Transcriptional activation of the Drosophila ecdysone receptor by insect and plant ecdysteroids.
A number of insect ecdysteroids, plant ecdysteroids and juvenoids were assayed for their ability to activate Drosophila nuclear receptors in transfected tissue culture cells. Discrete modifications to 20-hydroxyecdysone, the apparent natural ligand for the ecdysone receptor (EcR), conferred dramatic changes on the transcriptional activity of this receptor, suggesting that other biologically relevant EcR ligands may exist. Conversely, none of the compounds tested had a significant effect on the activity of three Drosophila orphan nuclear receptors: DHR38, DHR78 or DHR96. Taken together, these results demonstrate the selectivity of EcR for a series of natural and synthetic ecdysone agonists and suggest that as yet untested compounds may be responsible for activating DHR38, DHR78 and DHR96.
Baker
K D
KD
Howard Hughes Medical Institute, Department of Pharmacology, University of Texas Southwestern Medical Center at Dallas, 75390-9050, Dallas, TX, USA.
Warren
J T
JT
Thummel
C S
CS
Gilbert
L I
LI
Mangelsdorf
D J
DJ
D000818:Animals; D046508:Culture Techniques; D004330:Drosophila / Q000235:genetics / Q000502:physiology*; D004441:Ecdysterone / Q000494:pharmacology*; D007605:Juvenile Hormones / Q000494:pharmacology*; D008024:Ligands; D010937:Plant Growth Regulators / Q000494:pharmacology*; D011987:Receptors, Steroid / Q000096:biosynthesis / Q000235:genetics*; D014158:Transcription, Genetic
D007605:Juvenile Hormones; D008024:Ligands; D010937:Plant Growth Regulators; D011987:Receptors, Steroid; C055469:ecdysone receptor; D004441:Ecdysterone