Ligand interaction with target

Grunbeck, A., Sakmar, T. P. (2013). Probing G protein-coupled receptor—Ligand interactions with targeted photoactivatable cross-hnkers. Biochemistry, 52(48), 8625—8632. http //dx.doi.Org/10.1021/bi401300y. 

Affinity capillary electrophoresis- MS In electrophoretic buffer In running buffer for CE Bound ligands measured by mobility change of ligand upon interaction with target in electrophoretic buffer and identified by MS (Chu et al., 1996)... 

Beau has applied the DCC concept to a number of carbohydrate systems [13-16]. Carbohydrate-binding proteins often exhibit weak ligand interactions with millimolar dissociation constants, a quite different scenario to the enzyme-small molecule DCLs discussed thus far. The protein target initially chosen for study was hen egg-white lysozyme (HEWL), a glycosidase known to bind A-acetyl-o-glucosamine (d-G1cNAc) with... 

Thanks mainly to the efforts of the Strasbourg group of D. Moras and Pierre Chambon, and Paul Sigler s laboratory at Yale University, three-dimensional structural information is now available in the case of heterodimeric RXR/TR and RXR/RAR DBDs bound to direct DNA repeats (DR4 and DR5), respectively (Plate 24 and Fig. 11.11). This is one of the still rather rare cases where one can profitably explain, on a molecular basis, the interactions of a receptor with the ligand and with target genes. 

With the characterization of the SAR and the documentation of the effects of different pharmacophores and various substituents on biological activity, it is possible to theoretically model the way in which the ligand interacts with its target and thus derive a two- or... 

The classical sex hormone receptors such as ER, PR, and AR form homodimers upon ligand binding and then interact with target DNA via HREs to control target gene expression (Figure 2.1fi). In contrast, the orphan receptors or adopted orphan receptors form heterodimers with retinoid X receptors (RXRs) on direct repeat... 

Figure 21.3 Potential targeting of receptors and signaling pathways. This schematic illustrates potential sites of intervention of drug in a cell. In pathway A, the drug blocks the ligand interaction with the receptor. In pathways B-D, different sites in the bifurcating signal transduction pathway are inhibited.

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