The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
Activation of mammalian retinoid X receptors by the insect growth regulator methoprene.
Open accessAbstract
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.
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Cites
Identification of a receptor for the morphogen retinoic acid
Giguere, V., Ong, E. S., Segui, P., & Evans, R. M. (1987) · Nature · doi:10.1038/330624a0 · Cited by 1,965
9-cis retinoic acid is a high affinity ligand for the retinoid X receptor
Heyman, R. A., Mangelsdorf, D. J., Dyck, J. A., Stein, R. B., Eichele, G., Evans, R. M., & Thaller, C. (1992) · Cell · doi:10.1016/0092-8674(92)90479-v · Cited by 1,780
Self-citationOro, A. E., McKeown, M., & Evans, R. M. (1990) · Nature · doi:10.1038/347298a0 · Cited by 406
Cited by
An oxysterol signalling pathway mediated by the nuclear receptor LXRα
Janowski, B. A., Willy, P. J., Devi, T. R., Falck, J. R., & Mangelsdorf, D. J. (1996) · Nature · doi:10.1038/383728a0 · Cited by 1,591
Self-citationLXR, a nuclear receptor that defines a distinct retinoid response pathway.
Willy, P. J., Umesono, K., Ong, E. S., Evans, R. M., Heyman, R. A., & Mangelsdorf, D. J. (1995) · Genes & Development · doi:10.1101/gad.9.9.1033 · Cited by 1,123
Self-citationNew insecticides with ecdysteroidal and juvenile hormone activity
Dhadialla, T. S., Carlson, G. R., & Le, D. P. (1998) · Annual Review of Entomology · doi:10.1146/annurev.ento.43.1.545 · Cited by 912
Environmental Signaling: What Embryos and Evolution Teach Us About Endocrine Disrupting Chemicals
McLachlan, J. A. (2001) · Endocrine Reviews · doi:10.1210/edrv.22.3.0432 · Cited by 608
Ecdysone receptors and their biological actions
Riddiford, L. M., Cherbas, P., & Truman, J. W. (2000) · Vitamins & Hormones · doi:10.1016/s0083-6729(00)60016-x · Cited by 605
Metadata
- Authors
- Harmon, M. A., Boehm, M. F., Heyman, R. A., & Mangelsdorf, D. J.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 1995-06-20
- Volume
- 92
- Issue
- 13
- Pages
- 6157-6160
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W2024051621
- Cited by
- 240
- References
- 3
- FWCI
- 3.91
- Type
- journal article
- Language
- en
- Open access
- green
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- Harmon, M. A., Boehm, M. F., Heyman, R. A., & Mangelsdorf, D. J. (1995). Activation of mammalian retinoid X receptors by the insect growth regulator methoprene. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.92.13.6157
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