Bicyclo[2.2.2]octanes: close structural mimics of the nuclear receptor-binding motif of steroid receptor coactivators.

Bicyclo[2.2.2]octanes: close structural mimics of the nuclear receptor-binding motif of steroid receptor coactivators. Research Abstract Details 

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Bicyclo[2.2.2]octanes: close structural mimics of the nuclear receptor-binding motif of steroid receptor coactivators. Abstract Text:

Hai-Bing Zhou,Margaret L Collins,Jillian R Gunther,John S Comninos,John A Katzenellenbogen,

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.

Bicyclo[2.2.2]octanes: close structural mimics of the nuclear receptor-binding motif of steroid receptor coactivators. Publishing Authors By Initials

HB Zhou,ML Collins,JR Gunther,JS Comninos,JA Katzenellenbogen,

For similar proteins: transcription factors research abstracts see: proteins: transcription factors research

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Bicyclo[2.2.2]octanes: close structural mimics of the nuclear receptor-binding motif of steroid receptor coactivators. Journal Published:

PUBLICATION TYPE: Research Support, U.S. Gov't,

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 17

Page Numbers: 4118-22

Journal Abbreviation: Bioorg. Med. Chem. Lett.

ISSN: 0960-894X

DAY: 23

MONTH: 05

YEAR: 2007

Bicyclo[2.2.2]octanes: close structural mimics of the nuclear receptor-binding motif of steroid receptor coactivators. Information

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LANGUAGE: eng

NlmUniqueID: 9107377

Bicyclo[2.2.2]octanes: close structural mimics of the nuclear receptor-binding motif of steroid receptor coactivators. Keywords Mesh Terms:

KEYWORDS: Transcription Factors

MESH TERMS: metabolism

Chemical & Substance for Abstract: Bicyclo[2.2.2]octanes: close structural mimics of the nuclear receptor-binding motif of steroid receptor coactivators. Information

Substance Name: nuclear receptor coactivator 1

Registry Number: EC 2.3.1.48

Grant and Affiliation Information for Bicyclo[2.2.2]octanes: close structural mimics of the nuclear receptor-binding motif of steroid receptor coactivators.

AFFILIATION: Department of Chemistry, University of Illinois, 600 South Mathews Avenue, Urbana, IL 61801, USA.

Country: England

AGENCY: United States NIDDK

GRANT: 5R37 DK15556

ACRONYM: DK

MEDLINETA: Bioorg Med Chem Lett

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