Department of Biology, Wake Forest University, Winston-Salem, North Carolina 27109, USA.
Annu Rev Entomol. 2012;57:83-106. doi: 10.1146/annurev-ento-120710-100607. Epub 2011 Oct 10.
The nuclear receptors (NRs) of metazoans are an ancient family of transcription factors defined by conserved DNA- and ligand-binding domains (DBDs and LBDs, respectively). The Drosophila melanogaster genome project revealed 18 canonical NRs (with DBDs and LBDs both present) and 3 receptors with the DBD only. Annotation of subsequently sequenced insect genomes revealed only minor deviations from this pattern. A renewed focus on functional analysis of the isoforms of insect NRs is therefore required to understand the diverse roles of these transcription factors in embryogenesis, metamorphosis, reproduction, and homeostasis. One insect NR, ecdysone receptor (EcR), functions as a receptor for the ecdysteroid molting hormones of insects. Researchers have developed nonsteroidal ecdysteroid agonists for EcR that disrupt molting and can be used as safe pesticides. An exciting new technology allows EcR to be used in chimeric, ligand-inducible gene-switch systems with applications in pest management and medicine.
真核生物的核受体 (NRs) 是一个古老的转录因子家族，其特征是具有保守的 DNA 和配体结合结构域（分别为 DBD 和 LBD）。果蝇基因组计划揭示了 18 种典型的 NR（均具有 DBD 和 LBD）和 3 种仅具有 DBD 的受体。随后对测序昆虫基因组的注释表明，这种模式仅存在微小的偏差。因此，需要重新关注昆虫 NR 异构体的功能分析，以了解这些转录因子在胚胎发生、变态、繁殖和体内平衡中的多种作用。一种昆虫核受体，蜕皮激素受体 (EcR)，作为昆虫蜕皮激素蜕皮激素的受体发挥作用。研究人员已经开发出非甾体蜕皮激素激动剂用于 EcR，可破坏蜕皮并可用作安全的杀虫剂。一项令人兴奋的新技术允许 EcR 与嵌合、配体诱导的基因开关系统一起使用，可应用于害虫管理和医学领域。
