1z5x

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{{STRUCTURE_1z5x| PDB=1z5x | SCENE= }}
{{STRUCTURE_1z5x| PDB=1z5x | SCENE= }}
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'''hemipteran ecdysone receptor ligand-binding domain complexed with ponasterone A'''
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===hemipteran ecdysone receptor ligand-binding domain complexed with ponasterone A===
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==Overview==
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The ecdysone receptor is a hormone-dependent transcription factor that plays a central role in regulating the expression of vast networks of genes during development and reproduction in the phylum Arthropoda. The functional receptor is a heterodimer of the two nuclear receptor proteins ecdysone receptor (EcR) and ultraspiracle protein. The receptor is the target of the environmentally friendly bisacylhydrazine insecticides, which are effective against Lepidoptera but not against Hemiptera or several other insect orders. Here we present evidence indicating that much of the selectivity of the bisacylhydrazine insecticides can be studied at the level of their binding to purified ecdysone receptor ligand-binding domain (LBD) heterodimers. We report the crystal structure of the ecdysone receptor LBD heterodimer of the hemipteran Bemisia tabaci (Bt, sweet potato whitefly) in complex with the ecdysone analogue ponasterone A. Although comparison with the corresponding known LBD structure from the lepidopteran Heliothis virescens (Hv) ecdysone receptor revealed the overall mode of ponasterone A binding to be very similar in the two cases, we observed that the BtEcR ecdysteroid-binding pocket is structured differently to that of HvEcR in those parts that are not in contact with ponasterone A. We suggest that these differences in the ligand-binding pocket may provide a molecular basis for the taxonomic order selectivity of bisacylhydrazine insecticides.
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(as it appears on PubMed at http://www.pubmed.gov), where 15809296 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15809296}}
==About this Structure==
==About this Structure==
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[[Category: Ponasterone some]]
[[Category: Ponasterone some]]
[[Category: Usp]]
[[Category: Usp]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 17:12:43 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 14:51:26 2008''

Revision as of 11:51, 28 July 2008

Image:1z5x.png

Template:STRUCTURE 1z5x

hemipteran ecdysone receptor ligand-binding domain complexed with ponasterone A

Template:ABSTRACT PUBMED 15809296

About this Structure

Full crystallographic information is available from OCA.

Reference

The X-ray structure of a hemipteran ecdysone receptor ligand-binding domain: comparison with a lepidopteran ecdysone receptor ligand-binding domain and implications for insecticide design., Carmichael JA, Lawrence MC, Graham LD, Pilling PA, Epa VC, Noyce L, Lovrecz G, Winkler DA, Pawlak-Skrzecz A, Eaton RE, Hannan GN, Hill RJ, J Biol Chem. 2005 Jun 10;280(23):22258-69. Epub 2005 Apr 4. PMID:15809296

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