Truxillic acid derivatives act as peroxisome proliferator-activated receptor γ activators

Ramona Steri; Matthias Rupp; Ewgenij Proschak; Timon Schroeter; Heiko Zettl; Katja Hansen; Oliver Schwarz; Lutz Müller-Kuhrt; Klaus Robert Müller; Gisbert Schneider; Manfred Schubert-Zsilavecz

doi:10.1016/j.bmcl.2010.03.026

Truxillic acid derivatives act as peroxisome proliferator-activated receptor γ activators

Ramona Steri, Matthias Rupp, Ewgenij Proschak, Timon Schroeter, Heiko Zettl, Katja Hansen, Oliver Schwarz, Lutz Müller-Kuhrt, Klaus Robert Müller, Gisbert Schneider, Manfred Schubert-Zsilavecz

Research output: Contribution to journal › Article › peer-review

12 Citations (Scopus)

Abstract

In previous studies, we identified a truxillic acid derivative as selective activator of the peroxisome proliferator-activated receptor γ, which is a member of the nuclear receptor family and acts as ligand-activated transcription factor of genes involved in glucose metabolism. Herein we present the structure-activity relationships of 16 truxillic acid derivatives, investigated by a cell-based reporter gene assay guided by molecular docking analysis.

Original language	English
Pages (from-to)	2920-2923
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	9
DOIs	https://doi.org/10.1016/j.bmcl.2010.03.026
Publication status	Published - 2010 May 1

Bibliographical note

Funding Information:
We gratefully acknowledge financial support from the Else-Kroener-Fresenius-Stiftung, FIRST (Frankfurt International Research School for Translational Biomedicine) and Lipid Signaling Forschungszentrum Frankfurt (LiFF) . We are grateful to the Chemical Computing Group for a research license of MOE.

Keywords

Molecular docking
Nuclear receptors
PPARγ
Reporter gene assay
Structure-activity relationships
Truxillic acid derivatives

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2010.03.026

Cite this

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title = "Truxillic acid derivatives act as peroxisome proliferator-activated receptor γ activators",

abstract = "In previous studies, we identified a truxillic acid derivative as selective activator of the peroxisome proliferator-activated receptor γ, which is a member of the nuclear receptor family and acts as ligand-activated transcription factor of genes involved in glucose metabolism. Herein we present the structure-activity relationships of 16 truxillic acid derivatives, investigated by a cell-based reporter gene assay guided by molecular docking analysis.",

keywords = "Molecular docking, Nuclear receptors, PPARγ, Reporter gene assay, Structure-activity relationships, Truxillic acid derivatives",

author = "Ramona Steri and Matthias Rupp and Ewgenij Proschak and Timon Schroeter and Heiko Zettl and Katja Hansen and Oliver Schwarz and Lutz M{\"u}ller-Kuhrt and M{\"u}ller, {Klaus Robert} and Gisbert Schneider and Manfred Schubert-Zsilavecz",

note = "Funding Information: We gratefully acknowledge financial support from the Else-Kroener-Fresenius-Stiftung, FIRST (Frankfurt International Research School for Translational Biomedicine) and Lipid Signaling Forschungszentrum Frankfurt (LiFF) . We are grateful to the Chemical Computing Group for a research license of MOE.",

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doi = "10.1016/j.bmcl.2010.03.026",

language = "English",

volume = "20",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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T1 - Truxillic acid derivatives act as peroxisome proliferator-activated receptor γ activators

AU - Steri, Ramona

AU - Rupp, Matthias

AU - Proschak, Ewgenij

AU - Schroeter, Timon

AU - Zettl, Heiko

AU - Hansen, Katja

AU - Schwarz, Oliver

AU - Müller-Kuhrt, Lutz

AU - Müller, Klaus Robert

AU - Schneider, Gisbert

AU - Schubert-Zsilavecz, Manfred

N1 - Funding Information: We gratefully acknowledge financial support from the Else-Kroener-Fresenius-Stiftung, FIRST (Frankfurt International Research School for Translational Biomedicine) and Lipid Signaling Forschungszentrum Frankfurt (LiFF) . We are grateful to the Chemical Computing Group for a research license of MOE.

PY - 2010/5/1

Y1 - 2010/5/1

N2 - In previous studies, we identified a truxillic acid derivative as selective activator of the peroxisome proliferator-activated receptor γ, which is a member of the nuclear receptor family and acts as ligand-activated transcription factor of genes involved in glucose metabolism. Herein we present the structure-activity relationships of 16 truxillic acid derivatives, investigated by a cell-based reporter gene assay guided by molecular docking analysis.

AB - In previous studies, we identified a truxillic acid derivative as selective activator of the peroxisome proliferator-activated receptor γ, which is a member of the nuclear receptor family and acts as ligand-activated transcription factor of genes involved in glucose metabolism. Herein we present the structure-activity relationships of 16 truxillic acid derivatives, investigated by a cell-based reporter gene assay guided by molecular docking analysis.

KW - Molecular docking

KW - Nuclear receptors

KW - PPARγ

KW - Reporter gene assay

KW - Structure-activity relationships

KW - Truxillic acid derivatives

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DO - 10.1016/j.bmcl.2010.03.026

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AN - SCOPUS:77950858472

SN - 0960-894X

VL - 20

SP - 2920

EP - 2923

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 9

ER -

Truxillic acid derivatives act as peroxisome proliferator-activated receptor γ activators

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

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