Work

Synthesis of Biphenyl Proteomimetics as Estrogen Receptor-α Coactivator Binding Inhibitors

Year: 2009

Type: article

Abstract: A novel series of biphenyl proteomimetic compounds were designed as estrogen receptor-alpha (ER(alpha)) coactivator binding inhibitors. Synthesis was accomplished through a convergent approach, employing Suzuki coupling chemistry to ligate the individual modular units. Initial biological results support the ability of these compounds to compete for the ER(alpha) coactivator binding groove.

Source: Organic Letters

DOI: 10.1021/ol901999f

Authors: Anna B. Williams, Patrick T. Weiser, Robert N. Hanson, Jillian R. Gunther, John A. Katzenellenbogen

Institutions: Northeastern University, University of Illinois Urbana-Champaign

Language: English

Topic: Estrogen and related hormone effects

Subfield: Genetics

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

Open Access status: green

Funders: National Institute of General Medical Sciences, National Institute of Diabetes and Digestive and Kidney Diseases, National Institute of Environmental Health Sciences

Awards: MOLECULAR PROBES FOR STEROID RECEPTORS, Novel Ligands and Mechanisms to Achieve Selective Nuclear Receptor Activity, Dimensions in Endocrine Disruption: Altering Receptor Coregulator Interactions, Training Program at the Chemistry-Biology Interface