Affinity labeling of receptors

Katzenellenbogen JA, Katzenellenbogen BS (1984) Affinity labeling of receptors for steroid and thyroid hormones. Academic Press, New York... 

Receptors and Transport Systems Affinity labeling of receptors, 46, 572 nicotinic acetylcholine receptors, 46, 582 )8-adrenergic receptors, 46, 591 opiate receptors, 46, 601 amino acid transport proteins, 46, 607 the biotin transport system, 46, 613. 

Conclusions. These three examples indicate that 3 - and 5 -FSBA may be useful in the affinity labeling of receptor proteins as well as of the regulatory and active sites of enzymes. Within the constraints imposed by the limitations of solubility and stability of these compounds, the fluorosulfonylbenzoyladenosines thus may have broad applicability in the labeling of adenine nucleotide sites in proteins. 

Damle, V.N. and Karlin, A., Affinity labeling of one of two a-neurotoxin binding sites in acetylcholine receptor from Torpedo californica, Biochemistry, 17, 2039, 1978. 

Bowen, W.K., Hellewell, S B., Keleman, M., Huey, R., Stewart, D. Affinity labelling of 6-opiate receptors using [D-Ala2, Leu5, Cys6]enkephalin covalent attachment via thiol-disulfide exchange, J. Biol. Chem. 1987, 262, 13434-13439. 

Perret, P., Laube, B., Schemm, R., Betz, H., Goeldner, M. and Foucaud, B. (2002). Affinity labeling of cysteine-mutants evidences contact residues in modeled receptor binding sites. J. 

Affinity labelling of thyroid hormones to nuclear receptors indicated the presence of an abundant 47000 Da component and a less abundant 57000 Da species [40], Micrococcal nuclease also excises the two receptor forms. It is yet not clear whether these two forms are products of different genes or if the 57 000 Da form is converted or processed to the 47 000 Da species. 

Bidlack JM, Frey DK, Kaplan RA, Seyed-Mozaffari A, Archer S (1989) Affinity labelling of mu opioid receptors by sulhydryl alkylating derivatives of morphine and morphinone. Mol Pharmacol 37 50-59... 

Mukherjee, A., Kirkovsky, L.I., Kimura, Y., Marvel, M.M., Miller, D.D. and Dalton, J.T. (1999) Affinity labeling of the androgen receptor with nonsteroidal chemoaffinity ligands. Biochemical Pharmacology, 58, 1259-1267. 

Pearson, R., and Miller, L. (1987). Affinity Labeling of a Novel Cholecystekinin-binding Protein in Rat Pancreatic Plasma Lemma Using New Short Probes for the Receptor, J. Biol. Chem. 262 869-876. 

This small country occupies a leading position in the world of peptides. As early as 1949, publications on activation of N-blocked amino acids in the form of their reactive esters appeared from the laboratory of Robert Schwyzer (Plate 39) at CIBA in Basel. After his appointment to professor at the Eidgenossische Technische Hochschule (ETH) in Zurich, he established there, at the Institute of Molecular Biology and Biophysics, a distinguished school of peptide research. One of his students, P.W. Schiller, is professor at the University of Montreal. Another outstanding former student of Schwyzer, Alex Eberle, is a lecturer in Zurich, yet active in Basel, where he is engaged in affinity-labelling of hormone receptors. 

Nikodem, V. M., Cheng, S.-Y., and Rail, J. E. (1980). Affinity labeling of rat liver thyroid hormone nuclear receptor. Proc. Natl. Acad. Sci. USA 77 7064-7068. 

Simons SS Jr, Thompson EB (1981) Dexamethasone 21-methylate an affinity label of glucocorticoid receptors from rat hepatoma tissue culture cells. Proc Natl Acad Sci USA 78 3541-3545... 

Positive identification of receptors in preparations of subcellular fractions is feasible only on conditions that the receptor protein has been labeled before the disruption of the membrane. The labeling techniques commonly employed for the identification of receptor proteins are inadequate, however, since the latter constitute only a minor component of the total cell proteins. In principle, affinity labeling provides the high specificity needed for this purpose. By this method, the reagent interacts reversibly and specifically with the active site of the receptor and then forms a stable covalent bond with amino acid residues located at or near the active site. The attached moiety can be detected by virtue of a tailored chromophore that is radioactive, fluorescent, or spin label. In this connection it is of interest that affinity labeling of the norepinephrine a-receptor was reported as early as 1945. ... 

The application of affinity labeling to receptor sites may have one of several objectives. 

It has been claimed that affinity-labelling of acetylcholine receptors can be accomplished with p-ftrlmethylammonlum)benzene-dlazonium fluoborate (Tdf)75, 76 Phosphorylation of the... 

---