidation of the primary alcohol moiety. This compound is zwittcrionic and relatively polar and thus does not penetrate the BBB readily. Before its introduction in the United States, ectiri/ine was one of the most widely prescribed H antihistamines in Europe. It is highly selective in its interaction with various hormonal binding sites and highly potent ( terfenadinc) as well. " - "... 

Rigorous evaluation of free thyroid hormone methods is required before new assays are placed into clinical service. Performance data on analytical accuracy should be obtained not only on serum from patients with thyroid dysfunction but also in serum from patients with binding protein abnor-mahties. Effects of drugs that compete for hormone binding sites on serum proteins should also be evaluated. Moreover, adequate assessment requires an examination of the effects of progressive sample dilution. In theory, the free concentration of T4 and T3 should not decrease with dilution until about 20% of the bound ligand is dissociated. In the case of... 

Affinity Labeling of Hormone Binding Sites John A. Katzenellenbogen 9, 222 ... 

C.R. Grace, M.H. Perrin, M.R. DiGruccio, C.L. Miller, J.E. Rivier, W.W. Vale, R. Riek, NMR structure and peptide hormone binding site of the first extracellular domain of a type B1 G protein-coupled receptor,... 

F. 7.10. P2 Adrenergic receptor. The receptor has seven a-hehx domains that span the membrane and is therefore a member of the heptaheli-cal class of receptors. A. The transmembrane domains are drawn in an extended form. B. The seven transmembrane helices (shown as tubes) form a cylindrical structure. Loops connecting helices form the hormone binding site on the external side of the plasma membrane, and a binding site for a G-protein is on the intracellular side. The protein also contains oligosaccharide chains, pahnityl groups, and phosphorylation sites (shown in blue see Chapter 6). 

Hdltje, H.-D. and Dali, N. (1993) A molecular modelling study on the hormone binding site of the estrogen receptor. Die Pharmazie 48 243-249. 

The most useful technique would be affinity chromatography. Covalently attach the purified hormone to sepharose or some other form of an insoluble bead (see problem 4), and use the hormone-bead complex to fill a column. Homogenize liver cells, and add the homogenate to the column. Receptors should stick on the column because their hormone-binding sites are complementary in shape to the covalently bound hormone. You could elute the receptors from the column as hormone-receptor complexes by adding free hormone to compete with the hormone that is bound to the column. 

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