PMID- 7597096
OWN - NLM
STAT- MEDLINE
DCOM- 19950803
LR  - 20191210
IS  - 0027-8424 (Print)
IS  - 1091-6490 (Electronic)
IS  - 0027-8424 (Linking)
VI  - 92
IP  - 13
DP  - 1995 Jun 20
TI  - Activation of mammalian retinoid X receptors by the insect growth regulator 
      methoprene.
PG  - 6157-60
AB  - We report that methoprene and its derivatives can stimulate gene transcription in 
      vertebrates by acting through the retinoic acid-responsive transcription factors, 
      the retinoid X receptors (RXRs). Methoprene is an insect growth regulator in 
      domestic and agricultural use as a pesticide. At least one metabolite of 
      methoprene, methoprene acid, directly binds to RXR and is a transcriptional 
      activator in both insect and mammalian cells. Unlike the endogenous RXR ligand, 
      9-cis-retinoic acid, this activity is RXR-specific; the methoprene derivatives do 
      not activate the retinoic acid receptor pathway. Methoprene is a juvenile hormone 
      analog that acts to retain juvenile characteristics during insect growth, 
      preventing metamorphosis into an adult, and it has been shown to have ovicidal 
      properties in some insects. Thus, a pesticide that mimics the action of juvenile 
      hormone in insects can also activate a mammalian retinoid-responsive pathway. 
      This finding provides a basis through which the potential bioactivity of 
      substances exposed to the environment may be reexamined and points the way for 
      discovery of new receptor ligands in both insects and vertebrates.
FAU - Harmon, M A
AU  - Harmon MA
AD  - Howard Hughes Medical Institute, University of Texas Southwestern Medical Center, 
      Dallas 75235-9050, USA.
FAU - Boehm, M F
AU  - Boehm MF
FAU - Heyman, R A
AU  - Heyman RA
FAU - Mangelsdorf, D J
AU  - Mangelsdorf DJ
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - United States
TA  - Proc Natl Acad Sci U S A
JT  - Proceedings of the National Academy of Sciences of the United States of America
JID - 7505876
RN  - 0 (DNA-Binding Proteins)
RN  - 0 (Fungal Proteins)
RN  - 0 (GAL4 protein, S cerevisiae)
RN  - 0 (Receptors, Retinoic Acid)
RN  - 0 (Recombinant Proteins)
RN  - 0 (Retinoid X Receptors)
RN  - 0 (Retinoids)
RN  - 0 (Saccharomyces cerevisiae Proteins)
RN  - 0 (Transcription Factors)
RN  - 8B830OJ2UX (Methoprene)
RN  - EC 1.13.12.- (Luciferases)
RN  - EC 3.2.1.23 (beta-Galactosidase)
SB  - IM
MH  - Animals
MH  - Binding, Competitive
MH  - Cell Line
MH  - Chlorocebus aethiops
MH  - DNA-Binding Proteins
MH  - Drosophila melanogaster
MH  - Fungal Proteins/biosynthesis/metabolism
MH  - Gene Expression/*drug effects
MH  - Kidney
MH  - Kinetics
MH  - Luciferases/biosynthesis/metabolism
MH  - Methoprene/*pharmacology
MH  - Receptors, Retinoic Acid/biosynthesis/*drug effects/metabolism
MH  - Recombinant Proteins/biosynthesis/drug effects/metabolism
MH  - Retinoid X Receptors
MH  - Retinoids/metabolism
MH  - *Saccharomyces cerevisiae Proteins
MH  - Transcription Factors/biosynthesis/*drug effects/metabolism
MH  - Transcription, Genetic/drug effects
MH  - Transfection
MH  - beta-Galactosidase/biosynthesis
PMC - PMC41661
EDAT- 1995/06/20 00:00
MHDA- 1995/06/20 00:01
PMCR- 1995/12/20
CRDT- 1995/06/20 00:00
PHST- 1995/06/20 00:00 [pubmed]
PHST- 1995/06/20 00:01 [medline]
PHST- 1995/06/20 00:00 [entrez]
PHST- 1995/12/20 00:00 [pmc-release]
AID - 10.1073/pnas.92.13.6157 [doi]
PST - ppublish
SO  - Proc Natl Acad Sci U S A. 1995 Jun 20;92(13):6157-60. doi: 
      10.1073/pnas.92.13.6157.