Article
Creation and discovery of ligand-receptor pairs for transcriptional control with small molecules.
Proceedings of the National Academy of Sciences of the United States of America - 12 Oct 2004
Schwimmer Lauren J, Rohatgi Priyanka, Azizi Bahareh, Seley Katherine L, Doyle Donald F
Abstract excerpt
The nuclear receptor retinoid X receptor (RXR) is a ligand-activated transcription factor. To create receptors for a new ligand, a structure-based approach was used to generate a library of approximately 380,000 mutant RXR genes. To discover functional variants within the library, we used chemical complementation, a method of protein engineering that uses the power of genetic selection. Wild-type RXR has an EC50...
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