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Synthesis and Biological Evaluation of a Novel Series of G Protein‐Coupled Estrogen Receptor Antagonists for The Treatment of Gallstone Disease
Author(s) -
DeLeon Chlelsea,
Wilhelm McKenna,
Sweeney Patrick,
Arnatt Christopher
Publication year - 2017
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.31.1_supplement.lb599
Subject(s) - gper , estrogen , disease , medicine , estrogen receptor , gallbladder disease , laparoscopic cholecystectomy , antagonist , gallbladder , bioinformatics , receptor , biology , surgery , breast cancer , cancer
The prevalence of gallstone disease is a major public health issue globally. While laparoscopic cholecystectomy is the current standard of treatment, new research suggests that medicinal therapy may offer a non‐surgical option for patients with a functioning gallbladder. The G protein‐coupled estrogen receptor (GPER) is known to induce gallstone formation in response to 17b‐Estradiol (E2) treatment. Therefore, the design of GPER antagonist may significantly reduce gallstone formation and enable non‐surgical management of gallstone disease. Using a computational homology model of GPER, a novel series of antagonists were designed and synthesized. An original high‐throughput screening (HTS) biochemical assay was designed to analyze GPER activity. Preliminary results show no agonism of intended GPER antagonists. Support or Funding Information Saint Louis University