The identification of cellular targets of 17beta estradiol using a lytic (T7) cDNA phage display approach.

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Van Dorst B, Mehta J, Rouah-Martin E, De Coen W, Blust R, Robbens J

The identification of cellular targets of 17beta estradiol using a lytic (T7) cDNA phage display approach.

Toxicol In Vitro. 2011 Feb;25(1):388-93. doi: 10.1016/j.tiv.2010.10.012. Epub 2010 Oct 27.

PubMed ID
21034808 [ View in PubMed
]
Abstract

To unravel the mechanism of action of chemical compounds, it is crucial to know their cellular targets. A novel in vitro tool that can be used as a fast, simple and cost effective alternative is cDNA phage display. This tool is used in our study to select cellular targets of 17beta estradiol (E2). It was possible to select two potential cellular targets of E2 out of the T7 Select Human Breast cDNA phage library. The selected cellular targets, autophagy/beclin-1 regulator 1 (beclin 1) and ATP synthase F(0) subunit 6 (ATP6) have so far been unknown as binding proteins of E2. To confirm the E2 binding properties of these selected proteins, surface plasmon resonance (SPR) was used. With SPR the K(d) values were determined to be 0.178+/-0.031 and 0.401+/-0.142 nM for the ATP6 phage and beclin 1 phage, respectively. These K(d) values in the low nM range verify that the selected cellular proteins are indeed binding proteins for E2. The selection and identification of these two potential cellular targets of E2, can enhance our current understanding of its mechanism of action. This illustrates the potential of lytic (T7) cDNA phage display in toxicology, to provide important information about cellular targets of chemical compounds.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
EstradiolATP synthase subunit aProteinHumans
Unknown
Inhibitor
Details
EstradiolBeclin-1ProteinHumans
Unknown
Binder
Details
Estradiol acetateATP synthase subunit aProteinHumans
Unknown
Not AvailableDetails
Estradiol acetateBeclin-1ProteinHumans
Unknown
Not AvailableDetails
Estradiol benzoateATP synthase subunit aProteinHumans
Unknown
Not AvailableDetails
Estradiol benzoateBeclin-1ProteinHumans
Unknown
Not AvailableDetails
Estradiol cypionateATP synthase subunit aProteinHumans
Unknown
Not AvailableDetails
Estradiol cypionateBeclin-1ProteinHumans
Unknown
Not AvailableDetails
Estradiol dienanthateATP synthase subunit aProteinHumans
Unknown
Not AvailableDetails
Estradiol dienanthateBeclin-1ProteinHumans
Unknown
Not AvailableDetails
Estradiol valerateATP synthase subunit aProteinHumans
Unknown
Not AvailableDetails
Estradiol valerateBeclin-1ProteinHumans
Unknown
Not AvailableDetails