Receptor design principles

Receptor affinity chromatography, 3 847 Receptor blockers, 5 158 Receptor design, principles of, 76 769-775 Receptor purity, in microarray fabrication, 76 383... 

Experience across a wide variety of receptors with the screening of libraries designed in this way demonstrates that these design principles are effective and hits have been foimd for receptors which otherwise were considered to be difficult. Hits at a particular receptor are usually found in clusters giving an early indication of the SAR, and the same design considerations, used to produce the library, can be used in the lead optimization process. The extension of Thematic Analysis into Families B and C opens up the possibility of obtaining tractable leads in these areas as well. 

These basic design principles have been of value in the design and synthesis of varying P agonists with varying P receptor selectivities. 

Once administered, by whatever route, a drug must usually cross one or more membranes before the required biophase and target receptor are reached. Design principles can be applied to help access the biophase, and depend on knowledge of the mechanisms involved. 

Lanthanide ion lumophores have also been included in receptor,-spacer-receptor systems outside of the PET design principle. Nocera has targeted ionic or nonionic aromatic guests.187-189 The aromatic character of the guest is critical since receptor2 (as we as receptor,) is chosen to be optically transparent in this scheme. Since the guest serves to receive photonic excitation for subsequent EET to the lanthanide lumophore, the guest switches the luminescence on. ... 

Design Principles and Binding Motifs of Existing Receptors... 

Bioisosteres are defined as groups or molecules that have chemical and physical properties producing broadly similar biological properties. " Bioisosteres likely affect the same receptor site or pharmacological mechanism. This analog design principle was apphed to our DCK modification, and thio-DCK and DCK lactam derivatives were developed. 

Brown K T and Murakami M 1964 A new receptor potential of the monkey retina with no detectable latency Nature 201 626-8 Hong F T 1989 Relevance of light-induced charge displacements in molecular electronics design principles at the supramoleuclar level J. Mol. Electron. 5 163-85... 

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