Book Chapter

Structure and Function of Ecdysone Receptors-Interactions with Ecdysteroids and Synthetic Agonists

Ronald J Hill, Lloyd D Graham, Kathleen A Turner, Linda Howell, Donya Tohidi-Esfahani, Ross Fernley, Julian Grusovin, Bin Ren, Patricia Pilling, Louis Lu, Phan Tram, George O Lovrecz, Matthew Pollard, Anna Pawlak-Skrzecz, Victor A Streltsov, Thomas S Peat, David A Winkler, Michael C Lawrence

ADVANCES IN INSECT PHYSIOLOGY, VOL 43: INSECT GROWTH DISRUPTORS | Advances in Insect Physiology | ACADEMIC PRESS LTD-ELSEVIER SCIENCE LTD | Published : 2012

Abstract

The binding of ecdysteroids and the bisacylhydrazine insecticide, tebufenozide, to recombinant ecdysone receptor ligand-binding domains from pest insects points to conserved and variable features of the receptor's ligand-binding pocket. Fluorophores conjugated to the terminus of the ecdysteroid alkyl chain have surprisingly little effect on receptor binding, permitting the development of a fluorescence polarization chemical library screen that has led to the discovery of a new class of ecdysone receptor ligands, the methylene lactams. X-ray structures of ecdysone receptor ligand-binding domains have allowed identification of the conserved and variable features within the binding pocket. The ..

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University of Melbourne Researchers