Transcriptional activation of the Drosophila ecdysone receptor by insect and plant ecdysteroids

Keith D. Baker; James T. Warren; Carl S. Thummel; Lawrence I. Gilbert; David J. Mangelsdorf

doi:10.1016/S0965-1748(00)00075-8

Transcriptional activation of the Drosophila ecdysone receptor by insect and plant ecdysteroids

Keith D. Baker, James T. Warren, Carl S. Thummel, Lawrence I. Gilbert, David J. Mangelsdorf

Research output: Contribution to journal › Article › peer-review

55 Scopus citations

Abstract

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. (C) 2000 Elsevier Science Ltd.

Original language	English (US)
Pages (from-to)	1037-1043
Number of pages	7
Journal	Insect Biochemistry and Molecular Biology
Volume	30
Issue number	11
DOIs	https://doi.org/10.1016/S0965-1748(00)00075-8
State	Published - 2000

Keywords

Drosophila
Ecdysone receptor
Ecdysteroids
Orphan nuclear receptor
Ultraspiracle

ASJC Scopus subject areas

Biochemistry
Molecular Biology
Insect Science

Access to Document

10.1016/S0965-1748(00)00075-8

Cite this

@article{62f029fb6d734fb4af2d0d2180ecb247,

title = "Transcriptional activation of the Drosophila ecdysone receptor by insect and plant ecdysteroids",

abstract = "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. (C) 2000 Elsevier Science Ltd.",

keywords = "Drosophila, Ecdysone receptor, Ecdysteroids, Orphan nuclear receptor, Ultraspiracle",

author = "Baker, {Keith D.} and Warren, {James T.} and Thummel, {Carl S.} and Gilbert, {Lawrence I.} and Mangelsdorf, {David J.}",

note = "Funding Information: We thank Drs K. Nakanishi, R. Lafont, and Rohm and Haas for some of the hormones used in this study and W.A. Segraves for the pA5C–EcR expression construct. D.J.M. and C.S.T. are investigators of the Howard Hughes Medical Institute (HHMI). This work was funded by HHMI (D.J.M. and C.S.T.), by grants from the Robert A. Welch Foundation and Human Frontier Science Program (D.J.M.), and grants from NIH (DK30118) and NSF (IBN 9603710) (L.I.G.).",

year = "2000",

doi = "10.1016/S0965-1748(00)00075-8",

language = "English (US)",

volume = "30",

pages = "1037--1043",

journal = "Insect Biochemistry and Molecular Biology",

issn = "0965-1748",

publisher = "Elsevier Limited",

number = "11",

}

TY - JOUR

T1 - Transcriptional activation of the Drosophila ecdysone receptor by insect and plant ecdysteroids

AU - Baker, Keith D.

AU - Warren, James T.

AU - Thummel, Carl S.

AU - Gilbert, Lawrence I.

AU - Mangelsdorf, David J.

N1 - Funding Information: We thank Drs K. Nakanishi, R. Lafont, and Rohm and Haas for some of the hormones used in this study and W.A. Segraves for the pA5C–EcR expression construct. D.J.M. and C.S.T. are investigators of the Howard Hughes Medical Institute (HHMI). This work was funded by HHMI (D.J.M. and C.S.T.), by grants from the Robert A. Welch Foundation and Human Frontier Science Program (D.J.M.), and grants from NIH (DK30118) and NSF (IBN 9603710) (L.I.G.).

PY - 2000

Y1 - 2000

N2 - 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. (C) 2000 Elsevier Science Ltd.

AB - 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. (C) 2000 Elsevier Science Ltd.

KW - Drosophila

KW - Ecdysone receptor

KW - Ecdysteroids

KW - Orphan nuclear receptor

KW - Ultraspiracle

UR - http://www.scopus.com/inward/record.url?scp=0033808829&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0033808829&partnerID=8YFLogxK

U2 - 10.1016/S0965-1748(00)00075-8

DO - 10.1016/S0965-1748(00)00075-8

M3 - Article

C2 - 10989290

AN - SCOPUS:0033808829

SN - 0965-1748

VL - 30

SP - 1037

EP - 1043

JO - Insect Biochemistry and Molecular Biology

JF - Insect Biochemistry and Molecular Biology

IS - 11

ER -

Transcriptional activation of the Drosophila ecdysone receptor by insect and plant ecdysteroids

Abstract

Keywords

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this