2012
DOI: 10.1016/j.steroids.2012.02.021
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Dissecting rapid estrogen signaling with conjugates

Abstract: Hypothesizing that rapid estrogen signaling could be modulated from different estrogen receptors with unique localization patterns, a number of groups have attempted to design drug conjugates that target or restrict compounds to specific subcellular compartments. This article will briefly discuss the history of using conjugates to dissect rapid estrogen signaling and different strategies to attempt to target estrogens and antiestrogens to different locations. It will also detail some of the potential issues th… Show more

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Cited by 7 publications
(6 citation statements)
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“…In general, three design strategies have been employed: 1) conjugation to large proteins, such as bovine serum albumin (E2-BSA); (2) attachment to oligomeric/polymeric dendrimers (E2-PAMAM) or cyclodextrins; and (3) ionic E2 derivatives (E2-NMe 3 + ). The use and cautionary experimental considerations for the use of conjugates to investigate rapid E2 signaling was recently reviewed (Shearer et al, 2012).…”
Section: Membrane-impermeable Estrogen Probesmentioning
confidence: 99%
“…In general, three design strategies have been employed: 1) conjugation to large proteins, such as bovine serum albumin (E2-BSA); (2) attachment to oligomeric/polymeric dendrimers (E2-PAMAM) or cyclodextrins; and (3) ionic E2 derivatives (E2-NMe 3 + ). The use and cautionary experimental considerations for the use of conjugates to investigate rapid E2 signaling was recently reviewed (Shearer et al, 2012).…”
Section: Membrane-impermeable Estrogen Probesmentioning
confidence: 99%
“…BSA-conjugated steroids have often been used in rapid signaling studies because the large structure prevents hormones from crossing the plasma membrane, thereby ensuring that the hormone exclusively binds to and activates pathways originating from membrane receptors. However, BSA itself may interfere with the biological activity of cell signaling pathways [52]. Further, the conformation of BSA may lead to interference of the lipid rafts at the point of mNR localization [53].…”
Section: Approachesmentioning
confidence: 99%
“…Finally, other studies note that BPA exposure elicits a rapid (i.e. within 15 min of exposure) and potent estrogenic effects via nonclassical estrogen-triggered pathways (Alonso-Magdalena et al 2012, Shearer et al 2012.…”
Section: Selection Of Bpa As a Model Compoundmentioning
confidence: 99%