Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 15, Pages 4118-4122Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.05.058
Keywords
steroid receptor coactivators; coactivator-binding inhibitors; bicyclo[2.2.2]octanes; estrogen receptor
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Funding
- NIDDK NIH HHS [R01 DK015556, R37 DK015556, R37 DK015556-42, 5R37 DK15556] Funding Source: Medline
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Nuclear hormone receptor (NR) function relies on association of agonist-bound receptors with steroid receptor coactivator (SRC) proteins through a small pentapeptide motif (LXXLL) of the SRC that binds to a hydrophobic groove on the NR. We have synthesized a series of bicyclo[2.2.2]octanes that are close structural mimics of the two key leucine residues of this SRC sequence as bound in the hydrophobic groove of the estrogen receptor. These bicyclic systems block the NR-SRC interaction with modest potency. (c) 2007 Elsevier Ltd. All rights reserved.
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