Structurally similar estradiol analogs uniquely alter the regulation of intracellular signaling pathways.

ABSTRACT: Ligand structure can affect the activation of nuclear receptors, such as estrogen receptors (ERs), and their control of signaling pathways for cellular responses including death and differentiation. We hypothesized that distinct biological functions of similar estradiol (E(2)) analogs could be identified by integrating gene expression patterns obtained from human tumor cell lines with receptor binding and functional data for the purpose of developing compounds for treatment of a variety of diseases. We compared the estrogen receptor subtype selectivity and impact on signaling pathways for three distinct, but structurally similar, analogs of E(2). Modifications in the core structure of E(2) led to pronounced changes in subtype selectivity for estrogen receptors, ER-α or ER-β, along with var

SUBMITTER: Yarger JG 

PROVIDER: S-EPMC3535725 | biostudies-literature | 2013 Feb

REPOSITORIES: biostudies-literature