Protein Information

Name retinoid X receptor (protein family or complex)
Synonyms Retinoid X receptor; Retinoid X receptors; RXR; RXRs

Compound Information

Name methoprene
CAS

Reference List

PubMed Abstract RScore(About this table)
15180384 Schoff PK, Ankley GT: Effects of methoprene, its metabolites, and breakdown products on retinoid-activated pathways in transfected cell lines. Environ Toxicol Chem. 2004 May;23(5):1305-10.

Recent evidence suggests that a metabolite, methoprene acid, activates vertebrate retinoid X receptors (RXRs), and may interfere with retinoic acid-regulated developmental processes.
163(2,2,2,3) Details
7597096 Harmon MA, Boehm MF, Heyman RA, Mangelsdorf DJ: Activation of mammalian retinoid X receptors by the insect growth regulator methoprene. Proc Natl Acad Sci U S A. 1995 Jun 20;92(13):6157-60.

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).
112(1,2,2,2) Details
11349860 Peterson JK, Kashian DR, Dodson SI: Methoprene and 20-OH-ecdysone affect male production in Daphnia pulex. Environ Toxicol Chem. 2001 Mar;20(3):582-8.

Because methoprene has been found to bind to the mammalian retinoid X receptor, we also tested the effects of retinoic acid on Daphnia reproduction.
81(1,1,1,1) Details
19744992 Kushida A, Tamura H: Retinoic acids induce neurosteroid biosynthesis in human glial GI-1 Cells via the induction of steroidogenic genes. J Biochem. 2009 Dec;146(6):917-23. Epub 2009 Sep 10.

A retinoic acid receptor (RAR)-specific agonist, TTNPB, was unable to mimic this induction whereas a retinoid X receptor (RXR)-specific agonist, methoprene acid, in addition to 9-cis-RA, could do so.
81(1,1,1,1) Details
14754907 Abe A, Poucher HK, Hiraoka M, Shayman JA: Induction of lysosomal phospholipase A2 through the retinoid X receptor in THP-1 cells. J Lipid Res. 2004 Apr;45(4):667-73. Epub 2004 Feb 1.

The RXR agonist methoprene acid worked as well as all-trans-retinoic acid at increasing both mRNA and enzyme activity.
2(0,0,0,2) Details
16960373 Inoue Y, Kawahara H, Shirahata S, Sugimoto Y: Retinoic acid improves a hybridoma culture in a fructose-based medium by up-regulation of fructose incorporation via retinoid nuclear receptors. Biosci Biotechnol Biochem. 2006 Sep;70(9):2248-53. Epub 2006 Sep 7.


Selective activation of retinoid nuclear receptor by synthetic ligands showed that both retinoic acid receptors and retinoid X receptors might be related to the improvement of the fructose-based hybridoma culture.
1(0,0,0,1) Details
12970175 Svensson S, Ostberg T, Jacobsson M, Norstrom C, Stefansson K, Hallen D, Johansson IC, Zachrisson K, Ogg D, Jendeberg L: Crystal structure of the heterodimeric complex of LXRalpha and RXRbeta ligand-binding domains in a fully agonistic conformation. EMBO J. 2003 Sep 15;22(18):4625-33.

The nuclear receptor heterodimers of liver X receptor (LXR) and retinoid X receptor (RXR) are key transcriptional regulators of genes involved in lipid homeostasis and inflammation.
We report the crystal structure of the ligand-binding domains (LBDs) of LXRalpha and RXRbeta complexed to the synthetic LXR agonist T-0901317 and the RXR agonist methoprene acid (Protein Data Base entry 1UHL).
1(0,0,0,1) Details
17875330 Castro LF, Lima D, Machado A, Melo C, Hiromori Y, Nishikawa J, Nakanishi T, Reis-Henriques MA, Santos MM: Imposex induction is mediated through the Retinoid X Receptor signalling pathway in the neogastropod Nucella lapillus. Aquat Toxicol. 2007 Nov 15;85(1):57-66. Epub 2007 Aug 11.

Methoprene acid, a selective ligand for RXR, also induces imposex, albeit to a lower degree than that of the positive control.
1(0,0,0,1) Details
10600643 Alvarez R, Checa M, Brun S, Vinas O, Mampel T, Iglesias R, Giralt M, Villarroya F: Both retinoic-acid-receptor- and retinoid-X-receptor-dependent signalling pathways mediate the induction of the brown-adipose-tissue-uncoupling-protein-1 gene by retinoids. Biochem J. 2000 Jan 1;345 Pt 1:91-7.

Either RAR-specific inverted question markp-[(E)-2-(5,6,7,8,-tetrahydro-5,5,8, 8-tetramethyl-2-naphthalenyl)-1-propenyl] benzoic acid inverted question mark or RXR-specific [isopropyl-(E,E)-(R,S)-11-methoxy-3,7, 11-trimethyldodeca-2,4-dienoate, or methoprene] synthetic compounds increase the expression of UCP-1 mRNA and the activity of chloramphenicol acetyltransferase expression vectors driven by the ucp-1 promoter.
1(0,0,0,1) Details
9371088 Harmon MA, Scott TC, Li Y, Boehm MF, Phillips MA, Mangelsdorf DJ: Trypanosoma brucei: effects of methoprene and other isoprenoid compounds on procyclic and bloodstream forms in vitro and in mice. Exp Parasitol. 1997 Nov;87(3):229-36.

Of the other isoprenoids tested, juvenile hormone III and mammalian retinoid X receptor ligands were the most potent trypanocides.
1(0,0,0,1) Details
15583048 Brandebourg TD, Hu CY: Regulation of differentiating pig preadipocytes by retinoic acid. . J Anim Sci. 2005 Jan;83(1):98-107.

Glycerol-3-phoshphate dehydrogenase (GPDH) activity, a late marker of preadipocyte differentiation, was decreased (P < 0.01) by the addition of 0 to 10 microM of either ATRA, a nonspecific agonist for both the retinoic acid receptor (RAR) and the retinoid X receptor (RXR) or the selective RAR agonist, 4-(E-2-[5,6,7,8-tet-rahydro-5,5,8,8-tetramethyl-2-naphthalenyl]-1-propenyl ) benzoic acid (TTNPB).
Addition of methoprene acid, an RXR-specific agonist, increased (P < 0.01) GPDH activity.
1(0,0,0,1) Details
16302920 Shibuya N, Nemoto E, Kanaya S, Kunii R, Shimauchi H: Retinoic acid is a potential negative regulator for differentiation of human periodontal ligament cells. J Periodontal Res. 2005 Dec;40(6):432-40.


RA receptor (RAR)-alpha agonist (AM-580), but not retinoid X receptor agonist (methoprene acid), inhibited the mineralization, and reverse transcription-polymerase chain reaction analysis revealed that RAR-alpha was expressed on the cells, suggesting that RAR-alpha was involved in the inhibitory mechanism.
0(0,0,0,0) Details