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Ligand

Ecdysteroids (EcR)

Ecdysteroids are insect moulting and sex hormones which include ecdysone and its homologues such as 20-hydroxyecdysone. Ecdysteroids also occur in other invertebrates where they can play a different role. They also appear in many plants mostly as a protection agents (toxins or antifeedants) against herbivore insects. These phytoecdysteroids have medicinal value and are part of herbal adaptogenic remedies like cordyceps.

Physiological effects of EcR

Pulses of 20-hydroxyecdysone occur during insect development, whereupon this hormone binds to the ecdysone receptor, a ligand-activated transcription factor found in the nuclei of insect cells. This in turn leads to the activation of many other genes, as evidenced by chromosomal puffing at over a hundred sites. Ultimately the activation cascade causes physiological changes that result in ecdysis (moulting).

Potential applications of EcR LBD

EcR LBD can be fused with different DBDs in order to activate downstream gene expression depending on the binding site of the DBD.

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